Complexos polieletrólitos de quitosana e xantana carregados com ativos naturais e sintéticos: estudo físico/químico e microbiológico para aplicação de drug delivery / Polyelectrolyte complexes of chitosan and xanthan loaded with natural and synthetic actives: physicochemical and microbiological study for drug delivery application

A eficácia dos implantes osseointegrados é amplamente reconhecida na literatura científica. Contudo, infiltrações bacterianas na junção implante-pilar podem desencadear inflamação nos tecidos circundantes, contribuindo para a evolução de condições mais sérias, como a peri-implantite. O objetivo desse estudo foi produzir complexos polieletrólitos (PECs) de quitosana (Q) e xantana (X) em forma de membranas, carregá-las com ativos naturais e sintéticos antimicrobianos, caracterizálas estruturalmente e avaliá-las frente a degradação enzimática, cinética de liberação e ações antimicrobianas com finalidade de aplicação para drug delivery. Membranas de QX a 1% (m/v) foram produzidas em três proporções, totalizando doze grupos experimentais: QX (1:1); QX (1:2), QX (2:1), QX-P (com própolis) (1:1); QX-P (1:2); QX-P (2:1); QX-C (com canela) (1:1); QX-C (1:2); QX-C (2:1) e CLX (com clorexidina 0,2%) (1:1); CLX (1:2); CLX (2:1). Para os estudos de caracterização foram feitas análises da espessura em estado seco; análises morfológicas superficial e transversal em Microscopia Eletrônica de Varredura (MEV); análise estrutural de espectroscopia de infravermelho por transformada de Fourier (FTIR); análise de degradação por perda de massa sob ação da enzima lisozima; e análise da cinética de liberação dos ativos em saliva artificial. Para os testes microbiológicos, análises de verificação de halo de inibição e ação antibiofilme foram feitas contra cepas de Staphylococcus aureus (S. aureus) e Escherichia coli (E. coli). Os resultados demonstraram que a espessura das membranas variou conforme a proporção, sendo que o grupo QX (1:2) apresentou a maior média de 1,022 mm ± 0,2, seguida respectivamente do QX (1:1) com 0,641 mm ± 0,1 e QX (2:1) com 0,249 mm ± 0,1. Nas imagens de MEV é possível observar uma maior presença de fibras, rugosidade e porosidade nos grupos QX (1:2) e QX (1:1) respectivamente, e, no QX (2:1) uma superfície mais lisa, uniforme e fina. No FTIR foram confirmados os picos característicos dos materiais isoladamente, além de observar as ligações iônicas que ocorreram para formação dos PECs. Na análise de degradação, os grupos com ativos naturais adicionados tiveram melhores taxas de sobrevida do que os grupos QX. No teste de liberação, os grupos QX-P tiveram uma cinética mais lenta que os QX-C, cuja liberação acumulada de 100% foi feita em 24 h. Já nos testes do halo inibitório, somente os grupos CLX tiveram ação sobre as duas cepas, e os QX-P tiveram sobre S. aureus. Nas análises antibiofilme, os grupos CLX apresentaram as maiores taxas de redução metabólica nas duas cepas (± 79%); os grupos QX-P apresentaram taxas de redução similares em ambas as cepas, porém com percentual um pouco maior para E. coli (60- 80%) e os grupos QX-C tiveram grande discrepância entre as duas cepas: de 35 a 70% para S. aureus e 14 a 19% para E. coli. Pode-se concluir que, frente as análises feitas, o comportamento do material foi afetado diretamente pelos ativos adicionados a matriz polimérica. As proporções de Q ou X afetaram somente a espessura final. Quanto a aplicação proposta de drug delivery, os dispositivos apresentaram grande potencial, principalmente os grupos CLX e QX-P. (AU)

The effectiveness of osseointegrated implants is widely recognized in scientific literature. However, bacterial infiltrations at the implant-abutment interface may trigger inflammation in surrounding tissues, contributing to the development of more serious conditions, such as peri-implantitis. The aim of this study was to produce chitosan (Q) and xanthan (X) polyelectrolyte complexes (PECs) in the form of membranes, load and evaluate them for enzymatic degradation, release kinetics, and antimicrobial actions for drug delivery applications. QX membranes at 1% (w/v) were produced in three proportions, totaling twelve experimental groups: QX (1:1), QX (1:2), QX (2:1), QX-P (with propolis) (1:1), QX-P (1:2), QX-P (2:1), QX-C (with cinnamon) (1:1), QX-C (1:2), QX-C (2:1), and CLX (with 0.2% chlorhexidine) (1:1), CLX (1:2), CLX (2:1). Characterization studies included analyses of dry state thickness, surface and crosssectional morphology using Scanning Electron Microscopy (SEM), structural analysis by Fourier Transform Infrared (FTIR) spectroscopy, mass loss degradation analysis under lysozyme action, and active release kinetics analysis in artificial saliva. Microbiological tests included verification analyses of inhibition halos and antibiofilm action against strains of Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli). Results showed that membrane thickness varied according to proportion, with group QX (1:2) presenting the highest average of 1.022 mm ± 0.2, followed by QX (1:1) with 0.641 mm ± 0.1, and QX (2:1) with 0.249 mm ± 0.1. SEM images showed greater presence of fibers, roughness, and porosity in groups QX (1:2) and QX (1:1) respectively, while QX (2:1) exhibited a smoother, more uniform, and thinner surface. FTIR confirmed characteristic peaks of the materials individually, besides showing ionic bonds formed for PECs. Degradation analysis revealed that groups with added natural actives had better survival rates than QX groups. In release tests, QX-P groups exhibited slower kinetics than QX-C, with 100% cumulative release achieved in 24 h. inhibitory halo tests, only CLX groups exhibited action against both strains, while QX-P acted against S. aureus. Antibiofilm analyses showed CLX groups with the highest metabolic reduction rates in both strains (± 79%); QX-P groups showed similar reduction rates in both strains, slightly higher for E. coli (60-80%), and QX-C groups had a significant discrepancy between strains: 35-70% for S. aureus and 14-19% for E. coli. In conclusion, material behavior was directly affected by added actives to the polymeric matrix. Proportions of Q or X only affected final thickness. Regarding proposed drug delivery applications, the devices showed great potential, especially CLX and QX-P groups.(AU)

Anti-hyperglycemic and anti-hyperlipidemic effects of a methanolic extract of Debregeasia salicifolia in Alloxan-induced diabetic albino mice

Abstract Diabetes mellitus (DM), an endocrine syndrome characterized by high blood glucose levels due to abrogated insulin activity. The existing treatments for DM have side effects and varying degrees of efficacy. Therefore, it is paramount that novel approaches be developed to enhance the management of DM. Therapeutic plants have been accredited as having comparatively high efficacy with fewer adverse effects. The current study aims to elucidate the phytochemical profile, anti-hyperlipidemic, and anti-diabetic effects of methanolic extract D. salicifolia (leaves) in Alloxan-induced diabetic mice. Alloxan was injected intraperitoneally (150 mg kg-1, b.w), to induced diabetes in mice. The mice were divided into three groups (n=10). Group 1 (normal control) received normal food and purified water, Group II (diabetic control) received regular feed and clean water and group III (diabetic treated) received a methanolic extract of the plant (300 mg kg-1) for 28 days with a typical diet and clean water throughout the experiment. Blood samples were collected to checked serum glucose and concentration of LDL, TC, TG. The extract demonstrated significant antihyperglycemic activity (P 0.05), whereas improvements in mice's body weight and lipid profiles were observed after treatment with the extract. This study establishes that the extract has high efficacy with comparatively less toxicity that can be used for DM management.

Resumo Diabetes mellitus (DM) é uma síndrome endócrina caracterizada por níveis elevados de glicose no sangue devido à atividade anulada da insulina. Os tratamentos existentes para o DM têm efeitos colaterais e vários graus de eficácia. Portanto, é fundamental que novas abordagens sejam desenvolvidas para aprimorar o manejo do DM. As plantas terapêuticas foram acreditadas como tendo eficácia comparativamente alta com menos efeitos adversos. O presente estudo visa elucidar o perfil fitoquímico, efeitos anti-hiperlipidêmicos e antidiabéticos do extrato metanólico de D. salicifolia (folhas) em camundongos diabéticos induzidos por aloxana. Alloxan foi injetado por via intraperitoneal (150 mg kg-1, b.w), para induzir diabetes em camundongos. Os camundongos foram divididos em três grupos (n = 10). Grupo 1 (controle normal) recebeu ração normal e água purificada, Grupo II (controle diabético) recebeu ração regular e água limpa, e o grupo III (tratamento diabético) recebeu extrato metanólico da planta (300 mg kg-1) por 28 dias com uma dieta típica e água limpa durante todo o experimento. Amostras de sangue foram coletadas para verificar a glicose sérica e a concentração de LDL, TC, TG. O extrato demonstrou atividade anti-hiperglicêmica significativa (P 0,05), enquanto melhorias no peso corporal e no perfil lipídico dos camundongos foram observadas após o tratamento com o extrato. Este estudo estabelece que o extrato tem alta eficácia com comparativamente menos toxicidade e pode ser usado para o controle do DM.

Flavonoides como suplementos para mejorar el rendimiento físico deportivo

Introducción: El ejercicio físico puede generar especies reactivas de oxígeno que dañan componentes celulares esenciales, como la fatiga. Los flavonoides, debido a su baja toxicidad y actividad antioxidante, se han estudiado como potenciales suplementos alimenticios para mejorar el rendimiento deportivo. Objetivo: Describir la evidencia científica que se ha obtenido sobre la eficacia del uso de flavonoides como suplementos para mejorar el rendimiento físico deportivo. Métodos: Se realizó una búsqueda sobre la eficacia del uso de flavonoides como suplementos para el rendimiento físico y deportivo en las bases de datos PubMed y Google Scholar. Se utilizaron las palabras clave: flavonoid, supplementation, sport, exercise, fatigue, muscle, fats, physical activity, y se tomaron en cuenta los artículos publicados entre los años 2018 y 2022, en idioma inglés que cumplieron con los criterios de selección. Resultados: Los flavonoides son capaces de disminuir la fatiga debido al esfuerzo físico en un contexto deportivo, principalmente debido a su capacidad de regular la actividad de agentes antioxidantes endógenos como las enzimas superóxido dismutasa, catalasa y glutatión peroxidasa, que se encargan de la neutralización de las especies reactivas de oxígeno. Además, son capaces de favorecer la neutralización de metabolitos tóxicos que se generan durante el ejercicio y de aumentar las reservas energéticas (glicógeno en el hígado y músculos) y la resistencia muscular. Conclusiones: Existe evidencia científica de que los flavonoides son capaces de mejorar el rendimiento físico deportivo principalmente al disminuir la fatiga e incrementar la resistencia muscular.

Introduction: Physical exercise can generate reactive oxygen species that damage essential cellular components, such as fatigue. Flavonoids, due to their low toxicity and antioxidant activity, have been studied as potential dietary supplements to improve sports performance. Objective: To describe the scientific evidence that has been obtained on the efficacy of the use of flavonoids as supplements to improve sports physical performance. Methods: A search was carried out, in PubMed and Google Scholar databases, on the efficacy of the use of flavonoids as supplements for physical and sports performance. The keywords were used flavonoid, supplementation, sport, exercise, fatigue, muscle, fats, physical activity. Articles published from 2018 to 2022, in English, that met the selection criteria were taken into account. Results: Flavonoids are capable of reducing fatigue due to physical exertion in a sports context, mainly due to their ability to regulate the activity of endogenous antioxidant agents such as superoxide dismutase, catalase and glutathione peroxidase enzymes, which are responsible for the neutralization of reactive oxygen species. In addition, they are capable of favoring the neutralization of toxic metabolites that are generated during exercise and of increasing energy reserves (glycogen in the liver and muscles) and muscular resistance. Conclusions: There is scientific evidence that flavonoids are capable of improving sports physical performance, mainly by reducing fatigue and increasing muscular resistance.

Phytochemical Screening and Antibacterial Activity of Chrysophyllum albidum Collected in Nsukka, South East Nigeria

Background: Chrysophyllum albidum is widely used by African people for the treatment of various types of diseases such as ear infection, sore throat, typhoid, cellulites, septicaemia, bactericemia, abscesses and tooth infections. Aim: The study was conducted to investigate the chemical components and antibacterial activity of the extract and fractions from the root bark of Chrysophyllum albidum from Nsukka, South-east Nigeria. Methodology: The fresh roots were collected, washed, cut into small pieces, air dried and pulverized to powder using mechanical grinder. Extraction and fractionation were done by cold maceration method and technique of liquid–liquid extraction respectively. The phytochemical analysis of the methanol extract and, n-hexane, butanol, aqueous and ethylacetate fractions of the plant part was carried out using standard method. The antibacterial activities were determined using cup-plate agar diffusion and agar dilution methods. Results: The phytochemical screening of the extract revealed the presence of tannins, flavonoids, saponins, terpenoids, alkaloids, reducing sugar and cardiac glycosides. The inhibition zone diameter (IZD) produced by the agents against some selected Gram positive bacteria (GPB) and Gram negative bacteria (GNB) pathogens ranged from 6 – 25 mm and 6 – 12 mm respectively. The MIC and MBC values produced by the extract and fractions of the plant’s part against the GPB ranged from 1.25 – 40 mg/ml and 5 – 80 mg/ml respectively Many of the GNB were not sensitive to the agents tested except Pseudomonas aeruginosa and Klebsiella spp that exhibited mild to moderate sensitivity to the agents. Conclusion: These agents, therefore, exhibited a potent antibacterial activity against all the GPB and a few GNB pathogens tested due to their potent phytochemicals. The results of this work have corroborated the trado-medical use of root of Chrysophyllum albidum for treating ear infection, sore throat, typhoid, cellulites, septicaemia, bactericemia, boils and tooth infection/decay.

Phytochemical, Antioxidant and Anti-diabetic Potentials of the Ethanol Leave Extracts of four Medicinal Plants

For many years, medicinal plants have been a resource for healing in several local communities around the world and the phytochemicals in them such as flavonoids, alkaloids, phenolic, tannins, and terpenoids are attributed to their many medicinal values. Vernonia amydalina, Senna alata, Jatropha curcas, and Grewia pubescens are important plants with immense value. In this study, phytochemical screening, antioxidant analysis and the potential anti-hyperglycemic properties of the plants was investigated in-vitro. The ethanol leave extracts of the plants were subjected to qualitative phytochemical screening and tannin, flavonoids and phenol quantification. Ferric reducing antioxidant power and DPPH radical inhibition of the extracts was done by spectrophotometric method while the anti-diabetic potential was analyzed through the in-vitro ?-amylase and ?-glucosidase inhibition. Phytochemicals detected in the ethanol leave extracts of the four plants are tannins, flavonoids, phenolics, terpenoids, steroids, alkaloids, cardiac glycosides, and saponins. Flavonoids, phenols, and tannin content were highest in Senna alata (0.27±0.0.002 mg: mg of rutin per g of extract, 10.63±0.0.017 mg: mg of gallic acid per g of extract, and 6.72±0.06 mg/g respectively) followed by V. amygdalina (0.20±00.002 mg: mg of rutin per g of extract, 8.27±0.0.017 mg: mg of gallic acid per g of extract, and 7.98±0.03 mg/g respectively). While the least content of all was found in the extracts of Jatropha curcas. Concentration dependent and statistically significant difference was observed in both the FRAP and DPPH radical inhibition of all the extracts. Senna alata showed the strongest reducing power followed by the V. amygdalina. Both Senna alata and V. amygdalina showed DPPH radical inhibition that is not significantly (p>0.05) different from that of trolox. ?-amylase and ?-glucosidase inhibition was also demonstrated in a concentration dependent manner. In both the ?-amylase and ?-glucosidase inhibition, V. amygdalina and S. alata exhibited the most significant inhibitory properties among the plant extracts. The overall result in this study suggested that V. amygdalina, S. alata with the highest content of the phytochemicals, and antioxidant activities are potential source of antioxidant constituents and might be useful for the management of diseases such as diabetes.

In Silico Investigation of Phytochemicals against Typhoid: A Review

Typhoid fever is a serious bacterial infection caused by Salmonella enterica serovar Typhi, and is a major public health issue in developing countries. The emergence of multidrug-resistant strains of S. Typhi has raised concerns about the effectiveness of existing treatments and has prompted the exploration of alternative therapies. Phytochemicals, which are bioactive compounds found in plants, have been investigated as potential sources of new antibacterial agents against typhoid. In this review, we conducted an in silico investigation of phytochemicals and their potential activity against S. Typhi. Our review examined current literature on phytochemicals and their antibacterial activity against S. Typhi. Using molecular docking studies, we investigated the potential binding of these phytochemicals to the target protein, DNA gyrase, which is an important drug target in S. Typhi. Our results indicate that several phytochemicals exhibit promising binding affinities to DNA gyrase, suggesting their potential as effective antibacterial agents against typhoid. Overall, our findings highlight the potential of phytochemicals as a source of new therapeutics for typhoid fever, particularly in regions where multidrug-resistant strains of S. Typhi are prevalent. The in silico approach used in this review provides a valuable tool for screening and identifying potential candidates for further investigation. Further studies are needed to validate the results of in silico studies and to explore the potential of phytochemicals as antibacterial agents against typhoid.

Evaluation of Phytochemical and HPLC analysis of Crotalaria angulata , Momordica cymbalaria , Senna hirsuta and Indigofera linnaei and it’s biological applications

To encompass a quantitative evaluation of phytochemical analysis and HPLC analysis of ethanol extracts of Senna hirsuta ; Indigofera linnaei; Crotalaria angulata and Momordica cymbalaria leaves were experimented to have broad analysis on presence of bioactive components. The phytochemical tests showed the bioactive compounds in Senna hirsuta ethanolic extracts with Steroids, Glycosides, Anthraquinones, Saponins Glycosides, Flavonoids and Terpenoids. In Indigofera linnaei, ethanolic extracts of this plant contain Steroids, Glycosides, Saponins, Glycosides and Terpenoids, Anthraquinones, Tannins, Flavonoids and Saponins are absent for this plant. Test for Steroids, Anthraquinones, Tannins and Terpenoids are strongly present in the plant of Crotalaria angulata . The strong presence of Steroids, Glycosides, Tannins, Terpenoids, Saponins foam in the plant of Momordica cymbalaria . The effects of ethanolic extracts of Anti-Bacterial activity of S.hirsuta and Indigofera linnaei with some of bacteria pathogenic strains such as Shigella dysenteriae, Escherichia coli, Salmonella typhi, Proteus vulgaris, Klebsiella pneumoniae and Bacillus subtilis were experimented . The antibacterial activities of the ethanolic extracts were compared favorably with that standard antibiotic (Chloramphenicol). The Ethanolic extract of leaf showed a maximum zone of inhibition (11 mm) against Escherichia coli, a Gram negative bacteria. In Indigofera linnaei, the ethanolic extract, show a maximum zone of inhibition (19 mm) to Salmonella typhi . In chromatographic technique, the separation and movements of biomolecules has been investigated. Hence, these bio-techniques play a significant role in finding of important material for pharmaceutical industry and have substances that induce a great interest due to their versatile applications . The paper chromatographic technique showed the Rf value at chlorophyll ‘a’ is 0.569 and ‘b’ value 0.123 present in plant Crotalaria angulata . The Rf value at chlorophyll’a’0.569, and ‘b’ value is 0.353 present in the plant Momordica cymbalaria . HPLC analyses allow for the identification of samples of Momordica cymbalaria with peak value of 1676436 and Retention time is 4.092. This particular study revealed the strong quantitative phytochemicals in Crotalaria angulata and Momordica cymbalaria and the same has been found to be the most effective free radical quencher. As a culmination, these plant extracts can be a safe alternative to chemical drugs.

Proximate Analysis, Phytochemical Screening and High Resolution Liquid Chromatography Mass Spectrophotometry Analysis of Essential Oils of Hedychium Coronarium J. Koenig, a Medicinal and Aromatic Plant

Medicinal plants have been used in all cultures as a source of medicine since ages. When parts of plants such as rhizomes, leaves or barks and other natural materials are used as drugs to treat illnesses, they are called crude drugs and the study of crude drugs is called pharmacognosy. Proximate analysis in plants gives valuable information and help to assess the quality of a crude drug. Beneficial effects of crude drugs are believed to be attributed to plant phytochemicals. Hedychium coronarium J. Koenig, a medicinal and aromatic plant of high value is an endangered and red-listed plant. The rhizome of this plant is used for the treatment of various diseases. Crude extracts prepared from the rhizomes show antibacterial and antifungal properties. Essential oils obtained from Hedychium coronarium are found to be rich in terpenes and used for bactericidal, fungicidal, medicinal and cosmetic applications. The present study assesses the quality of crude drugs prepared from this highly medicinal plant. Proximate analysis and phytochemical screening of rhizomes of Hedychium coronarium, which is frequently consumed as food and as medicine were carried out. Ash content was found to be low) when compared to the moisture content. The water extractive value was more than alcohol extractive. Preliminary tests carried out on phytochemicals revealed the presence of terpenoids and oils. High Resolution Liquid Chromatography Mass Spectrophotometry was carried to ascertain the different components of essential oils and revealed the presence of eucalyptol (1,8-cineole), caryophyllene oxide, camphor, linoleic acid, ricinin, phloroglucinol, 6-gingerol, carvone and arjungenin.

A comprehensive overview on the role of phytocompounds in human immunodeficiency virus treatment / 中西医结合学报

Acquired immune deficiency syndrome (AIDS) is a worldwide epidemic caused by human immunodeficiency virus (HIV) infection. Newer medicines for eliminating the viral reservoir and eradicating the virus are urgently needed. Attempts to locate relatively safe and non-toxic medications from natural resources are ongoing now. Natural-product-based antiviral candidates have been exploited to a limited extent. However, antiviral research is inadequate to counteract for the resistant patterns. Plant-derived bioactive compounds hold promise as powerful pharmacophore scaffolds, which have shown anti-HIV potential. This review focuses on a consideration of the virus, various possible HIV-controlling methods and the recent progress in alternative natural compounds with anti-HIV activity, with a particular emphasis on recent results from natural sources of anti-HIV agents. Please cite this article as: Mandhata CP, Sahoo CR, Padhy RN. A comprehensive overview on the role of phytocompounds in human immunodeficiency virus treatment. J Integr Med. 2023; 21(4):332-353.

Applicability of an HPLC method for analysis of alcoholic and glycolic Brazilian green-propolis extracts

Abstract Brazilian green propolis has been widely used in food and pharmaceutical products due to its valuable source of phenolic compounds and versatile biological activities. The development and validation of analytical methods are extremely useful for the characterization and quality control of products containing propolis. Therefore, the aim of this study was to optimize, validate and investigate the applicability of a reversed-phase HPLC method for analysis of different types of Brazilian green propolis extracts (glycolic and ethanolic). The method showed to be selective for the propolis phenolic markers. The analysis of variance and residues demonstrated that the method had significant linear regression, without lack of fit. It was also a precise, accurate and robust method, which was of utmost importance to analyze both glycolic and ethanolic extracts and at different concentrations. Moreover, as these products can display most complex matrices to analyze, a valid HPLC method can also prove to be specific and versatile.

Association between the Phytochemical Index and Risk Factors for Cardiovascular Disease in Adults

Abstract Background There are few publications about the association between the phytochemical index (PI) and risk factors for cardiovascular disease. Objective To evaluate the association between the PI and risk factors for cardiovascular disease in adults. Methods This was a cross-sectional study with 141 adults, between 20 and 59 years of age. We analyzed lifestyle (physical activity), sociodemographic data (sex, age), anthropometric data (body mass index [BMI], waist circumference [WC]), biochemical data (lipid profile, blood glucose), food consumption, and phytochemical intake (expressed as PI = daily energy derived from phytochemical-rich foods ÷ total daily energy intake × 100). We performed bivariate analyses (Spearman's correlation) and multiple linear regression adjusted for potential confounders, considering p < 0.05 as significant. Results The median PI was 9.80 (interquartile range: 11.45). PI was inversely correlated with BMI (rs: −0.43) and WC (rs: −0.36) and positively correlated with high-density lipoprotein cholesterol (HDL-cholesterol) (rs: 0.25), all with p < 0.05. In multiple regression analysis, PI was inversely associated with BMI (B: −0.08; 95%CI: −0.15, −0.01) after adjusting for total energy, sex, age, and physical activity; and positively associated with HDL-cholesterol (Model 1 adjusted for total energy, sex, age, and physical activity [B: 0.21; 95% CI: 0.02, 0.41]; Model 2 adjusted for BMI, sex, age, and physical activity [B: 0.21; 95% CI: 0.008, 0.40]; Model 3 adjusted for WC, sex, age, and physical activity [B: 0.20; 95%CI: 0.01, 0.40]), all with p < 0.05. Conclusion The results have demonstrated that higher phytochemical intake, expressed by PI, was inversely associated with BMI and positively associated with HDL-cholesterol.

Acute and subacute oral toxicity characterization and safety assessment of COVID organics® (Madagascar's Anti­COVID Herbal Tea) in animal models

Introduction: Coronavirus disease 2019 (COVID 19) is an infectious disease caused by severe acute respiratory syndrome coronavirus 2. No drug has been generally approved as safe and effective for the treatment of COVID 19. Several therapeutic agents such as COVID Organics® (CVO) have been explored as treatment options. CVO is an herbal tea composed of 62% of Artemisia annua and 38% of other plants. There is presently no existing scientific report and data on the safety and efficacy of CVO herbal drug. Thus, acute and subacute toxicity studies were undertaken to evaluate the safety and toxicity of CVO on short and long term usage in animal models. Materials and Methods: Phytochemical and nutritional compositions of CVO were determined using standard methods. Acute oral toxicity was investigated using female Swiss albino mice (three per group). While subacute oral toxicity was done using female and male Swiss albino rats (five per group). The animals were administered 2000 mg/kg, 5000 mg/kg, therapeutic dose; 5500 mg/kg and supratherapeutic dose; 11,000 mg/kg of CVO herbal product. The control group received water ad libitum. The oral toxicity studies were done in accordance with Organization for Economic Corporation and Development guidelines. The experimental protocol was approved by the Institutional Animal Care and Use Committee, Nigerian Institute of Medical Research (Ethics No. IRB/17/043). Results: CVO is rich in antioxidants: flavonoids(10.3%), tannins(29.1%), and phenolics(434.4 mg). It contains proteins (33.8%), carbohydrates (34.5%), fat (6.8%), and fiber (0.5%). In the acute toxicity study, no mortality was recorded in all the treated and untreated groups. The lethal dose of CVO is >5000 mg/kg body weight. The hematological, biochemical, lipid profile, and histologic parameters were all normal at therapeutic doses when compared to the control group. Conclusion: The acute and subacute oral toxicity studies revealed that CVO is not toxic. The specific organ toxicity evaluations also indicated that CVO has no toxic effects on blood parameters and vital organs structure and function at therapeutic dose. Thus, CVO is safe for short and long term usage. We recommend that CVO should be subjected to efficacy studies to investigate whether it is effective for COVID 19 treatment as claimed by the manufacturer.

Phytochemicals Screening and Anti-proliferative Activities of Anacardium occidentale Shoot Extract in Breast Cancer Cells

@#Introduction: Anacardium occidentale or cashew are popular traditional food and have raised research interest for complementary cancer treatment. Cancer has become leading cause of death and treatment involved severe side effects. In present study, we aim to study the anti-proliferative effects of cashew shoots in breast cancer (MDAMB-231), colorectal cancer (HT-29) and liver cancer (HepG2) cell lines. Methods: Cell lines were treated with 70% ethanolic cashew extract for cytotoxicity test with MTT assay. AO/PI dual fluorescent assay and RNase/PI staining were used to determine apoptosis induction effects. Phytochemicals screening was carried out by using gas chromatography mass spectrometry (GCMS) and liquid chromatography mass spectrometry (LCMS). Results: The cytotoxicity assay of cashew shoot extract demonstrated IC50 of 81.1 ± 0.11 μg/ml for MDA-MB-231, 307.5 ± 2.31 μg/ml for HT-29 and 272.6 ± 1.91 μg/ml for HepG2 cell lines. The apoptotic bodies include chromatin condensation, cell blebbing and nuclear fragmentation and apoptosis induction were shown by AO/PI staining. There was significant increase of cell count in sub-G0 phase in MDA-MB-231 cell lines treated with cashew shoot extract. It was demonstrated that cashew shoot extract contained 38 compounds from GCMS such as sitosterol, tannin, pyrogallol, phenol and 20 compounds from LCMS such as citric acid, gallic acid, myricetin and hinokiflavone that may give rise to its anti-cancer effect. Conclusion: Cashew shoot extract demonstrated potential anti-cancer properties thus further study is required to investigate its mechanism as anti-cancer agent.

Principales fitoquímicos con potencial terapéutico en el tratamiento de la retinopatía diabética con fitofármacos / Major Phytochemicals with Therapeutic Potential in the Treatment of Diabetic Retinopathy

La diabetes mellitus tipo 2 representa uno de los principales problemas de salud pública a nivel mundial hoy en día. Entre las principales complicaciones generadas por esta enfermedad se encuentra la retinopatía diabética, la cual puede conducir a pérdida de la visión de manera permanente, por lo que investigaciones sobre tratamientos para esta patología van en aumento. Es por esto que tratamientos en base a químicos obtenidos de plantas medicinales están siendo ampliamente investigados debido a que podrían proveer una alternativa más segura, de menor costo y menor toxicidad que la medicina estándar para el tratamiento de esta patología ocular de alta incidencia mundial. El objetivo de este estudio fue identificar los principales fitoquímicos con potencial para ser usados como tratamiento de la retinopatía diabética. Para lograr este cometido se llevó a cabo una revisión de la literatura publicada entre el enero 2017 y de junio 2021 utilizando las bases de datos WOS, PubMed y Scopus en inglés y español, con el fin de recopilar evidencia científica actualizada sobre el uso y efectos de fitoquímicos en la retinopatía diabética. Diversas familias de fitoquímicos útiles fueron identificadas, entre estas las más comunes fueron las de origen fenólico, aunque menos comunes también se encontraron carotenoides, terpenos y preparaciones constituidas por varias especies de plantas y fitoquímicos. Sus mecanismos de acción también fueron identificados, siendo los más comunes la supresión de la neovascularización mediada por VEGF, la protección y restauración de la barrera hematorretinal, la reducción en la actividad de las especies reactivas del oxígeno y el efecto antiinflamatorio. Dada la evidencia respecto a la utilidad de los fitoquímicos para el tratamiento de la retinopatía diabética, mayores investigaciones deben ser realizadas(AU)

Type 2 diabetes mellitus represents one of the main public health problems worldwide today. Among the main complications generated by this disease is diabetic retinopathy, which can lead to permanent vision loss. For this reason, research on treatments for this pathology is increasing. This is why treatments based on chemicals obtained from medicinal plants are widely investigated as they could provide a safer, less costly and less toxic alternative to standard medicine for the treatment of this eye disease of high incidence worldwide. The aim of this study was to identify the main phytochemicals with potential to be used as treatment for diabetic retinopathy. In order to achieve this purpose, a review of the literature published between January 2017 and June 2021 was conducted using the WOS, PUBMED and Scopus databases in English and Spanish, in order to compile updated scientific evidence on the use and impact of phytochemicals in diabetic retinopathy. Several families of useful phytochemicals were identified. Among these, the most common were those of phenolic origin, although less common were also found carotenoids, terpenes and blends consisting of various plant species and phytochemicals. Their mechanisms of action were also identified, the most common being suppression of vascular endothelial growth factor-mediated neovascularization, protection and restoration of the blood-retinal barrier, reduction in reactive oxygen species activity and anti-inflammatory effect. Given the evidence regarding the usefulness of phytochemicals for the treatment of diabetic retinopathy, further research should be conducted(AU)

Phytochemical Screening and Antimicrobial Properties of Carissa edulis Extracts Obtained from Kaimosi Forest, Vihiga County, Kenya

Medicinal plants still play an important role in human and animal healthcare. About 60% of the world’s population and 80% of Africa’s population depend on herbal medicine for their primary healthcare. In Vihiga county Kenya, C. edulis has been reported to manage several human disease conditions such as epilepsy, headache, toothache, cough, chest complaints, sickle cell anemia, gonorrhea, syphilis and rabies among others. Its therapeutic efficacy is attributed to numerous phytochemicals present in its extracts. In this study, a phytochemical analysis was carried out in the roots, leaves and bark extracts, antimicrobial effects on Escherichia coli and staphylococcus aureus laboratory cultures determined. The extracts were modified by grinding and ethanol used as solvent in the extraction. Different concentrations of 25%, 50%, 75% and 100% of plant extracts were used in the analysis and sterile distilled water used as the control. Data on zone growth inhibition was subjected to analysis of variance and the means were separated and compared using least significant differences at p? 0.05 by use of SAS statistical package. The results showed the presence of an array of phytochemicals in the leaves, bark and roots of the plant. The bark for example tested positive for tannins, saponins, flavanoids, terpenoids, glycosides and sterols while the leaves and roots tested negative for saponins and flavanoids respectively. The leaves exhibited the greatest inhibition against Escherichia coli with a mean diameter of 7.57mm and all the three parts exhibited a significant difference. The different concentrations also showed that inhibition increased with increase in concentration. The mean inhibition diameter at 100% was 8.96 while at 25% it was 7.21.

Estudo do potencial antiviral sobre o Sars-Cov-2 dos compostos identificados no extrato bruto das folhas de Tetradenia riparia / Study of antiviral potential on Sars-Cov-2 of compounds identified in Tetradenia riparia leaves crude extract / Estudio del potencial antiviral sobre el Sars-Cov-2 de los componentes identificados en el extracto crudo de las hojas de Tetradenia riparia

A COVID-19 surgiu de forma repentina, acometendo milhões de pessoas e causando muitas mortes no mundo todo. Diante disso, torna-se necessário a busca de substâncias bioativas com propriedades antivirais. No Brasil, a espécie Tetradenia riparia foi inserida como planta ornamental exótica, com aroma intenso e agradável, sendo cultivada em parques, jardins, residenciais e hortos. O objetivo deste estudo foi identificar compostos presentes no extrato bruto das folhas de Tetradenia riparia com interesse antiviral. O extrato bruto das folhas secas foi obtido por maceração dinâmica por esgotamento do solvente e após, concentrado em evaporador rotativo. A composição química do extrato bruto foi analisada por cromatografia líquida de ultra eficiência acoplada à espectrometria de massas de alta resolução (UHPLC-ESI/qTOF). Foram identificados 31 compostos que foram investigados por meio de levantamento bibliográfico quanto ao seu potencial anti- SARS-CoV-2. Os compostos rosmanol, procianidina, cianidina, betulina, ácido betulínico e o ácido sagerínico, apresentaram potencial atividade antiviral sobre o SARS-CoV-2. Esta investigação é promissora, indicando possivelmente que no extrato bruto das folhas de T. ripária existem compostos que podem combater o SARS-CoV-2. Neste sentido, estudos de ancoramento molecular (docking) e análises in silico sobre a proteína Mpro do vírus devem ser realizadas corroborando desta forma a ação dos compostos identificados.

COVID-19 appeared suddenly, affecting millions of people and causing many deaths worldwide. Therefore, it is necessary to search for bioactive substances with antiviral properties. In Brazil, Tetradenia riparia was inserted as an exotic ornamental plant, with an intense and pleasant aroma, cultivated in parks, residential and vegetable gardens. This study aimed to identify compounds present in the crude extract of Tetradenia riparia leaves with antiviral interest. The crude extract of the dried leaves was obtained by dynamic maceration with solvent exhaustion and then concentrated in a rotary evaporator. The chemical composition of the crude extract was analyzed by ultra- performance liquid chromatography coupled with high-resolution mass spectrometry (UHPLC- ESI/qTOF). We identified 31 compounds investigated through a literature review for their anti- SARS-CoV-2 potential. The compounds rosmanol, procyanidin, cyanidin, betulin, betulinic acid, and sagerinic acid showed potential antiviral activity against SARS-CoV-2. Therefore, this investigation is promising, possibly indicating that in the crude extract of T. riparia leaves, there are compounds that can fight SARS-CoV-2. In this sense, molecular docking studies and in silico analyzes on the virus Mpro protein must be carried out, thus corroborating the action of the identified compounds.

SARS-CoV-19 ha aparecido repentinamente, afectando a millones de personas y causando muchas muertes en todo el mundo. Por ello, se hace necesaria la búsqueda de sustancias bioactivas con propiedades antivirales. En Brasil, la especie Tetradenia riparia ha sido introducida como planta ornamental exótica, con un aroma intenso y agradable, siendo cultivada en parques, jardines, residencias y centros de jardinería. El objetivo de este estudio fue identificar los compuestos presentes en el extracto crudo de las hojas de Tetradenia riparia con interés antiviral. El extracto crudo de las hojas secas se obtuvo por maceración dinámica por agotamiento del disolvente y después, se concentró en el evaporador rotatorio. La composición química del extracto crudo se analizó mediante cromatografía líquida de ultra rendimiento acoplada a espectrometría de masas de alto rendimiento (UHPLC-ESI/qTOF). Se identificaron 31 compuestos y se investigó su potencial anti-SARS-CoV-2 mediante un estudio bibliográfico. Los compuestos rosmanol, procianidina, cianidina, betulina, ácido betulínico y ácido sagerínico, mostraron una potencial actividad antiviral sobre el SARS-CoV-2. Esta investigación es prometedora, pues posiblemente indica que en el extracto crudo de las hojas de T. riparia hay compuestos que pueden combatir el SARS-CoV-2. En este sentido, deben realizarse estudios de docking y análisis in silico sobre la proteína Mpro del virus para corroborar la acción de los compuestos identificados.

Phytochemical Analysis and In-vitro Antioxidant Activities of Some Selected Higher Fungi from Oyo State, South West of Nigeria

Higher-fungi (Hf) of the polypore mushrooms are considered to have unique secondary metabolites, making them reservoirs of therapeutically significant bioactive compounds. Phytochemical and antioxidant properties of the Hf were accessed in this study. Four Hf, which were found in several wild locations in Oyo state, Nigeria, were collected. At the University of Ibadan Botany Department Laboratory, the species of the four Hf were determined. In-vitro antioxidant activity were assessed using the 1,1-Diphenyl-2-picrylhydrazyl (DPPH), Ferric Reducing Antioxidant Power (FRAP), and Hydrogen peroxide (H2O2) assays using methanol extracts of air-dried and powdered Hf. Results were presented as Mean SEM, graphs were created in Excel, one-way ANOVA was used for the analysis, and p ?0.05 was regarded as significant. These Hf were identified as Lycoperdon rimlatum (Lr) FFUI1, Trametes versicolor (Tv) FFUI2, Ganoderma lucidum (Gl) FFUI3, and Daedelia quarcina (Dq) FFUI4 and were recorded on the NCBI with accession numbers EU833664.1, JQ621899, JQ520179.1 and KP171209.1, respectively. All the Hf showed positive tests for the presence of saponin, tannin, alkaloid, terpenoid, carbohydrate,tannin and flavonoids. The Hf showed antioxidant activities, the highest DPPH inhibition was by Tv (94.48%), FRAP was by Gl (0.16 mg/g) and H2O2 inhibition was by Lr (70.90%). The antioxidant activities observed were due to the presence of useful phytochemicals making them therapeutically significant.

Review of the Literature on Oral Cancer: Epidemiology, Management and Evidence-based Traditional Medicine Treatment

Oral cavity cancers are part of the upper aerodigestive tract cancers and represent a significant burden worldwide. Its epidemiology varies from country to country with high frequencies in South East Asian countries. Tobacco and alcohol are the main risk factors. Survival of oral cancer is low i.e., less than 40% in the advanced stage (stage III and IV), diagnosis of oral cavity cancer is based on a complete clinical examination of the oral cavity complete with biopsy, bio-markers are an adjunct to screening and diagnosis of oral cavity cancers, surgery, radiotherapy, chemotherapy and immunotherapy are part of the therapeutic armamentarium of oral cancer but also have limitations. Traditional medicine is an important and proven alternative in the treatment and support of patients with oral cavity cancer. Prevention of oral cavity cancers includes not only early detection of precancerous and cancerous lesions but also control of risk factors and education of the population. Surgery, radiotherapy, chemotherapy and immunotherapy are part of the therapeutic strategy of oral cancer treatment but also have limitations. Traditional Medicine is an important and proven alternative in the treatment and support of patients with oral cavity cancer. It is thus desirable to scientifically validate phytochemicals in order to integrate alternative medicine as part of national cancer management strategy. In silico advanced studies on secondary metabolites of medicinal plants traditionally used to treat oral cancer are in progress.

Nutritional Contents of Two Varieties of Sweet Potatoes (Ipomoea batatas (L.) Lam ) Cultivated IN North Western Nigeria

Background and Objectives: Food shortages and nutritional imbalances are among the main food security problems in many countries around the world. In this study, the nutrients content of the yellow and red-fleshed sweet potatoes varieties cultivated in Nigeria were assessed. Materials and Methods: The proximate composition, mineral elements analysis, phytochemicals, and vitamins content of the red and yellow-fleshed sweet potatoes were determined using the standard methods of analysis. Results: The proximate analysis has shown that, the moisture (17.927%) and fat (2.703%) content of the yellow sweet potato were significantly (p<0.05) higher than in the red potato with a content of 16.68% and 1.693% respectively. The protein and fiber content of the red potato are 14.280% and 14.572% respectively, this is quite higher than in the yellow cultivar having 12.987% and 10.443% of the nutrients respectively. The ash and carbohydrate content were same in both. The red potato exhibits high level of sodium (11.420 mg/l), potassium (1.206 mg/l), and magnesium (8.468 mg/l) in contrast to the red potato containing 10.270 mg/l, 1.035 mg/l and 6.127 mg/l of the respective elements. Iron and zinc content were comparable in both cultivars while the calcium content (1.444 mg/l) of the yellow cultivar is significantly higher than in the red variety (1.144 mg/l). The vitamin A, B and E content of the red potato are 8.740 µmol/L, 2.977 mg/dl, and 13.267 mg/dl respectively. These values are significantly (p<0.05) higher than in the yellow potato containing 6.047 µmol/L, 1.680 mg/dl, and 11.110 mg/dl of the respective vitamins. There is no significant difference with respect to the vitamin C content of both yellow (11.850 mg/dl) and red potato (12.520 mg/dl). The phytochemicals: tannins, flavonoids, phenols, terpenes, and anthocyanins content of the red sweet potato are 0.967 mg/g, 1.577 mg/g, 1.867 mg/g, 6.590 mg/g and 2.660 mg/g respectively. Terpenes and anthocyanins were not found in the yellow cultivar. However, saponins (0.823 mg/g) were found in the yellow variety but not in the red potato. Amount of the tannins, flavonoids and phenols observed in the yellow-fleshed potato are 0.667 mg/g, 1.027 mg/g and 1.287 mg/g respectively. These values are lower than in the corresponding red potato. Conclusion: In this study, the nutritional contents of sweet potato varieties have been assessed which will immensely contribute to reducing the menace of malnutrition bedeviling the Northwestern part of Nigeria.

Acute toxicity study and phytochemical screening of Pterocarpus marsupium heartwood

Background: Conventionally, Ayurvedic herbs are being used to treat various diseases. These medicinal compounds have to be evaluated for their safety and presence of therapeutic compounds for the clinical application. Aims and Objectives: The present study was designed to obtain the scientific knowledge on the safety profile as well as to assess the presence of pharmacologically active principles in the Pterocarpus marsupium heartwood. Materials and methods: The aqueous extract of P. marsupium heartwood was subjected to an acute toxicity in albino rats. The animals were divided into four groups (n = 6) and fed with graded doses (1000, 2000, and 5000 mg/kg p.o.) of plant extract, respectively, whereas control group had received 2 ml distilled water orally. Animals were continuously observed for the toxicological symptoms for 2 h and intermittently for 48 h and latter once in a day for 14 days. The body weight of the animals was recorded. In addition, the qualitative phytochemical investigations were conducted to identify the presence of active principles. Results: The animals fed with aqueous extract of P. marsupium heartwood did not exhibit any toxic symptoms and the mortality. However, there was a significant (P < 0.05) dose-dependent change in the weight gain observed in comparison to the control group. The median lethal dose (LD50) of the plant extract was considered as >5000 mg/kg. Furthermore, the phytochemical investigations of the plant extract showed the presence of carbohydrates, flavonoids, triterpenoids, saponins, tannins and phenols. Conclusion: The aqueous extract of P. marsupium heartwood was found to be safe and well tolerated even at a large dose of 5000 mg/kg. Furthermore, the plant extract found to possess pharmacologically active principles having wide pharmacological spectrum. Hence, it can be preferred in various therapeutic conditions.