ABSTRACT
Intramuscular haemangiomas (IH) are rare lesions, accounting for less than 1% of all haemangiomas. This article presents the case of a woman in her 40s with a swelling in her left cheek. CT revealed an intramuscular lesion within the masseter, suggestive of a venous malformation. Surgical treatment was carried out with intraoral access to the lesion, allowing for complete removal, resulting in temporary swelling and trismus. There was no facial paralysis. We discuss information on IH in the head and neck and their surgical approaches.
Subject(s)
Hemangioma, Cavernous , Masseter Muscle , Humans , Masseter Muscle/pathology , Masseter Muscle/surgery , Female , Hemangioma, Cavernous/surgery , Hemangioma, Cavernous/diagnostic imaging , Hemangioma, Cavernous/pathology , Adult , Muscle Neoplasms/surgery , Muscle Neoplasms/diagnostic imaging , Muscle Neoplasms/pathology , Tomography, X-Ray ComputedABSTRACT
This review presents advances in the implementation of high - throughput se quencing and its application to the knowledge of medicinal plants. We conducted a bibliographic search of papers published in PubMed, Science Direct, Google Scholar, Scopus, and Web of Science databases and analyzed the obtained data using VOSviewer (versi on 1.6.19). Given that medicinal plants are a source of specialized metabolites with immense therapeutic values and important pharmacological properties, plant researchers around the world have turned their attention toward them and have begun to examine t hem widely. Recent advances in sequencing technologies have reduced cost and time demands and accelerated medicinal plant research. Such research leverages full genome sequencing, as well as RNA (ribonucleic acid) sequencing and the analysis of the transcr iptome, to identify molecular markers of species and functional genes that control key biological traits, as well as to understand the biosynthetic pathways of bioactive metabolites and regulatory mechanisms of environmental responses. As such, the omics ( e.g., transcriptomics, metabolomics, proteomics, and genomics, among others) have been widely applied within the study of medicinal plants, although their usage in Colombia is still few and, in some areas, scarce. (185)
El extracto de cloroformo (CE) y las fracciones obtenidas de las raíces de Aldama arenaria se evaluaron para determinar su actividad antiproliferativa in vitro contra 10 líneas ce lulares tumorales humanas [leucemia (K - 562), mama (MCF - 7), ovario que expresa un fenotipo resistente a múltiples fármacos (NCI/ADR - RES), melanoma (UACC - 62), pulmón (NCI - H460), próstata (PC - 3), colon (HT29), ovario (OVCAR - 3), glioma (U251) y riñón (786 - 0)]. CE presentó actividad antiproliferativa débil a moderada (log GI 50 medio 1.07), mientras que las fracciones 3 y 4, enriquecidas con diterpenos de tipo pimarane [ent - pimara - 8 (14), ácido 15 - dien - 19 - oico y ent - 8(14),15 - pimaradien - 3 ß - ol], presentaron activid ad moderada a potente para la mayoría de las líneas celulares, con un log GI 50 medio de 0.62 y 0.59, respectivamente. Los resultados mostraron una acción antiproliferativa in vitro prometedora de las muestras obtenidas de A. arenaria , con los mejores resul tados para NCI/ADR - RES, HT29 y OVCAR - 3, y valores de TGI que van desde 5.95 a 28.71 µg.mL - 1, demostrando que los compuestos de esta clase pueden ser prototipos potenciales para el descubrimiento de nuevos agentes terapéuticos
Subject(s)
Plants, Medicinal , High-Throughput Nucleotide Sequencing , Multiomics , Medicine, Traditional , ColombiaABSTRACT
Chagas disease, caused by the protozoan Trypanosoma cruzi, affects 6-7 million people worldwide. The dichloromethane extract obtained from the aerial parts of Gymnocoronis spilanthoides var subcordata showed trypanocidal activity in vitro. The fractionation of the dewaxed organic extract via column chromatography led to the isolation of three diterpenoids: ent-9α,11α-dihydroxy-15-oxo-kaur-16-en-19-oic acid or adenostemmoic acid B, (16R)-ent-11α-hydroxy-15-oxokauran-19-oic acid and ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic acid. These compounds showed IC50 values of 10.6, 15.9 and 4.8 µM against T. cruzi epimastigotes, respectively. When tested against amastigotes, the diterpenoids afforded IC50 values of 6.1, 19.5 and 60.6 µM, respectively. The cytotoxicity of the compounds was tested on mammalian cells using an MTT assay, resulting in CC50s of 321.8, 23.3 and 14.8 µM, respectively. The effect of adenostemmoic acid B on T. cruzi was examined at the ultrastructural level using transmission microscopy. Treatment with 20 µM for 48 h stimulated the formation of abnormal cytosolic membranous structures in the parasite. This compound also showed an anti-inflammatory effect in murine macrophages stimulated with LPS and other TLR agonists. Treatment of macrophages with adenostemmoic acid B was able to reduce TNF secretion and nitric oxide production, while increasing IL-10 production. The combination of adenostemmoic acid B with benznidazole resulted in greater inhibition of NF-kB and a decrease in nitrite concentration. The administration of adenostemmoic acid B to mice infected with trypomastigotes of T. cruzi at the dose of 1 mg/kg/day for five days produced a significant decrease in parasitemia levels and weight loss. Treatment with the association with benznidazole increased the survival time of the animals. In view of these results, adenostemmoic acid B could be considered a promising candidate for further studies in the search for new treatments for Chagas disease.
ABSTRACT
Ent-hardwickiic acid is the major compound of Copaifera pubiflora Benth oleoresin traditionally used in Brazilian folk medicine as an antimicrobial agent. Microbial transformation of ent-hardwickiic by Cunninghamella elegans ATCC 10028b resulted in two and five antifungal derivatives (four new ones) produced in the Czapek modified and Koch's K1 media, respectively. The derivatives were isolated and their structures were determined by spectral analysis, namely 1D/2D NMR and HR-ESIMS. All compounds were tested for cytotoxic and antifungal activities and they were not cytotoxic to the tested cell lines, but all derivatives showed fungicidal activity against Candida glabrata and Candida krusei, which have emerged as resistant to fluconazole. One of the yet unreported biotransformation products displayed the strongest activity with minimum fungicidal concentration values smaller than the other compounds, including fluconazole.
Subject(s)
Antifungal Agents , Diterpenes , Fluconazole , Fluconazole/pharmacology , Candida , Molecular Structure , Microbial Sensitivity TestsABSTRACT
Trypanosoma cruzi is the pathogen of Chagas disease, a neglected tropical disease that affects more than 6 million people worldwide. There are no vaccines to prevent infection, and the therapeutic arsenal is very minimal and toxic. The unique E-NTPDase of T. cruzi (TcNTPDase1) plays essential roles in adhesion and infection and is a virulence factor. Quercetin is a flavonoid with antimicrobial, antiviral, and antitumor activities. Its potential as a partial inhibitor of NTPDases has also been demonstrated. In this work, we synthesized the non-natural L-glycoside derivatives of quercetin and evaluated them as inhibitors of recombinant TcNTPDase1 (rTcNTPDase1). These compounds, and quercetin and miquelianin, a natural quercetin derivative, were also tested. Compound 16 showed the most significant inhibitory effect (94%). Quercetin, miquelianin, and compound 14 showed inhibition close to 50%. We thoroughly investigated the inhibitory effect of 16. Our data suggested a competitive inhibition with a Ki of 8.39 µM (± 0.90). To better understand the interaction of compound 16 and rTcNTPDase1, we performed molecular dynamics simulations of the enzyme and docking analyses with the compounds. Our predictions show that compound 16 binds to the enzyme's catalytic site and interacts with important residues for NTPDase activity. As an inhibitor of a critical T. cruzi enzyme, (16) could be helpful as a starting point in the developing of a future treatment for Chagas disease. Furthermore, the discovery of (16) as an inhibitor of TcNTPDase1 may open new avenues in the study and development of new inhibitors of E-NTPDases.
ABSTRACT
This study aimed at evaluating the potential of Copaifera lucens, specifically its oleoresin (CLO), extract (CECL), and the compound ent-polyalthic acid (PA), in combating caries and toxoplasmosis, while also assessing its toxicity. The study involved multiple assessments, including determining the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against cariogenic bacteria. CLO and PA exhibited MIC and MBC values ranging from 25 to 50 µg/mL, whereas CECL showed values equal to or exceeding 400 µg/mL. PA also displayed antibiofilm activity with minimum inhibitory concentration of biofilm (MICB50) values spanning from 62.5 to 1000 µg/mL. Moreover, PA effectively hindered the intracellular proliferation of Toxoplasma gondii at 64 µg/mL, even after 24 h without treatment. Toxicological evaluations included in vitro tests on V79 cells, where concentrations ranged from 78.1 to 1250 µg/mL of PA reduced colony formation. Additionally, using the Caenorhabditis elegans model, the lethal concentration (LC50) of PA was determined as 1000 µg/mL after 48 h of incubation. Notably, no significant differences in micronucleus induction and the NDI were observed in cultures treated with 10, 20, or 40 µg/mL of CLO. These findings underscore the safety profile of CLO and PA, highlighting their potential as alternative treatments for caries and toxoplasmosis.
ABSTRACT
From the bioactive extract of the euphorbiaceous Croton niveus Jacq., three previously unreported ent-rosane diterpenes have been isolated and characterized by conventional methods, in addition to the known compounds lupeol, cajucarinolide and some phytosterols. Two of the ent-rosane diterpenes displayed activity against HCT-15 and PC-3 cancer cell lines, and the results of docking calculations of these compounds with NF-κB and STAT3 receptors agreed with the proposed mode of action of diterpenes against PC-3 cells.
Subject(s)
Antineoplastic Agents , Croton , Diterpenes, Kaurane , Diterpenes , Euphorbiaceae , Molecular Structure , Diterpenes/pharmacology , Antineoplastic Agents/pharmacologyABSTRACT
Life-threatening Candida infections have increased with the COVID-19 pandemic, and the already limited arsenal of antifungal drugs has become even more restricted due to its side effects associated with complications after SARS-CoV-2 infection. Drug combination strategies have the potential to reduce the risk of side effects without loss of therapeutic efficacy. The aim of this study was to evaluate the combination of ent-hardwickiic acid with low concentrations of amphotericin B against Candida strains. The minimum inhibitory concentration (MIC) values were determined for amphotericin B and ent-hardwickiic acid as isolated compounds and for 77 combinations of amphotericin B and ent-hardwickiic acid concentrations that were assessed by using the checkerboard microdilution method. Time-kill assays were performed in order to assess the fungistatic or fungicidal nature of the different combinations. The strategy of combining both compounds markedly reduced the MIC values from 16 µg/mL to 1 µg/mL of amphotericin B and from 12.5 µg/mL to 6.25 µg/mL of ent-hardwickiic acid, from isolated to combined, against C. albicans resistant to azoles. The combination of 1 µg/mL of amphotericin B with 6.25 µg/mL of ent-hardwickiic acid killed all the cells of the same strain within four hours of incubation.
ABSTRACT
PURPOSE: To relate the creation and expert validation (face and content validity) of an affordable three-dimensional (3-D) printed model of temporal bones with chronic otitis media with cholesteatoma (COMC) as a simulator for mastoidectomy. METHODS: We performed computed tomography (CT) of the temporal bones of a patient with COMC followed at the University of São Paulo (USP) Hospital with 3-D Slicer to create a 3-D model of the affected bone using light-curing resin and silicone (cholesteatoma). The final 3-D printed images were scored by 10 otologists using a customized version of the Michigan Standard Simulation Scale Experience (MiSSES). Internal consistency and inter-rater reliability were assessed using Cronbach's α and intraclass correlations. RESULTS: Otologists consistently scored the model positively for fidelity, educational value, reactions, and the overall model quality. Nine otologists agreed that the model was a good educational device for surgical training of COMC. All experts deemed the model ready-or nearly ready-for use. The final cost of the model, including raw materials and manufacturing, was 120 USD. CONCLUSIONS: Using 3-D printing technology, we created the first anatomically accurate, low-cost, disease-reproducing 3-D model of temporal bones for mastoidectomy training for cholesteatoma.
Subject(s)
Cholesteatoma , Mastoidectomy , Humans , Mastoidectomy/education , Reproducibility of Results , Printing, Three-Dimensional , Temporal Bone/diagnostic imaging , Temporal Bone/surgery , Cholesteatoma/surgeryABSTRACT
OBJECTIVES: The aim of the study was to compare lecture-based teaching and simulation-based hybrid training for ENT induction and objectively assess the performance of trainees in a simulated environment. METHODS: This is a prospective interventional study that included 60 interns in their rotatory internship with no prior exposure to ENT emergencies. The interns came in batches of 5â6 for their 15-days ENT postings. On the first day, a pre-test questionnaire, lecture-based teaching on three scenarios and then allocation into one of the three simulation groups- Group A (Tracheostomy group), Group B (Nasogastric tube group), and Group C (Epistaxis group) was done. Hands-on simulation training was given only to the assigned group. At the end of 15-days, post-test questionnaire and an objective assessment of the three scenarios in a simulated environment was conducted. The same training was repeated for each batch of participants who attended the posting. RESULTS: The participants had significant improvement in the post-test scores in all three scenarios (pâ¯<⯠0.05), and these improvements were marked in those who had received simulated training. On comparing simulation scores, the participants who received hands-on training on a particular scenario outperformed other (pâ¯<⯠0.05). CONCLUSION: Simulation-based training improves cognition and overall confidence in managing ENT skills and emergencies. In simulation training, objective and standardized assessment is the key to achieve specific learning objectives to improve the psychomotor and cognitive skill. LEVEL OF EVIDENCE: II.
Subject(s)
Internship and Residency , Simulation Training , Humans , Emergencies , Prospective Studies , Tracheostomy , Clinical CompetenceABSTRACT
Abstract Objectives: The aim of the study was to compare lecture-based teaching and simulation-based hybrid training for ENT induction and objectively assess the performance of trainees in a simulated environment. Methods: This is a prospective interventional study that included 60 interns in their rotatory internship with no prior exposure to ENT emergencies. The interns came in batches of 5-6 for their 15-days ENT postings. On the first day, a pre-test questionnaire, lecture-based teaching on three scenarios and then allocation into one of the three simulation groups- Group A (Tracheostomy group), Group B (Nasogastric tube group), and Group C (Epistaxis group) was done. Hands-on simulation training was given only to the assigned group. At the end of 15-days, post-test questionnaire and an objective assessment of the three scenarios in a simulated environment was conducted. The same training was repeated for each batch of participants who attended the posting. Results: The participants had significant improvement in the post-test scores in all three scenarios (p < 0.05), and these improvements were marked in those who had received simulated training. On comparing simulation scores, the participants who received hands-on training on a particular scenario outperformed other (p < 0.05). Conclusion: Simulation-based training improves cognition and overall confidence in managing ENT skills and emergencies. In simulation training, objective and standardized assessment is the key to achieve specific learning objectives to improve the psychomotor and cognitive skill. Level of evidence: II.
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Objetivo: verificar os comportamentos alimentares de indivíduos com doenças crônicas não transmissíveis. Método: Estudo descritivo, transversal, quantitativo com coleta de dados primários. Resultados: Sobre os comportamentos alimentares 48,6% (36) relataram realizar refeições em frente às telas, a maioria executa café da manhã, almoço e jantar e grande parte do grupo expôs consumir alimentos protetores e ultraprocessados. Conclusão: Os comportamentos alimentares encontrados entres os indivíduos com DCNT foram em geral desfavoráveis, mesmo com uma divisão adequada e inclusão de alguns bons alimentos, houve prevalência no consumo de biscoitos recheados, doces e bebidas adoçadas, além do péssimo hábito de se alimentar em frente a televisão.
Objective: to assess the dietary behaviors of individuals with chronic non-communicable diseases. Method: The study followed a descriptive, cross-sectional, quantitative approach with primary data collection. Results: The results revealed that 48.6% (36) reported having meals in front of screens, and the majority of the participants had breakfast, lunch, and dinner. A significant portion of the group reported consuming both protective foods and ultra-processed foods. Conclusion: In conclusion, the dietary behaviors observed among individuals with NCDs were generally unfavorable. Despite proper meal distribution and the inclusion of some healthy foods, there was a prevalence of consumption of filled cookies, sweets, and sugary beverages, along with the detrimental habit of eating in front of the television.
Objetivo: verificar los comportamientos alimentarios de individuos con enfermedades crónicas no transmisibles que asisten a una clínica integrada en el extremo sur de Santa Catarina. Método: Se llevó a cabo un estudio descriptivo, transversal y cuantitativo con recolección de datos primarios. Resultados: En cuanto a los comportamientos alimentarios, el 48,6% (36) informó realizar comidas frente a las pantallas, y la mayoría de los participantes desayunaban, almorzaban y cenaban. Además, una parte significativa del grupo declaró consumir alimentos protectores y ultraprocesados. Conclusión: Los comportamientos alimentarios encontrados entre los individuos con enfermedades crónicas no transmisibles fueron generalmente desfavorables. A pesar de una adecuada distribución de las comidas e inclusión de algunos alimentos saludables, hubo una prevalencia en el consumo de galletas rellenas, dulces y bebidas azucaradas, además del mal hábito de comer frente al televisor.
Subject(s)
Noncommunicable Diseases , Nutritional Sciences , Feeding BehaviorABSTRACT
Phytochemical screening of an ethanol-water extract (EWE) from the bark of Croton guatemalensis led to the isolation and identification of eight compounds, among them: five ent-clerodane diterpenoids [junceic acid (1), 6(s)-acetoxy-15,16-diepoxy-ent-cleroda-3,13(16),14-trien-20-oic acid (crotoguatenoic acid A) (2), 6(s)-hydroxyoxy-15,16-diepoxy-ent-cleroda-3,13(16),14-trien-20-oic acid (crotoguatenoic acid B) (3), formosin F (4), bartsiifolic acid (5)], and three flavonoids [rutin (6), epicatechin (7), and quercetin (8)]. Of these, 2 and 3 are reported here for the first time. Structures were established through conventional spectroscopy methods and their absolute configurations were determined by optical rotation and comparison of experimental electronic circular dichroism (ECD) and theoretical calculated ECD spectra. A suitable high performance liquid chromatography (HPLC) method for quantifying rutin (6) was developed and validated according to standard protocols. Affinity-directed fractionation was used to identify possible in vitro active compounds on α-glucosidases from Saccharomyces cerevisiae. HPLC-ESI-MS was used to identify the inhibitors as free ligands after being released from the enzymatic complex by denaturing acidic conditions. The affinity studies led to the identification of ent-clerodane diterpenoids as active compounds. In silico analysis allowed us to determine the best conformational rearrangement for the α-glucosidase inhibitors.
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Abstract Introduction The nasopharynx and oropharynx are the main colonization sites of coronavirus. Therefore, patients with paranasal sinuses and pharyngeal problems (ear, nose, and throat [ENT] patients) predispose coronavirus infection. Ear, nose, and throat patients with concomitant asymptomatic coronavirus infection may develop severe pneumonia following surgical procedures. As a result, presurgical screening for coronavirus infection is a substantial concern. Objective We evaluated the usefulness of a spiral chest computed tomography (CT) scan in the diagnosis of asymptomatic coronavirus infection in the presurgical assessment of ENT patients Methods In this study, candidates of paranasal sinus or pharyngeal surgery were evaluated for coronavirus infection. Patients with neither history of coronavirus disease 2019 (COVID-19) nor compatible symptoms and signs were screened for asymptomatic coronavirus infection. These patients composed two groups: the first group underwent a reverse transcription polymerase chain reaction (RT-PCR) test of nasopharyngeal sample and spiral chest CTscan, but for the second one, only the latter was performed. Results In the first group, which consisted of 106 patients, 11 (10.4%) cases had positive RT-PCR test results, and 17 (16%) patients showed positive findings in favor of coronavirus infection in the spiral chest CT scan. In the second group, which consisted of 173 patients, 34 (19.7%) cases had positive chest CT scan results. Conclusion The chest CT scan has a valuable role in the early diagnosis of asymptomatic coronavirus carriers in patients highly predisposed to infection, especially in low resource areas, where the RT-PCR test is unavailable.
ABSTRACT
The current study aimed to scale up the favorable bio-stimulants for enhancing the growth and breeding strategies of Stevia rebaudiana to increase sugar productivity. Inoculation of 45-day-old S. rebaudiana plantlets with Bacillus cereus and Azospirillum brasilense alone or in combination for 30 days allowed comparisons among their effects on enhancement and improvement of plant growth, production of bioactive compounds and expression of steviol glycoside genes. B. cereus SrAM1 isolated from surface-sterilized Stevia rebaudiana leaves was molecularly identified using 16s rRNA and tested for its ability to promote plant growth. Beneficial endophytic B. cereus SrAM1 induced all plant growth-promoting traits, except solubilization of phosphate, therefore it showed high effectiveness in the promotion of growth and production of bioactive compounds. Treatment of plants with B. cereus SrAM1 alone revealed carbohydrates content of 278.99 mg/g, total soluble sugar of 114.17 mg/g, total phenolics content of 34.05 mg gallic acid equivalent (GAE)/g dry weight) and total antioxidants activity of 32.33 mg (A.A)/g dry weight). Thus, plantlets inoculated with B. cereus SrAM1 alone exhibited the greatest responses in physiological and morphological parameters, but plantlets inoculated with B. cereus SrAM1 + A. brasilense showed a maximal upregulation of genes responsible for the biosynthesis of steviol glycosides (Kaurene oxidase, ent-KO; UDP-dependent glycosyl transferases of UGT85C2, UGT74G1, UGT76G1). Taken together, the used bacterial strains, particularly B. cereus SrAM1 could significantly improve the growth of S. rebaudiana via dynamic interactions in plants.
Subject(s)
Azospirillum brasilense , Diterpenes, Kaurane , Stevia , Antioxidants/metabolism , Azospirillum brasilense/genetics , Azospirillum brasilense/metabolism , Bacillus cereus/genetics , Diterpenes, Kaurane/metabolism , Gallic Acid/pharmacology , Gene Expression Regulation, Plant , Glucosides/metabolism , Glycosides/metabolism , Molecular Biology , Phosphates/metabolism , Plant Breeding , Plant Leaves/metabolism , RNA, Ribosomal, 16S , Stevia/metabolism , Sugars/metabolism , Transferases/genetics , Uridine Diphosphate/metabolismABSTRACT
Introduction The nasopharynx and oropharynx are the main colonization sites of coronavirus. Therefore, patients with paranasal sinuses and pharyngeal problems (ear, nose, and throat [ENT] patients) predispose coronavirus infection. Ear, nose, and throat patients with concomitant asymptomatic coronavirus infection may develop severe pneumonia following surgical procedures. As a result, presurgical screening for coronavirus infection is a substantial concern. Objective We evaluated the usefulness of a spiral chest computed tomography (CT) scan in the diagnosis of asymptomatic coronavirus infection in the presurgical assessment of ENT patients Methods In this study, candidates of paranasal sinus or pharyngeal surgery were evaluated for coronavirus infection. Patients with neither history of coronavirus disease 2019 (COVID-19) nor compatible symptoms and signs were screened for asymptomatic coronavirus infection. These patients composed two groups: the first group underwent a reverse transcription polymerase chain reaction (RT-PCR) test of nasopharyngeal sample and spiral chest CT scan, but for the second one, only the latter was performed. Results In the first group, which consisted of 106 patients, 11 (10.4%) cases had positive RT-PCR test results, and 17 (16%) patients showed positive findings in favor of coronavirus infection in the spiral chest CT scan. In the second group, which consisted of 173 patients, 34 (19.7%) cases had positive chest CT scan results. Conclusion The chest CT scan has a valuable role in the early diagnosis of asymptomatic coronavirus carriers in patients highly predisposed to infection, especially in low resource areas, where the RT-PCR test is unavailable.
ABSTRACT
This study presents the cytotoxic activity evaluation of the natural diterpenes ent-kaurenoic acid (1) and its 15ß-hydroxy (2), 15ß-senecioyloxy (3), and 15ß-tiglinoyloxy (4) derivatives, isolated from Brazilian native plants, Baccharis retusa and B. lateralis (Asteraceae). Using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) colorimetric assay, it was observed that compound 1 displayed in vitro activity towards the aggressive MDA-MB-231 adenocarcinoma cell line and reduced toxicity against MCF-10A nontumorigenic epithelial cells, indicating expressive selectivity. On the contrary, compounds 2-4 exhibited reduced toxicity and selectivity in both tested cell lines. Based on the chemical structures of compounds 1-4, it is suggested that the presence of additional functional groups at the C-15 position-a hydroxyl group in compound 2 and isomeric isoprene units in compounds 3 and 4-might be responsible for the reduction in the potential/selectivity. In silico studies show, for compounds 1-4, good predictions regarding bioavailability and ADME (absorption, distribution, metabolism, and excretion) properties as well as no alerts for PAINS (pan-assay structures interference). In conclusion, ent-kaurenoic acid (1), a common diterpenoid isolated in high amounts from different plants belonging to the Baccharis genus, has been shown to be a promising cytotoxic agent against an aggressive adenocarcinoma cell line (MDA-MB-23) and, if well exploited, could be used as a scaffold in the development of molecular prototypes for the treatment of breast cancer.
Subject(s)
Adenocarcinoma , Antineoplastic Agents , Baccharis , Diterpenes, Kaurane , Diterpenes , Antineoplastic Agents/chemistry , Baccharis/chemistry , Diterpenes/pharmacology , Diterpenes, Kaurane/chemistry , Humans , Structure-Activity RelationshipABSTRACT
The objective of the work was to study the cytotoxic effect of ent-kaurene acid derivatives obtained from Coespeletia moritziana (Sch. Bip. Ex Wedd.) Cuatrec., After analysis by GC/MS, IR and NMR. Isolating: kaurenic acid (I), grandifloric acid (II), 15-α-hydroxy kaurenic acid (III), 15 α-acetoxy-kaur 16-en-19-oic acid (IV), Kaurenol (V); and by hemisynthesis: 15,16-epoxy-17-acetoxy-kauran 19-oic acid (VI), 15-oxo-ent-kaur-16-en-19-oic acid (VIII), ester 2,3,4,6 -15-oxo-kaur-16-en-19-oic acid acetyl α-D-pyranosyl tetra-tetra (VII). Cytotoxicity was tested in human cancer cell lines: uterus (HeLa), lung (A-549), breast (MCF-7), African green monkey kidney non-tumor line (Vero) and human peripheral blood mononuclear cells (CMPS). Compound (I) was active against HeLa, A-549 and Vero. Compounds (II and VIII) showed moderate and good (IC50 ≤ 9 µM) cytotoxicity, respectively, against the five cell lines. Compound (V) showed moderate activity against A-549 and compound (VII), slight cytotoxicity against HeLa and A-549. Results that show the cytotoxic specificity of the isolated kaurenes and derivatives of Coespeletia moritzianaand their therapeutic potential.
El objetivo del trabajo fue estudiar el efecto citotóxico de derivados del ácido ent-kaureno obtenidos de Coespeletia moritziana (Sch. Bip. ex Wedd.) Cuatrec., previo análisis mediante GC/MS, IR y RMN. Aislandose: ácido kaurénico(I), ácido grandiflorénico (II), ácido 15-α-hidroxi kaurénico(III), ácido 15 α-acetoxi-kaur 16-en-19-oico (IV), Kaurenol (V); y por hemisíntesis: ácido 15,16-epoxi-17-acetoxi-kauran 19-oico (VI), ácido15-oxo-ent-kaur-16-en-19-oico (VIII), éster 2,3,4,6-tetra acetil α-D-piranosilo del ácido 15-oxo-kaur-16-en-19-oico (VII). La citotóxicidad fue ensayada en líneas celulares cancerosas humanas: útero (HeLa), pulmón(A-549), mama (MCF-7), línea no tumoral de riñón de mono verde africano (Vero) y células mononucleares humanas de sangre periférica (CMPS). El compuesto (I) resultó activo frente a HeLa, A-549 y Vero. Los compuestos (II y VIII), mostraron moderada y buena (IC50≤9µM) citotoxicidad respectivamente, frente a las cinco líneas celulares. El compuesto (V) presentó moderada actividad frente a A-549 y el (VII), leve citotoxicidad frente a HeLa y A-549. Resultados que evidencian la especificidad citotóxica de los kaurenos aislados y derivados de Coespeletia moritzianay su potencial terapéutico.
Subject(s)
Plant Extracts/pharmacology , Plant Extracts/chemistry , Asteraceae/chemistry , Cell Line, Tumor/drug effects , Diterpenes/isolation & purification , Spectrophotometry, Infrared , Magnetic Resonance Imaging , Chromatography, Thin Layer , Diterpenes, Kaurane , Diterpenes/pharmacology , Gas Chromatography-Mass SpectrometryABSTRACT
The objective of this work was to collect information on the curative use of plants in the municipality of Teziutlán, Puebla through semi-structured interviews. Thus, 78 plants used for medicinal purposes were identified, of which 40 are native to Mexico and 38 introduced; The value of use (UV) of each one and the Informant's Consensus Factor (FCI) of 10 categories of diseases were calculated. The five most frequently used plants are Ruta chalepensis L., Rosmarinus officinalis, Arnica montana, Loeselia mexicana (Lam.) Brandegee and Sambucus cerulea var., Neomexicana, which underwent a chemical and pharmacological review. On the other hand, the most frequent preparations are infusion and decoction, using mainly leaves (49.34%) and flowers (19.51%). It is concluded that the inhabitants of Teziutlán have a fairly homogeneous ethnomedical knowledge, setting the standard for research on its pharmacological properties.
El objetivo del presente trabajo fue recopilar información sobre el uso curativo de las plantas del municipio de Teziutlán, Puebla por medio de entrevistas semiestructuradas. Así, se identificaron 78 plantas utilizadas con fines medicinales, de las cuales 40 son propias de México y 38 introducidas; se calculó el valor de uso (UV) de cada una y el Factor de Consenso del Informante (FCI) de 10 categorías de padecimientos. Las cinco plantas utilizadas con mayor frecuencia son Ruta chalepensis L., Rosmarinus officinalis, Arnica montana, Loeselia mexicana (Lam.) Brandegee y Sambucus cerulea var., neomexicana, a las que se les hizo una revisión química y farmacológica. Por otro lado, las preparaciones más frecuentes son infusión y decocción, utilizando principalmente hojas (49.34 %) y flores (19.51 %). Se concluye que los habitantes de Teziutlán cuentan con un conocimiento etnomédico bastante homogéneo, dando la pauta para investigaciones sobre sus propiedades farmacológicas.
Subject(s)
Humans , Plants, Medicinal , Ethnobotany , Surveys and Questionnaires , MexicoABSTRACT
Abstract Introduction COVID-19 has been one of the worst pandemics faced by the human civilization, and otorhinolaryngological manifestations are commonly seen in this disease. Objective The present study was done to profile the ear, nose, and throat (ENT) manifestations in patients diagnosed with COVID-19. An attempt has also been made to assess whether there was any difference between the symptoms of different strains of COVID-19. A brief review of the current knowledge of the transmission of the disease and its treatment has also been done. Methods A cross-sectional, record-based study was conducted in a COVID hospital of India between May and July 2020. Descriptive statistics were used and appropriate parametric/nonparametric tests were applied to assess the association between various variables. Results Out of 250 patients, 80 cases were asymptomatic and 170 were symptomatic. Most of the symptomatic patients had sore throat and nasal congestion. Conclusion Knowledge of the ENT manifestations of COVID-19 is essential for its early identification and to devise appropriate prevention protocols for the benefit of health care workers (HCWs) and of the general population.