Synthesis and evaluation of 2-phenylamino-1, 4-naphthoquinones derivatives as potential hypoglycaemic agents / Síntese e avaliação de derivados de 2-fenilamino-1, 4-naftoquinonas como potenciais agentes hipoglicemiantes

Due to the severe side effects revealed by most of the currently used antidiabetic medicines, search for finding new and safe drugs to manage diabetes is continued. Naphthoquinones possessing strong antioxidant properties have been employed as candidates for diabetes therapy. Present study is aimed at finding the antioxidant and hypoglycaemic potential of some novel derivatives of 2-phenylamino-1,4-naphthoquinones (PAN) including chloro, nitro, methyl and bromo (5a-d) derivatives synthesized by single pot experiment. Product crystals were purified by TLC and characterized by FT-IR. The antioxidant potential of the compounds was assayed through DPPH radical scavenging and reducing power activities noted as UV-vis. absorbance. The DPPH assay has showed the powerful antioxidant activity of nitro and bromo derivatives, while the nitro derivative showed the significant reduction potential towards FRAP assay. Hypoglycaemic potential of the compounds was studied in rat animal model. All synthesized compounds revealed better hypoglycaemic activity; however, the chloro-derivative exhibited the more potent hypoglycaemic activity showing about 43% reduction in the mean blood glucose levels of the treated animals. As the bioreduction of naphthoquinones may be influenced by changing its redox properties, it has been noticed that the e-donating resonance effect (+R) of 'chloro' group has shown the significant effects on biological activity through stabalization of its imine form which limits the potential of generation of free radicals during bioreduction of quinones and thus has been proposed as the reason of its hypoglycaemic activity. Future studies employing the properties of e-donating groups of PAN may optimize the drug-receptor interaction for better drug designing and drug development strategies against diabetes and also for the clinical trials.

Em razão dos graves efeitos colaterais causados pela maioria dos medicamentos antidiabéticos atualmente utilizados, continua a busca por novos medicamentos seguros para o controle do diabetes. As naftoquinonas, que possuem fortes propriedades antioxidantes, têm sido empregadas como candidatas à terapia do diabetes. O presente estudo visa encontrar o potencial antioxidante e hipoglicemiante de alguns novos derivados de 2-fenilamino-1,4-naftoquinonas (PAN), incluindo derivados de cloro, nitro, metil e bromo (5a-d) sintetizados por experimento em pote único. Os cristais do produto foram purificados por TLC e caracterizados por FT-IR. O potencial antioxidante dos compostos foi testado por meio de atividades de sequestro de radicais DPPH e redução de energia observada como absorção no UV-vis. O ensaio DPPH mostrou a poderosa atividade antioxidante dos derivados nitro e bromo, enquanto o derivado nitro mostrou o potencial de redução significativo para o ensaio FRAP. O potencial hipoglicêmico dos compostos foi estudado em modelo animal de rato. Todos os compostos sintetizados revelaram melhor atividade hipoglicemiante; no entanto, o derivado cloro apresentou atividade hipoglicêmica mais potente, com redução de 43% nos níveis médios de glicose no sangue dos animais tratados. Como a biorredução de naftoquinonas pode ser influenciada pela alteração de suas propriedades redox, notou-se que o efeito da doação eletrônica por ressonância (+R) do grupo "cloro" tem sido significativo na atividade biológica por meio da estabilização de sua forma imina, que limita o potencial de geração de radicais livres durante a biorredução de quinonas, e, portanto, tem sido proposto como a razão de sua atividade hipoglicemiante. Estudos futuros empregando as propriedades de grupos de doação eletrônica de PAN podem otimizar a interação droga-receptor para melhor planejamento de medicamentos e estratégias de desenvolvimento de medicamentos contra o diabetes e também para os ensaios clínicos.

Metformin Inhibits ROS/TNF-alpha Axis-Mediated Chronic Kidney Disease Induced by TAA Independent of Leukocyte Infiltration in Association with the Inhibition of Kidney Injury Biomarkers / La Metformina Inhibe la Enfermedad Renal Crónica Mediada por el Eje ROS/TNF-alfa Inducida por TAA Independientemente de la Infiltración de Leucocitos en Asociación con la Inhibición de Biomarcadores de Lesión Renal

SUMMARY: The toxic effects of thioacetamide (TAA) and carbon tetrachloride on the human body are well recognized. In this study, we examined whether TAA intoxication can induce kidney leukocyte infiltration (measured as leukocyte common antigen CD45) associated with the augmentation of the reactive oxygen species (ROS)/tumor necrosis factor-alpha (TNF-α) axis, as well as biomarkers of kidney injury with and without metformin treatment. Rats were either injected with TAA (200 mg/kg; twice a week for 8 weeks) before being sacrificed after 10 weeks (experimental group) or were pre-treated with metformin (200 mg/kg) daily for two weeks prior to TAA injections and continued receiving both agents until the end of the experiment, at week 10 (protective group). Using basic histology staining, immunohistochemistry methods, and blood chemistry analysis, we observed profound kidney tissue injury such as glomerular and tubular damage in the experimental group, which were substantially ameliorated by metformin. Metformin also significantly (p0.05) increase in kidney expression of CD45 positive immunostaining cells. In conclusion, we found that TAA induces kidney injury in association with the augmentation of ROS/TNF-α axis, independent of leukocyte infiltration, which is protected by metformin.

Son bien conocidosos los efectos tóxicos de la tioacetamida (TAA) y el tetracloruro de carbono en el cuerpo humano. En este estudio, examinamos si la intoxicación por TAA puede inducir la infiltración de leucocitos renales (medida como antígeno leucocitario común CD45) asociada con el aumento de las especies reactivas de oxígeno (ROS)/factor de necrosis tumoral-alfa (TNF-α), así como biomarcadores de daño renal con y sin tratamiento con metformina. A las ratas se les inyectó TAA (200 mg/kg; dos veces por semana durante 8 semanas) antes de sacrificarlas a las 10 semanas (grupo experimental) o se les pretrató con metformina (200 mg/kg) diariamente durante dos semanas antes de las inyecciones de TAA y continuaron recibiendo ambos agentes hasta el final del experimento, en la semana 10 (grupo protector). Usando tinción histológica básica, métodos de inmunohistoquímica y análisis químico de la sangre, observamos una lesión profunda del tejido renal, como daño glomerular y tubular en el grupo experimental, que mejoraron sustancialmente con la metformina. La metformina también inhibió significativamente (p0,05) en la expresión renal de células de inmunotinción positivas para CD45. En conclusión, encontramos que el TAA induce la lesión renal en asociación con el aumento del eje ROS/TNF-α, independientemente de la infiltración de leucocitos, que está protegida por metformina.

Compuestos bioactivos de canela y su efecto en la disminución del síndrome metabólico: revisión sistemática / Bioactive compounds of cinnamon and their effect on decreasing metabolic syndrome: systematic review

Introducción. El síndrome metabólico (SM) aumenta el ingreso hospitalario y el riesgo de desarrollar COVID-19, los fármacos utilizados para su tratamiento ocasionan efectos secundarios por lo que se ha optado por la búsqueda de alternativas terapéuticas a base de compuestos bioactivos contenidos en plantas medicinales. La canela se utiliza como agente terapéutico debido a sus propiedades comprobadas con diversos mecanismos de acción reportados en el tratamiento de varias patologías. Objetivo. Documentar los estudios in vitro, in vivo, estudios clínicos y los mecanismos de acción reportados del efecto de la administración de extractos y polvo de canela en las comorbilidades relacionadas con el SM. Materiales y métodos. Revisión sistemàtica de artículos en bases de datos electrónicas, incluyendo estudios de canela en polvo, extractos acuosos, de acetato de etilo y metanol de la corteza de canela, período de 5 años, excluyendo todo artículo relacionado a su efecto antimicrobiano, antifúngico y aceite de canela. Resultados. Las evidencias de los principales compuestos bioactivos contenidos en la canela validan su potencial en el tratamiento de enfermedades relacionadas al SM, con limitados estudios que indagan en los mecanismos de acción correspondientes a sus actividades biológicas. Conclusiones. Las evidencias de las investigaciones validan su potencial en el tratamiento de estas patologías, debido a sus principales compuestos bioactivos: cinamaldehído, transcinamaldehído, ácido cinámico, eugenol y, antioxidantes del tipo proantocianidinas A y flavonoides, los cuales participan en diversos mecanismos de acción que activan e inhiben enzimas, con efecto hipoglucemiante (quinasa y fosfatasa), antiobesogénico (UPC1), antiinflamatorio (NOS y COX), hipolipemiante (HMG-CoA) y antihipertensivo (ECA)(AU)

Introduction. Metabolic syndrome (MS) increases hospital admission and the risk of developing COVID-19. Due to the side effects caused by the drugs used for its treatment, the search for therapeutic alternatives based on bioactive compounds contained in medicinal plants has been chosen. Cinnamon is used as a therapeutic agent due to its proven properties with various mechanisms of action reported in the treatment of various pathologies. Objective. To document the in vitro and in vivo studies, clinical studies and the mechanisms of action reported on the effect of the administration of cinnamon extracts and powder on comorbidities related to MS. Materials and methods. Systematic review of articles in electronic databases, including studies of cinnamon powder, aqueous extracts, ethyl acetate and methanol from cinnamon bark, over a period of 5 years, excluding all those articles related to its antimicrobial, antifungal and antimicrobial effect. cinnamon oil. Results. The evidence of the main bioactive compounds contained in cinnamon validates its potential in the treatment of diseases related to MS, with limited studies that investigate the mechanisms of action corresponding to its biological activities. Conclusions. Research evidence validates its potential in the treatment of these pathologies, due to its main bioactive compounds: cinnamaldehyde, transcinnamaldehyde, cinnamic acid, eugenol, and antioxidants of the proanthocyanidin A type and flavonoids, which participate in various mechanisms of action that activate and they inhibit enzymes, with hypoglycemic (kinase and phosphatase), antiobesogenic (UPC1), anti-inflammatory (NOS and COX), lipid-lowering (HMG-CoA) and antihypertensive (ACE) effects(AU)

Study of antidiabetic activity of two novel Schiff base derived dibromo and dichloro substituted compounds in streptozotocin-nicotinamide-induced diabetic rats: pilot study

Abstract Schiff bases are aldehyde-or ketone-like chemical compounds in which an imine or azomethine group replaces the carbonyl group. Such compounds show various beneficial biological activities, such as anti-inflammation and antioxidants. The present study addresses comprehensiveevaluation of antidiabetic effect of two novel dibromides and dichlorides substituted Schiff bases substituted Schiff bases (2,2'-[1,2-cyclohexanediylbis (nitriloethylidyne)]bis[4-chlorophenol] (CNCP) and 2, 2'-[1,2-cyclohexanediylbis(nitriloethylidyne)]bis[4-bromophenol] (CNBP) with two different doses, high (LD) and low (LD) in streptozotocin and nicotinamide induced diabetic rats. The rats were separated into normal, untreated, treated and reference groups. Except for the normal group, diabetes traits were induced in the rest animals. Insulin level was measured, and the effect of the compounds on biochemical parameters of liver function and lipid profile were evaluated. High glucose and decreased insulin level are observed in the groups. The histological evaluation confirms that the hepatic architecture in the treated animals with a low dose of CNCP is quite similar to that of the normal hepatic structure and characterized by normal central vein, hepatocytes without any fatty alterations and mild red blood cell infiltration. CNCP (LD) and CNBP (HD) are more successful in enhancing cell survival in the diabetic rat's liver and can be responsible for causing much healthier structure and notable morphology improvement.

Awareness of the diagnosis, treatment, and control of diabetes mellitus in Brazil / Conhecimento do diagnóstico, tratamento e controle do diabetes mellitus no Brasil

ABSTRACT OBJECTIVE To estimate the proportions of awareness, treatment, and control of diabetes mellitus (DM) in the Brazilian adult population. METHOD This is a cross-sectional study, with data from a representative sample of the Brazilian population, taken from the National Health Survey(PNS 2014/2015). Outcomes were defined based on glycated hemoglobin (HbA1c) measurements, self-reported DM diagnosis, and use of hypoglycemic agents or insulin. The proportion of DM awareness, treatment, and control was estimated according to sociodemographic characteristics, health conditions, and access to health services, and their respective 95% confidence intervals. RESULTS DM prevalence in the Brazilian population was of 8.6% (95%CI: 7.8-9.3): 68.2% (95%CI: 63.9-72.3) were aware of their diagnosis, 92.2% (95%CI: 88.6-94.7) of those who were aware were undergoing drug treatments, and, of these, 35.8% (95%CI: 30.5-41.6) had controlled HbA1c levels. The proportions of DM awareness, control, and treatment were lower in men aged 18 to 39 years, individuals with low education, without health insurance, and beneficiaries of the Bolsa Família program. CONCLUSION Approximately one in ten Brazilians has DM. A little more than half of this population is aware of their diagnosis, a condition measured by HbA1c dosage and clinical diagnosis. Among those who know, the vast majority are undergoing drug treatments. However, less than half of these have their HbA1c levels controlled. Worse scenarios were found in subgroups with high social vulnerability.

RESUMO OBJETIVO Estimar as proporções dos indivíduos que têm conhecimento do diagnóstico, tratamento e controle do diabetes mellitus (DM) na população adulta brasileira. MÉTODO Este é um estudo transversal, com dados de amostra representativa da população brasileira, provenientes da Pesquisa Nacional de Saúde (PNS 2014/2015). Os desfechos foram definidos com base na medida de hemoglobina glicada (HbA1c), no diagnóstico autorreferido de DM e no uso de hipoglicemiantes ou de insulina. Estimou-se a proporção do conhecimento, tratamento e controle do DM de acordo com as características sociodemográficas, condição de saúde e de acesso aos serviços de saúde, e seus respectivos intervalos de 95% de confiança (IC95%). RESULTADOS A prevalência de DM na população brasileira foi 8,6% (IC95% 7,8-9,3), 68,2% (IC95% 63,9-72,3) tinham conhecimento do seu diagnóstico, 92,2% (IC95% 88,6-94,7) dos que tinham conhecimento realizam tratamento medicamentoso, e desses, 35,8% (IC95% 30,5-41,6) tinham os níveis de HbA1c controlados. As proporções de conhecimento, controle e tratamento foram menores nos homens, com idade de 18 a 39 anos, indivíduos que possuem baixa escolaridade, sem plano de saúde e beneficiários do Programa Bolsa Família. CONCLUSÃO Aproximadamente um em cada dez brasileiros apresenta DM. Um pouco mais da metade desta população tem conhecimento do seu diagnóstico, condição aferida por dosagem de HbA1c e diagnóstico clínico. Entre os que sabem, a grande maioria está sob tratamento medicamentoso. Porém, menos da metade destes tem seus níveis de HbA1c controlados. Cenários piores foram encontrados em subgrupos com alta vulnerabilidade social.

Efficacy of acupuncture on cardiovascular complications in patients with diabetes mellitus in Korea: A nationwide retrospective cohort / 中西医结合学报

OBJECTIVE@#The main aim of this study is to investigate whether acupuncture could be an effective complementary treatment for reducing the risk of macrovascular complications in diabetic patients currently taking antidiabetic medications using a nationwide population-based database.@*METHODS@#We conducted a retrospective cohort study to assess the efficacy of acupuncture on cardiovascular complications in diabetic patients using data from patients between 40 and 79 years of age, newly diagnosed with diabetes between 2003 and 2006, found in the National Health Insurance Service-National Sample Cohort (NHIS-NSC) in Korea. From the data, we identified 21,232 diabetic patients who were taking antidiabetic medication between 2003 and 2006. The selected patients were divided into two groups-those who received acupuncture at least three times and those who received no acupuncture (non-acupuncture) in the year following their diagnosis of diabetes. After 1:1 propensity score matching (PSM), each group had 3350 patients, and the observation ceased at the occurrence of a major adverse cardiovascular event (MACE), which was defined as either myocardial infarction, stroke, or death due to cardiovascular cause.@*RESULTS@#After PSM, the acupuncture group had a lower incidence of MACE (hazard ratio [HR]: 0.87; 95% confidence interval [CI]: 0.81-0.94; P = 0.0003) and all-cause mortality (HR: 0.77; 95% CI: 0.70-0.84; P < 0.0001) than the non-acupuncture group; the HRs for stroke-related mortality (HR: 0.75; 95% CI: 0.56-1.00; P = 0.0485), ischemic heart disease mortality (HR: 0.53; 95% CI: 0.34-0.84; P = 0.006) and circulatory system disease mortality (HR: 0.67; 95% CI: 0.55-0.82; P < 0.0001) were lower in the acupuncture group than in the non-acupuncture group in the secondary analysis.@*CONCLUSION@#Our results indicate that diabetic patients receiving acupuncture treatment might have a lower risk of MACE, all-cause mortality and cardiovascular mortality. This population-based retrospective study suggests beneficial effects of acupuncture in preventing macrovascular complications associated with diabetes. These findings call for further prospective cohort or experimental studies on acupuncture treatment for cardiovascular complications of diabetes. Please cite this article as: Jung H, Won T, Kim GY, Jang J, Yeo S, Lim S. Efficacy of acupuncture on cardiovascular complications in patients with diabetes mellitus in Korea: A nationwide retrospective cohort. J Integr Med. 2023; 21(2): 176-183.

Chinese expert consensus on metformin in clinical practice: 2023 update / 中华内科杂志

Metformin has robust glucose-lowering effects and multiple benefits beyond hypoglycemic effects. It can also be used in combination with various hypoglycemic drugs and is cost effective. In the absence of the strong indications of glucagon like peptide-1 receptor agonist (GLP-1RA) or sodium glucose cotransporter 2 inhibitor (SGLT2i) for cardiorenal protection, metformin should be used as the first-line pharmacological treatment for newly diagnosed type 2 diabetes and the basic drug for the combined treatment of hypoglycemic drugs. Metformin does not increase the risk of liver and kidney function damage, but patients with renal dysfunction should adjust the dosage of metformin based on estimated glomerular filtration rate (eGFR) levels. Moreover, the correct use of metformin does not increase the risk of lactic acidosis. Because long-term use of metformin is associated with a decrease in vitamin B12 levels, patients with insufficient intake or absorption of vitamin B12 should be regularly monitored and appropriately supplemented with vitamin B12. In view of the new progress made in the basic and clinical research related to metformin, the consensus updating expert group updated the consensus on the basis of the Expert Consensus on the Clinical Application of Metformin (2018 Edition).

Physiochemical and nutritional evaluation of whole kumquat fruits powder and its protective effect on thyroid hormones and blood sugar levels in diabetic rats / Avaliação físico-química e nutricional de frutas inteiras de kumquat em pó e seu efeito protetor sobre os hormônios da tireoide e os níveis de açúcar no sangue em ratos diabéticos

The present study was conducted to evaluate the chemical composition, antioxidant activity and hypoglycemic effects of whole kumquat (Ku) powder in diabetic rats fed a high-fat-high-cholesterol (HFHC) diet. The antioxidant activities were evaluated using stable 1,1-diphenyl 2-picrylhydrazyl (DPPH) free radical scavenging method, 2,2'-azinobis (3-ethyl benzo thiazoline-6-sulphonic acid) radical cation (ABTS) and Ferric reducing antioxidant power (FRAP). Total phenolic content was (51.85 mg GAE/g) and total flavonoid content was (0.24 mg Cateachin Equivalent, CE/g). DPPH and ABTS values were 3.32 and 3.98 mg Trolox equivalent (TE)/g where FRAP value was 3.00 mM Fe²+/kg dry material. A total of 90 albino rats were used in the present study. Rats group were as follows: normal diet; normal treated (2, 4, and 6% Ku.), diabetic rats (non-treated), diabetic + HFHC diet (non-treated), HFHC (non-treated), Diabetic (treated), HFHC (treated) and Diabetic + HFHC (treated). The diets were followed for 8 weeks. Blood samples were collected at the end of the experiment. Serum glucose was recorded and thyroid hormones (T4, Thyroxine and T3, Triiodothyronine) were conducted. Diet supplemented with Kumquat at different concentrations have a hypoglycemic effect and improve the thyroid hormones of both diabetic rats and HFHC diabetic rats.

O presente estudo foi conduzido para avaliar a composição química, a atividade antioxidante e os efeitos hipoglicêmicos do pó de kumquat (Ku) em ratos diabéticos alimentados com uma dieta rica em gordura e colesterol (HFHC). As atividades antioxidantes foram avaliadas usando o método de eliminação de radicais livres de 1,1-difenil 2-picrilhidrazil (DPPH), 2,2'-azinobis (ácido 3-etilbenzotiazolina-6-sulfônico) radical cátion (ABTS) e antioxidante redutor férrico potência (FRAP). O conteúdo fenólico total foi (51,85 mg GAE / g) e o conteúdo total de flavonoides foi (0,24 mg Cateachin Equivalent, CE / g). Os valores de DPPH e ABTS foram 3,32 e 3,98 mg equivalente de Trolox (TE) / g, em que o valor de FRAP foi de 3,00 mM Fe²+ / kg de material seco. Um total de 90 ratos albinos foi usado no presente estudo. O grupo dos ratos foi o seguinte: dieta normal: tratados normais (2, 4 e 6% Ku.), ratos diabéticos (não tratados), diabéticos + dieta HFHC (não tratados), HFHC (não tratados), diabéticos (tratados), HFHC (tratados) e diabéticos + HFHC (tratados). As dietas foram seguidas por 8 semanas. Amostras de sangue foram coletadas ao final do experimento. A glicose sérica foi registrada e os hormônios tireoidianos (T4, Tiroxina e T3, Triiodotironina) foram conduzidos. A dieta suplementada com kumquat em diferentes concentrações tem um efeito hipoglicêmico e melhora os hormônios tireoidianos tanto de ratos diabéticos quanto de ratos diabéticos com HFHC.

Metformin use and risk of ischemic stroke in patients with type 2 diabetes: A cohort study / 北京大学学报(医学版)

OBJECTIVE@#To explore the association between the use of metformin and the risk of ischemic stroke in patients with type 2 diabetes.@*METHODS@#A prospective cohort study was designed from the Fangshan family cohort in Beijing. According to metformin use at baseline, 2 625 patients with type 2 diabetes in Fangshan, Beijing were divided into metformin group or non-metformin group and the incidence of ischemic stroke between the different groups during follow-up was estimated and compared by Cox proportional hazard regression model. The participants with metformin were first compared with all the parti-cipants who did not use metformin, and then were further compared with those who did not use hypoglycemic agents and those who used other hypoglycemic agents.@*RESULTS@#The patients with type 2 diabetes were with an average age of (59.5±8.7) years, and 41.9% of them were male. The median follow-up time was 4.5 years. A total of 84 patients developed ischemic stroke during follow-up, with a crude incidence of 6.4 (95%CI: 5.0-7.7) per 1 000 person-years. Among all the participants, 1 149 (43.8%) took metformin, 1 476 (56.2%) were metformin non-users, including 593 (22.6%) used other hypoglycemic agents, and 883 (33.6%) did not use any hypoglycemic agents. Compared with metformin non-users, the Hazard ratio (HR) for ischemic stroke in metformin users was 0.58 (95%CI: 0.36-0.93; P = 0.024). Compared with other hypoglycemic agents, HR was 0.48 (95%CI: 0.28-0.84; P < 0.01); Compared with the group without hypoglycemic agents, HR was 0.65 (95%CI: 0.37-1.13; P=0.13). The association between metformin and ischemic stroke was statistically significant in the patients ≥ 60 years old compared with all the metformin non-users and those who used other hypoglycemic agents (HR: 0.48, 95%CI: 0.25-0.92; P < 0.05). Metformin use was associated with a lower incidence of ischemic stroke in the patients with good glycemic control (0.32, 95%CI: 0.13-0.77; P < 0.05). In the patients with poor glycemic control, and the association was not statistically significant (HR: 0.97, 95%CI: 0.53-1.79; P>0.05). There was an interaction between glycemic control and metformin use on incidence of ischemic stroke (Pinteraction < 0.05). The results of the sensitivity analysis were consistent with the results in the main analysis.@*CONCLUSION@#Among patients with type 2 diabetic in rural areas of northern China, metformin use was associated with lower incidence of ischemic stroke, especially in patients older than 60 years. There was an interaction between glycemic control and metformin use in the incidence of ischemic stroke.

Hypoglycemic effect of electroacupuncture at "Tianshu" (ST 25) combined with metformin on rats with type 2 diabetes mellitus based on AMPK / 中国针灸

OBJECTIVE@#To observe the hypoglycemic effect of electroacupuncture (EA) at "Tianshu" (ST 25) combined with metformin on rats with type 2 diabetes mellitus (T2DM) as well as its effect on expression of adenosine monophosphate activated protein kinase (AMPK) in liver and pancreas.@*METHODS@#Thirty-six male SD rats were randomly divided into a blank group (6 rats) and a model establishing group (30 rats). The rats in the model establishing group were fed with high-fat diet and treated with intraperitoneal injection of low-dose streptozotocin (STZ) to establish T2DM model. The rats with successful model establishment were randomly divided into a model group, a control group, a metformin group, an EA group and a combination group, 6 rats in each group. The rats in the EA group were treated with EA at "Tianshu" (ST 25), dense-disperse wave, 2 Hz/15 Hz in frequency and 2 mA in current intensity, 20 min each time. The rats in the metformin group were treated with intragastric administration of metformin (190 mg/kg) dissolved in 0.9% sodium chloride solution (2 mL/kg). The rats in the combination group were treated with EA at "Tianshu" (ST 25) and intragastric administration of metformin. The rats in the control group were treated with intragastric administration of 0.9% sodium chloride solution with the same dose. All the treatments were given once a day for 5 weeks. After the intervention, the body mass and random blood glucose were detected; the serum insulin level was detected by ELISA; the expression of AMPK and phosphorylated adenosine monophosphate activated protein kinase (p-AMPK) in liver and pancreas was detected by Western blot method; the expression of protein gene product 9.5 (PGP9.5) was detected by immunofluorescence.@*RESULTS@#①Compared with the blank group, the body mass in the model group was decreased (P<0.05); compared with the model group, the body mass in the EA group and the combination group was decreased (P<0.05); the body mass in the EA group and the combination group was lower than the metformin group (P<0.05). Compared with the blank group, the random blood glucose in the model group was increased (P<0.01); compared with the model group, the random blood glucose in the metformin group, the EA group and the combination group was decreased (P<0.01). The random blood glucose in the combination group was lower than the metformin group and the EA group (P<0.05). ②Compared with the blank group, the insulin level in the model group was decreased (P<0.05); compared with the model group, the insulin level in the metformin group, the EA group and the combination group was all increased (P<0.05). The insulin level in the combination group was higher than the metformin group and the EA group (P<0.05). ③Compared with the blank group, the protein expression of AMPK and p-AMPK in liver tissue was decreased (P<0.05), and the protein expression of AMPK and p-AMPK in pancreatic tissue was increased (P<0.05) in the model group. Compared with the model group, the protein expression of AMPK and p-AMPK in liver tissue in the metformin group, the EA group and the combination group was increased (P<0.05, P<0.01); the protein expression of AMPK in pancreatic tissue in the metformin group was increased (P<0.05); the protein expression of AMPK in pancreatic tissue in the EA group and the combination group was decreased (P<0.05); the protein expression of p-AMPK in pancreatic tissue in the metformin group, the EA group and the combination group was decreased (P<0.05). The protein expression of AMPK and p-AMPK in liver tissue in the combination group was higher than that in the metformin group and the EA group (P<0.05); the protein expression of AMPK in pancreatic tissue in the EA group and the combination group was less than that in the metformin group (P<0.05), and the expression of p-AMPK protein in pancreatic tissue in the combination group was less than that in the metformin group and the EA group (P<0.05). ④Compared with the blank group, the expression of PGP9.5 in pancreatic tissue in the model group was increased (P<0.01); compared with the model group, the expression of PGP9.5 in pancreatic tissue in the metformin group, the EA group and the combination group was decreased (P<0.05, P<0.01). The expression of PGP9.5 in pancreatic tissue in the EA group was lower than the metformin group and the combination group (P<0.05).@*CONCLUSION@#Electroacupuncture at "Tianshu" (ST 25) could promote the effect of metformin on activating AMPK in liver tissue of T2DM rats, improve the negative effect of metformin on AMPK in pancreatic tissue, and enhance the hypoglycemic effect of metformin. The mechanism may be related to the inhibition of pancreatic intrinsic nervous system.

A review of patent literature on the regulation of glucose metabolism by six phytocompounds in the management of diabetes mellitus and its complications / 中西医结合学报

Diabetes mellitus is a chronic disease, typified by hyperglycemia resulting from failures in complex multifactorial metabolic functions, that requires life-long medication. Prolonged uncontrolled hyperglycemia leads to micro- and macro-vascular complications. Although antidiabetic drugs are prescribed as the first-line treatment, many of them lose efficacy over time or have severe side effects. There is a lack of in-depth study on the patents filed concerning the use of natural compounds to manage diabetes. Thus, this patent analysis provides a comprehensive report on the antidiabetic therapeutic activity of 6 phytocompounds when taken alone or in combinations. Four patent databases were searched, and 17,649 patents filed between 2001 and 2021 were retrieved. Of these, 139 patents for antidiabetic therapeutic aids that included berberine, curcumin, gingerol, gymnemic acid, gymnemagenin and mangiferin were analyzed. The results showed that these compounds alone or in combinations, targeting acetyl-coenzyme A carboxylase 2, serine/threonine protein kinase, α-amylase, α-glucosidase, lipooxygenase, phosphorylase, peroxisome proliferator-activated receptor-γ (PPARγ), protein tyrosine phosphatase 1B, PPARγ co-activator-1α, phosphoinositide 3-kinase and protein phosphatase 1 regulatory subunit 3C, could regulate glucose metabolism which are validated by pharmacological rationale. Synergism, or combination therapy, including different phytocompounds and plant extracts, has been studied extensively and found effective, whereas the efficacy of commercial drugs in combination with phytocompounds has not been studied in detail. Curcumin, gymnemic acid and mangiferin were found to be effective against diabetes-related complications. Please cite this article as: DasNandy A, Virge R, Hegde HV, Chattopadhyay D. A review of patent literature on the regulation of glucose metabolism by six phytocompounds in the management of diabetes mellitus and its complications. J Integr Med. 2023; 21(3): 226-235.

The development and benefits of metformin in various diseases / 医学前沿

Metformin has been used for the treatment of type II diabetes mellitus for decades due to its safety, low cost, and outstanding hypoglycemic effect clinically. The mechanisms underlying these benefits are complex and still not fully understood. Inhibition of mitochondrial respiratory-chain complex I is the most described downstream mechanism of metformin, leading to reduced ATP production and activation of AMP-activated protein kinase (AMPK). Meanwhile, many novel targets of metformin have been gradually discovered. In recent years, multiple pre-clinical and clinical studies are committed to extend the indications of metformin in addition to diabetes. Herein, we summarized the benefits of metformin in four types of diseases, including metabolic associated diseases, cancer, aging and age-related diseases, neurological disorders. We comprehensively discussed the pharmacokinetic properties and the mechanisms of action, treatment strategies, the clinical application, the potential risk of metformin in various diseases. This review provides a brief summary of the benefits and concerns of metformin, aiming to interest scientists to consider and explore the common and specific mechanisms and guiding for the further research. Although there have been countless studies of metformin, longitudinal research in each field is still much warranted.

Bioactivity evaluation of least explored traditionally acclaimed medicinally potent herb Nanorrhinum ramosissimum(Wall. ) Betsche

Abstract Present study analysed the therapeutic potential of traditionally acclaimed medicinal herb Nanorrhinum ramosissimum, using plant parts extracted with different solvents (10 mg/mL). Shoot extracts exhibited comparatively better antimicrobial properties, in comparison to root extracts. Total phenolic content was estimated, to ascertain its dependency on antioxidant properties of plant extracts. Antioxidant assay revealed promising results in comparison to IC50 value of standard ascorbic acid (52.2±0.07 µg/mL), for methanolic extracts of shoot (61.07±0.53 µg/mL and 64.33±0.33 µg/mL) and root (76.705±0.12 µg/mL and 89.73±0.28 µg/ mL) for in vivo and in vitro regenerants respectively. Correlation coefficient R2 values ranged between 0.90-0.95, indicating a positive correlation between phenolic contents and antioxidant activity. Plant extracts were also able to inhibit DNA oxidative damage again indicating their antioxidative potential. Antidiabetic potential was confirmed by alpha amylase inhibition assay where shoot methanolic extracts (invivo, in vitro) exhibited the best IC50 values (54.42±0.16 µg/mL, 66.09±0.12 µg/mL) in comparison to standard metformin (41.92±0.08 µg/mL). Ethanolic extracts of roots (in vitro, invivo) exhibited the relative IC50 values (88.97±0.32µg/mL,96.63±0.44 µg/mL) indicating that shoot parts had a better alpha amylase inhibition property; thus proving the herb's bioactive potential and its prospective therapeutic source for curing various ailments.

Antioxidant, Antidiabetic and Lipid Profiling of Spermadicyton Suaveolens in Streptozotocin (STZ) Induced Diabetic Rats

ABSTRACT Diabetes is a life-threatening disease, and currently available synthetic medicines for treating diabetes are associated with various side effects. Therefore, there is an unmet need to develop herbal remedies against diabetes as an alternative to synthetic medicines. Although local healers use the roots of Spermadicyton suaveolens (SS) to manage diabetes, there is negligible research to validate its antidiabetic properties. The present investigation aims to the assess the antioxidant, antidiabetic, and antihyperlipidemic potential of the ethanolic extract of S. Suaveolen's roots (EESS) on streptozotocin (STZ) induced diabetic rats. The extract was screened for in vitro antioxidant and antidiabetic activity. The in vivo antidiabetic potential of EESS (at 200 and 400 mg/kg) was studied on STZ-induced diabetic rats for 20 days. The EESS displayed significant (p<0.05) antidiabetic and antioxidant properties. The administration of 200 mg/kg and 400 mg/kg EESS in STZ-induced diabetic rats significantly reduced hyperglycemia, and restored antioxidant enzymes and lipid profile-a high density lipoprotein (HDL) increased by the administration of a single dose of streptozotocin. Thus, EESS could be a promising herbal medicine in the treatment of diabetes and hyperlipidemia

Bioactivity-guided isolation of the antidiabetic principle in Pterocarpus Santalinoides leaf extract

Abstract Pterocarpus santalinoides is used in Nigerian ethnomedicine to treat diabetes mellitus. This study aimed to establish the antidiabetic property of the plant, and isolate and characterize its active principle. Dried and pulverized leaves (500 g) of P. santalinoides were extracted with 1.8 L of 80 % hydromethanol by cold maceration. The dried extract (10 g) was partitioned into n-hexane, ethyl acetate (EtOAc), n-butanol, and water. Antidiabetic activitiy-guided isolation by column chromatographic separation of the EtOAc soluble and purification of the sub-fractions by repeated preparative thin layer chromatography (pTLC) yielded a C-glycosyl flavonoid, identified as isovitexin. The chemical structure was elucidated based on high-resolution mass spectroscopy, 1D, and 2D nuclear magnetic resonance spectroscopic analyses. Alloxan-induced diabetic rat model was adopted for antidiabetic screening. The extract of P. santalinoides (100-200 mg/kg), fraction F4 (50 mg/kg), sub-fraction F4.3 (10 mg/kg), and the semi-purified compound F4.3.2 (5 mg/kg) significantly (p<0.05) reduced the fasting blood glucose of alloxan-induced diabetic rats, causing 48.4, 69.4, 57.7 and 64.5 % antidiabetic activity respectively, compared with > 68 % recorded in glibenclamide (2 mg/kg) control. These results reveal that isovitexin is the antidiabetic principle in P. santalinoides

Efeitos da nanopartícula de ácido poli lático-co-glicólico (PLGA) associada ao cloridrato de metformina na doença periodontal em ratos diabéticos / Effects of polylactic-co-glycolic acid (PLGA) nanoparticle associated with metformin hydrochloride on periodontal disease in diabetic rats

Existe uma associação entre diabetes e a periodontite, e a Metformina (MET) além de controlar os níveis glicêmicos, tem apresentado efeitos antiinflamatórios e na diminuição da perda óssea periodontal. Ao se veicular a MET a um sistema de nanopartículas pode-se apresentar a vantagem de aumento da eficácia terapêutica. Objetivos: esse estudo consistiu na avaliação dos efeitos antiinflamatórios, perda óssea e disponibilidade in vitro/in vivo de uma nanopartícula de ácido poli lático-co-glicólico (PLGA) associada à MET em um modelo de periodontite induzida por ligadura. Materiais e métodos: o PLGA carreado com diferentes doses da MET foi caracterizado pelo seu diâmetro médio, tamanho da partícula, índice de polidispensão e eficiência de aprisionamento. Foram utilizados ratos machos da linhagem Wistar, divididos aleatoriamente, em grupos controles e experimentais com diferentes doses de MET associadas ou não ao PLGA, os quais receberam diferentes tratamentos. Amostras de maxilas e tecidos gengivais foram utilizadas para avaliação de perda óssea e inflamação, por meio da microtomografia computadorizada, histopatológico, imunohistoquímica, análise de citocinas inflamatórias e expressão gênica de proteínas por RT-PCR quantitativo. Para o ensaio de liberação in vitro, utilizou-se o dispositivo de células de difusão vertical de Franz estáticas. Para a disponibilidade in vivo, as amostras de sangue foram coletadas em diferentes intervalos de tempo e analisadas por cromatografia líquida de alta eficiência acoplado a espectrometria de massas (HPLC-MS/MS). Resultados: o diâmetro médio das nanopartículas de PLGA carreadas com MET estava em um intervalo de 457,1 ± 48,9 nm (p <0,05) com um índice de polidispersidade de 0,285 (p <0,05), potencial Z de 8,16 ± 1,1 mV (p <0,01) e eficiência de aprisionamento (EE) de 66,7 ± 3,73. O tratamento com a MET 10 mg / kg + PLGA mostrou uma baixa concentração de células inflamatórias, fraca imunomarcação para RANKL, Catepsina K, OPG e osteocalcina. Diminuição dos níveis de IL-1ß e TNF-α (p <0,05), aumento da expressão gênica do AMPK (p <0,05) e diminuição do NF-κB p65, HMGB1 e TAK-1 (p <0,05). O 10 mg/kg MET + PLGA foi liberado no ensaio in vitro sugerindo um modelo cinético de difusão parabólica com um perfil de liberação que atinge 50% de seu conteúdo em 2h e permanece em liberação constante em torno de 60% até o final de 6h. O ensaio in vivo mostrou o volume aparente de distribuição Vz/F (10 mg/kg MET + PLGA, 46,31 mL/kg vs. 100 mg/kg MET + PLGA, 28,8 mL/kg) e o tempo médio de residência MRTinf (PLGA + MET 10 mg /kg, 37,66h vs. MET 100 mg/kg, 3,34h). Conclusão: o PLGA carreado com MET diminuiu a inflamação e a perda óssea na periodontite em ratos diabéticos. O 10 mg/kg MET + PLGA teve uma taxa de eliminação mais lenta em comparação com o MET 100 mg/kg. A formulação modifica os parâmetros farmacocinéticos, como volume de distribuição aparente e tempo médio de residência (AU).

There is an association between diabetes and periodontitis, and Metformin (MET) in addition to controlling glycemic levels, has shown anti-inflammatory effects and decreased periodontal bone loss. By transferring MET to a nanoparticle system, the advantage of increasing therapeutic efficacy can be presented. Objectives: this study consisted of evaluating the antiinflammatory effects, bone loss and in vitro/in vivo availability of a polylactic-co-glycolic acid (PLGA) nanoparticle associated with MET in a ligature-induced periodontitis model. Materials and methods: PLGA loaded with different doses of MET was characterized by its mean diameter, particle size, polydispension index and entrapment efficiency. Male Wistar rats were used, randomly divided into control and experimental groups with different doses of MET associated or not with PLGA, which received different treatments. Samples of jaws and gingival tissues were used to assess bone loss and inflammation, using computed microtomography, histopathology, immunohistochemistry, analysis of inflammatory cytokines and gene expression of proteins by quantitative RT-PCR. For the in vitro release assay, the static Franz vertical diffusion cell device was used. For in vivo availability, blood samples were collected at different time intervals and analyzed by high performance liquid chromatography coupled with mass spectrometry (HPLC-MS/MS). Results: the mean diameter of MET-loaded PLGA nanoparticles was in the range of 457.1 ± 48.9 nm (p <0.05) with a polydispersity index of 0.285 (p <0.05), Z potential of 8.16 ± 1.1 mV (p <0.01) and trapping efficiency (EE) of 66.7 ± 3.73. Treatment with MET 10 mg/kg + PLGA showed a low concentration of inflammatory cells, weak immunostaining for RANKL, Cathepsin K, OPG and osteocalcin. Decreased IL-1ß and TNF-α levels (p <0.05), increased AMPK gene expression (p <0.05) and decreased NF-κB p65, HMGB1 and TAK-1 (p <0. 05). The 10 mg/kg MET + PLGA was released in the in vitro assay suggesting a kinetic model of parabolic diffusion with a release profile that reaches 50% of its content in 2h and remains in constant release around 60% until the end of 6h . The in vivo assay showed the apparent volume of distribution Vz/F (10 mg/kg MET + PLGA, 46.31 mL/kg vs. 100 mg/kg MET + PLGA, 28.8 mL/kg) and the mean MRTinf residency (PLGA + MET 10 mg/kg, 37.66h vs. MET 100 mg/kg, 3.34h). Conclusion: MET-loaded PLGA decreased inflammation and bone loss in periodontitis in diabetic rats. 10 mg/kg MET + PLGA had a slower rate of elimination compared to 100 mg/kg MET. The formulation modifies pharmacokinetic parameters such as apparent volume of distribution and mean residence time (AU).

Perfiles de hipoglicemiantes e insulinas en pacientes con diabetes mellitus tipo 2 y su efecto en control metabólico, hipoglicemia y otros efectos adversos / Profile of glucose lowering drug use in outpatients with type 2 diabetes mellitus

BACKGROUND: The use of glucose lowering agents with favorable weight profile is a growing practice in Diabetology. AIM: To characterize medication combinations in patients with type 2 Diabetes (T2D) and their effect on metabolic control. MATERIAL AND METHODS: Review of medical records of 249 outpatients with T2D with a median age of 66 years, cared for at a medical network. Clinical characteristics, glycated hemoglobin (HbA1c), details of Diabetes treatment (types of drugs or insulin), renal function, lipids and B12 vitamin levels were registered. RESULTS: The median disease duration was 16 years. The most recent HbA1c was 7.4%. No patient was using sulfonylureas, 45 were using Dipeptidyl peptidase 4 inhibitors, 113 were using Sodium-glucose Cotransporter-2 (SGLT2i) Inhibitors, 21 used Glucagon-like Peptide-1 Receptor Agonists (GLP1ra), 158 used basal insulin and 61 on basal plus bolus insulin. The use of SGLT2i or GLP1ra was associated with a metabolic control similar to those patients not using them, while patients on rapid insulin had a significantly worse metabolic control and a tendency to greater body mass index. The use of basal insulin and rapid insulin was significantly associated with more hypoglycemia events. CONCLUSIONS: The use of SGLT2i and GLP1ra in patients with T2D is associated with better metabolic control than rapid insulin with less risk of hypoglycemia. The use of these therapies should be prioritized in the future.

Alternativas de controle do diabetes / Alternatives for diabetes control / Alternativas para el control de la diabetes

O Diabetes desde a antiguidade tem sido uma das maiores causas de morte entre as populações do globo, e segundo a Organização Mundial da Saúde continua assolando nos nossos dias. Apesar das descobertas de tratamentos mais eficazes, a doença vem avançando em progressões assustadoras atualmente, com projeções preocupantes para a saúde pública. Como estratégia de acompanhamento terapêutico, estatístico direcionado a portadores de diabetes, o Governo Federal lançou o programa HIPERDIA (Hipertensos e Diabéticos), que faz o acompanhamento da evolução da doença e das complicações dos pacientes. E neste sentido, também são utilizadas terapêuticas mais acessíveis como as plantas medicinais. O objetivo desta pesquisa consiste em realizar uma revisão bibliográfica abordando as opções de terapias de controle do diabetes oferecidas no Sistema Único de Saúde e pesquisar fitoterápicos com potencial hipoglicêmico aprovados pela Anvisa. Através de levantamento bibliográfico, foram identificadas oito espécies vegetais utilizadas pela medicina popular no controle do diabetes, sendo estas: Bauhinia Forficata, Syzygium Cumini, Annona Muricata, Cynara Scolymus, Momordica Charantia, Eugenia Uniflora e Baccharis Trimera. Essas plantas do programa, embora tenham comprovação de seu efeito hipoglicêmico e redutores dos sintomas diabéticos, pelas suas propriedades antioxidantes e antiinflamatórias, colabora para uma melhor qualidade de vida aos pacientes.

Since antiquity, Diabetes has been one of the biggest causes of death amon-g populations around the globe, and according to the World Health Organization, it continues to plague our days. Despite discoveries of more effective treatments, the disease is currently advancing in frightening progressions, with worrying projections for public health. As a therapeutic, statistical follow-up strategy aimed at people with diabetes, the Federal Government launched the HIPERDIA (Hypertensive and Diabetic) program, which monitors the evolution of the disease and the complications of patients. And in this sense, more accessible therapies such as medicinal plants are also used. The objective of this research is to carry out a literature review addressing the options for diabetes control therapies offered in the Unified Health System and to search for herbal medicines with hypoglycemic potential approved by Anvisa. Through a bibliographical survey, eight plant species used by folk medicine to control diabetes were identified, namely: Bauhinia Forficata, Syzygium Cumini, Annona Muricata, Cynara Scolymus, Momordica Charantia, Eugenia Uniflora and Bacharis Trimera. These plants in the program, although they have evidence of their hypoglycemic effect and reduce diabetic symptoms, due to their antioxidant and anti-inflammatory properties, contribute to a better quality of life for patients.

La diabetes ha sido desde la antigüedad una de las principales causas de muerte entre las poblaciones del planeta, y según la Organización Mundial de la Salud sigue haciendo estragos en nuestros días. A pesar de los descubrimientos de tratamientos más eficaces, la enfermedad avanza actualmente con una progresión aterradora, con proyecciones preocupantes para la salud pública. Como estrategia de seguimiento terapéutico, estadísticamente dirigida a las personas con diabetes, el Gobierno Federal puso en marcha el programa HIPERDIA (Hipertensión y Diabetes), que controla la evolución de la enfermedad y las complicaciones de los pacientes. En este sentido, también se utilizan terapias más accesibles, como las plantas medicinales. El objetivo de esta investigación es realizar una revisión bibliográfica que aborde las opciones de terapias para el control de la diabetes ofrecidas en el Sistema Único de Salud y buscar fitoterapias con potencial hipoglucemiante aprobadas por Anvisa. Mediante un estudio bibliográfico, se identificaron ocho especies vegetales utilizadas por la medicina popular en el control de la diabetes, a saber: Bauhinia Forficata, Syzygium Cumini, Annona Muricata, Cynara Scolymus, Momordica Charantia, Eugenia Uniflora y Baccharis Trimera. Estas plantas del programa, aunque han demostrado su efecto hipoglucemiante y reductor de los síntomas diabéticos, por sus propiedades antioxidantes y antiinflamatorias, colaboran a una mejor calidad de vida para los pacientes.

Bauhinia spp. (pata-de-vaca) and its biological potentialities ­ literature review / Bauhinia spp. (pata-de-vaca) e suas potencialidades biológicas ­ revisão da literatura / Bauhinia spp. (pata-de-vaca) y sus potencialidades biológicas - revisión de la literatura

The genus Bauhinia popularly known as "pata-de-vaca", "unha de vaca", "unha de boi", "unha de anta" e "casco de vaca" is widely used in the form of teas and other herbal preparations. The aim of this literature review was to show the diversity and biological potential of Bauhinia species for health promotion. A search was carried out for articles listing some species of medical interest. The pharmacological activities of B. forficata were also highlighted in articles published in the last twenty years using the PubMed database. Research has shown that Bauhinia is used as a hypoglycemic and antidiabetic agent, diuretic, cholesterol reducer, in the treatment of cystitis, intestinal parasites, elephantiasis, tumors and other ailments, including infections and painful processes. In the last eleven years, 86% of the works carried out with B. forficata used the plant collected or acquired in Brazil, predominantly publications from the southern region of the country where almost 60% reported activity on diabetes and its complications and/or antioxidant effect. Despite the literature pointing out the great medicinal potential of Bauhinia in chronic diseases and their complications, there is still a need for more translational research.

O gênero Bauhinia conhecido popularmente como "pata-de-vaca", "unha de vaca", "unha de boi", "unha de anta" e "casco de vaca" é amplamente utilizado em forma de chás e outras preparações fitoterápicas. O objetivo desta revisão de literatura foi mostrar a diversidade e potencial biológico das espécies de Bauhinia para a promoção a saúde. Foi realizada a busca de artigos elencando algumas espécies de interesse médico. Destacou-se também as atividades farmacológicas de B. forficata em artigos publicados nos últimos vinte anos utilizando a base de dados PubMed. A pesquisa mostrou que a Bauhinia é utilizada como hipoglicemiante e antidiabética, diurética, redutora de colesterol, no tratamento da cistite, parasitoses intestinais, elefantíase, tumores e outros males, incluindo infecções e processos dolorosos. Nos últimos onze anos, 86% dos trabalhos realizados com B. forficata utilizaram a planta coletada ou adquirida no Brasil sendo predominante publicações oriundas da região sul do país onde quase 60% relataram atividade sobre o diabetes e suas complicações e/ou efeito antioxidante. Apesar da literatura apontar o grande potencial medicinal da Bauhinia em doenças crônicas e suas complicações ainda há a necessidade de mais pesquisas de caráter translacional.

El género Bauhinia, conocido popularmente como "garra de vaca", "garra de ganado", "garra de tapir" y "pezuña de vaca", se utiliza ampliamente como té y otros preparados fitoterapéuticos. El objetivo de esta revisión bibliográfica era mostrar la diversidad y el potencial biológico de las especies de Bauhinia para la promoción de la salud. Se llevó a cabo una búsqueda de artículos que incluyeran algunas especies de interés médico. Las actividades farmacológicas de B. forficata también fueron destacadas en artículos publicados en los últimos veinte años utilizando la base de datos PubMed. La investigación demostró que la Bauhinia se utiliza como hipoglucemiante y antidiabético, diurético, reductor del colesterol, en el tratamiento de la cistitis, la parasitosis intestinal, la elefantiasis, los tumores y otras dolencias, incluyendo infecciones y procesos dolorosos. En los últimos once años, el 86% de los estudios realizados con B. forficata utilizaron la planta recolectada o adquirida en Brasil, siendo predominantes las publicaciones de la región sur del país, donde casi el 60% reportó actividad sobre la diabetes y sus complicaciones y/o efecto antioxidante. Aunque la bibliografía señala el gran potencial medicinal de la Bauhinia en las enfermedades crónicas y sus complicaciones, todavía es necesario realizar más investigaciones traslacionales.

Cyperus esculentus L. protects testis and sperm morphology of hyperglycaemic rats / Cyperus esculentus L. protege la morfología de los testículos y los espermatozoides de ratas hiperglicémicas

Cyperus esculentus L. (tiger nut) is a tuberous plant that promotes and protects reproductive functions, which are usually hampered in diabetics. The present study investigated the effect of Cyperus esculentus tuber extract (CETE) on testicular histology and sperm viability of alloxan-induced hyperglycaemic Wistar rats. Twenty-five adult male Wistar rats weighing 150-200g and grouped into five (n=5): Group 1, the control, administered tap water (20mL/kg), while groups 2-5 were administered a single intraperitoneal dose (120mg/kg b.w.) of alloxan, and each further received orally tap water (20mL/kg), CETE (100mg/kg), CETE (500 mg/kg) and metformin (500 mg/kg), respectively for 21 days. The animals were sacrificed, their sperm collected for analysis, while the testes were harvested, and processed for histology. Results showed significantly increased (p<0.05) blood glucose and testosterone, and significantly decreased (p<0.05) sperm pH, motility, count, morphology and density, as well as disruptions and hypertrophy of the spermatogenic and Sertoli cells of the hyperglycaemic group. There were significant (p<0.05) blood glucose decline, while the sperm parameters and testicular weight improved with normal testicular histology in the 100 mg/kg CETE, 500 mg/kg CETE, and metformin-treated groups compared to the control and hyperglycaemic group. Treatment with CETE showed blood glucose amelioration and improved sperm quality, as well as testicular damage attenuation.

Cyperus esculentus L. es una planta tuberosa que promueve y protege las funciones reproductivas, que generalmente se ven afectadas en los diabéticos. El presente estudio investigó el efecto del extracto de tubérculo de Cyperus esculentus (CETE) sobre la histología testicular y la viabilidad de los espermatozoides de ratas wistar con hiperglicemia inducida por alloxan. Veinticinco ratas Wistar macho adultas que pesaban 150-200 g y se agruparon en cinco (n = 5): el grupo 1, el control, administró agua del grifo (20ml / kg), mientras que los grupos 2-5 se les administró una dosis intraperitoneal única (120 mg / kg p.v.) de alloxan, y agua del grifo por vía oral (20ml/kg), CETE (100 mg/kg), CETE (500 mg/kg) y metformina (500 mg/kg), respectivamente durante 21 días. Los animales fueron sacrificados, su esperma recolectada para su análisis, mientras que los testículos fueron retirados y procesados para histología. Los resultados mostraron un aumento significativo (p<0,05) de la glucosa en sangre y la testosterona, y una disminución significativa (p<0,05) del pH, la motilidad, el recuento, la morfología y la densidad de los espermatozoides, así como interrupciones e hipertrofia de las células espermatogénicas y sertoli del grupo hiperglucémico. Hubo una disminución significativa (p<0,05) de la glucosa en sangre, mientras que los parámetros espermáticos y el peso testicular mejoraron con la histología testicular normal en los grupos de 100 mg / kg de CETE, 500 mg / kg de CETE y tratados con metformina en comparación con el grupo de control e hiperglucémico. El tratamiento con CETE mostró una mejora de la glucosa en sangre y una mejora de la calidad de los espermatozoides, así como atenuación del daño testicular.