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1.
Food Sci Nutr ; 11(12): 7664-7672, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38107140

RESUMO

The current study aimed to explore the anti-diabetic effect of aqueous extracts of Gymnema sylvestre, Trigonella foenum-graecum and mixture of both the plants in alloxan-induced diabetic rabbits. A total of 30 rabbits were grouped into six equal groups as: normal control, diabetic control, diabetic treated with 300 mg/kg body weight (bw) G. sylvestre, diabetic treated with 300 mg/kg bw T. foenum-graecum, diabetic treated with 300 mg/kg bw mixture of both the plants and diabetic treated with 500 mg/kg bw metformin for 4 weeks. Diabetes was induced to all the study group animals except normal control by intravenous administration of alloxan monohydrate (80 mg/kg bw). Blood glucose was measured by glucometer and other biochemical parameters were determined through various kit methods. Serum insulin was measured through ELISA kit method. Results showed that both the plants and metformin significantly (p < .05) decreased the fasting blood glucose. Hypoglycemic activity of aqueous extract of G. sylvestre and metformin was found slightly higher than aqueous extract of T. foenum-graecum and the mixture of both the plants. However, a significant (p < .05) rise in insulin secretion was observed in studied plants extract treated rabbits. Serum urea, creatinine, and liver enzymes were found reduced significantly (p < .05) in treated rabbits whereas packed cell volume was also returned to normal in treated animals as compared to control group. The study concluded that G. sylvestre and T. foenum-graecum extracts have comparable effects with metformin in normalizing the blood glucose level and have more pronounced effect than metformin in restoring the serum biochemical parameters to normal levels. Hence, these plants may be the good alternative medicine in managing the diabetes mellitus.

2.
Microbiol Resour Announc ; 12(9): e0047323, 2023 Sep 19.
Artigo em Inglês | MEDLINE | ID: mdl-37606380

RESUMO

Bacillus subtilis has emerged as a species with potential for versatile nonribosomal peptides and polyketides of therapeutic importance, including antibiotics. From our molecular bioprospecting project, we report a full genome of Bacillus subtilis strain MARUCo01 locally isolated from sediments of the Indian Ocean along the coast of Bagamoyo in Tanzania.

3.
Data Brief ; 48: 109119, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-37383809

RESUMO

Priestia is a genus of biotechnologically important bacteria adapted to thrive in a wide range of environmental conditions including the marine sediments. Here, we screened and isolated a strain from the Bagamoyo marine mangrove-inhabited sediments and then employed whole genome sequencing to recover and define its full genome. De novo-assembly with Unicycler (v. 0.4.8) and annotation with Prokaryotic Genome Annotation Pipeline (PGAP) revealed that that its genome contains one chromosome (5,549,131 bp), with a GC content of 37.62%. Further analysis showed that the genome contains 5,687 coding sequences (CDS), 4 rRNAs, 84 tRNAs, 12 ncRNAs, and at least 2 plasmids (1,142 bp and 6,490 bp). On the other hand, antiSMASH-based secondary metabolite analysis revealed that the novel strain (MARUCO02) contains gene clusters for biosynthesis of MEP-DOXP-dependent versatile isoprenoids (eg. carotenoids), siderophores (synechobactin and schizokinen) and polyhydroxyalkanoates (PHA). The genome dataset also informs about the presence genes encoding enzymes required for generation of hopanoids, compounds that confer adaption to harsh environmental conditions including industrial cultivation recipes. Our data from this novel Priestia megaterium strain MARUCO02 can be used for reference and in genome-guided selection of strains for production of isoprenoids as well as industrially useful siderophores and polymers, amenable for biosynthetic manipulations in a biotechnological process.

4.
Food Sci Nutr ; 11(6): 2500-2529, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-37324906

RESUMO

Phytobioactive compounds are plant secondary metabolites and bioactive compounds abundantly present in medicinal plants and have remarkable therapeutic potential. Oxidative stress and antibiotic resistance are major causes of present-day ailments such as diabetes, atherosclerosis, cardiovascular disorders, cancer, and inflammation. The data for this review were collected from Google Scholar, PubMed, Directory of Open Access Journals (DOAJ), and Science Direct by using keywords: "Medicinal plants, Phytobioactive compounds, Polyphenols, Alkaloids, Carotenoids etc." Several studies have reported the pharmacological and therapeutic potential of the phytobioactives. Polyphenols, alkaloids, terpenes, and polysaccharides isolated from medicinal plants showed remarkable antioxidant, anticancer, cytotoxic, anti-inflammatory, cardioprotective, hepatoprotective, immunomodulatory, neuroprotective, and antidiabetic activities. This literature review was planned to provide comprehensive insight into the biopharmacological and therapeutic potential of phytobioactive compounds. The techniques used for the extraction and isolation of phytobioactive compounds, and bioassays required for their biological activities such as antioxidant, antimicrobial, anti-inflammatory, and cytotoxic activities, have been discussed. Characterization techniques for the structural elucidation of phytobioactive compounds such as HPLC, TLC, FTIR, GC-MS/MS, and NMR have also been discussed. This review concludes that phytobioactive compounds may be used as potential alternative to synthetic compounds as therapeutic agents for the treatment of various diseases.

5.
Front Mol Biosci ; 9: 1039286, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36567944

RESUMO

Amidst rising cases of antimicrobial resistance, antimicrobial peptides (AMPs) are regarded as a promising alternative to traditional antibiotics. Even so, poor pharmacokinetic profiles of certain AMPs impede their utility necessitating, a careful assessment of potential AMPs' absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties during novel lead exploration. Accordingly, the present study utilized ADMET scores to profile seven previously isolated African catfish antimicrobial peptides (ACAPs). After profiling, the peptides were docked against approved bacterial protein targets to gain insight into their possible mode of action. Promising ACAPs were then chemically synthesized, and their antibacterial activity was validated in vitro utilizing the broth dilution method. All seven examined antimicrobial peptides passed the ADMET screening, with two (ACAP-IV and ACAP-V) exhibiting the best ADMET profile scores. The ACAP-V had a higher average binding energy (-8.47 kcal/mol) and average global energy (-70.78 kcal/mol) compared to ACAP-IV (-7.60 kcal/mol and -57.53 kcal/mol), with the potential to penetrate and disrupt bacterial cell membrane (PDB Id: 2w6d). Conversely, ACAP-IV peptide had higher antibacterial activity against E. coli and S. aureus (Minimum Inhibitory Concentration, 520.7 ± 104.3 µg/ml and 1666.7 ± 416.7 µg/ml, respectively) compared to ACAP-V. Collectively, the two antimicrobial peptides (ACAP-IV and ACAP-V) are potential novel leads for the food, cosmetic and pharmaceutical industries. Future research is recommended to optimize the expression of such peptides in biological systems for extended evaluation.

6.
Anticancer Agents Med Chem ; 22(11): 2063-2079, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34702156

RESUMO

World Health Organization categorized breast cancer as one of the leading cancer types in females worldwide, and its treatment remains challenging. Accumulated evidence suggested the role of estrogen and its metabolites in pre- and post-menopausal women. Upregulation of estrogen-dependent aromatase is significantly involved in the pathogenesis of breast cancer. Several aromatase inhibitors, such as exemestane, formestane, and letrozole, are being used clinically, owing to their estrogen suppression role. Apart from these drugs, several other molecules, such as natural and synthetic flavonoids, have been reported widely for a similar biological activity. However, some reasonable modifications are required for these structures to achieve desired efficacy and to alleviate toxicity. Designing a novel aromatase inhibitor will be possible if we can establish a rational correlation between the chemistry and biological features of the existing molecules. The benzopyranone- ring system, present in the flavonoid molecules, has been reported as a pharmacophore due to its inhibitory activity on aromatase, which helps repress breast cancer progression. This essential feature has been utilized to modify several natural flavonoids into 5 and 7 hydroxy/methoxy flavone, 4-imidazolyl/triazolyl flavone, 5,4'- diamino flavone, 7,8- benzo-4-imidazolyl flavone, α-naphthoflavone, and 2-azole/thiazolyl isoflavone derivatives. These scaffolds have been considered in this review for meticulous study in aspects of the structure-activity relationship for aromatase inhibitory activity, and it would likely pave the way for designing a potential lead candidate in the future.


Assuntos
Neoplasias da Mama , Flavonas , Aromatase/metabolismo , Inibidores da Aromatase/química , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/metabolismo , Estrogênios , Feminino , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Humanos , Relação Estrutura-Atividade
7.
Front Pharmacol ; 12: 757090, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34776975

RESUMO

Several studies have been conducted and published on medicinal plants used to manage Diabetes Mellitus worldwide. It is of great interest to review available studies from a country or a region to resort to similarities/discrepancies and data quality. Here, we examined data related to ethnopharmacology and bioactivity of antidiabetic plants used in the Democratic Republic of Congo. Data were extracted from Google Scholar, Medline/PubMed, Scopus, ScienceDirect, the Wiley Online Library, Web of Science, and other documents focusing on ethnopharmacology, pharmacology, and phytochemistry antidiabetic plants used in the Democratic Republic of Congo from 2005 to September 2021. The Kew Botanic Royal Garden and Plants of the World Online web databases were consulted to verify the taxonomic information. CAMARADES checklist was used to assess the quality of animal studies and Jadad scores for clinical trials. In total, 213 plant species belonging to 72 botanical families were reported. Only one plant, Droogmansia munamensis, is typically native to the DRC flora; 117 species are growing in the DRC and neighboring countries; 31 species are either introduced from other regions, and 64 are not specified. Alongside the treatment of Diabetes, about 78.13% of plants have multiple therapeutic uses, depending on the study sites. Experimental studies explored the antidiabetic activity of 133 plants, mainly in mice, rats, guinea pigs, and rabbits. Several chemical classes of antidiabetic compounds isolated from 67 plant species have been documented. Rare phase II clinical trials have been conducted. Critical issues included poor quality methodological protocols, author name incorrectly written (16.16%) or absent (14.25%) or confused with a synonym (4.69%), family name revised (17.26%) or missing (1.10%), voucher number not available 336(92.05%), ecological information not reported (49.59%). Most plant species have been identified and authenticated (89.32%). Hundreds of plants are used to treat Diabetes by traditional healers in DRC. However, most plants are not exclusively native to the local flora and have multiple therapeutic uses. The analysis showed the scarcity or absence of high-quality, in-depth pharmacological studies. There is a need to conduct further studies of locally specific species to fill the gap before their introduction into the national pharmacopeia.

8.
Malawi Med J ; 33(2): 85-107, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-34777704

RESUMO

The Coronavirus Disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has triggered an international pandemic that has led to significant public health problems. To date, limited evidence exists to suggest that drugs are effective against the disease. As possible treatments are being investigated, herbal medicines have shown potential for producing novel antiviral agents for the COVID-19 disease. Aim: This review explored the potential of Malawi's traditional medicinal plants for the management of COVID-19. Methods: The authors searched on PubMed and Google scholar for medicinal plants that are used in Malawi and published in openly available peer reviewed journals. Plants linked with antiviral treatment, anti-COVID-19 activity or COVID-19 symptoms management were targeted. These included activity against pneumonia, inflammation, cough, difficulty in breathing, pain/aches, fever, diarrhoea, rheumatism, fatigue, asthma, immunocompromised and cardiovascular diseases. Results: 11 studies were found with 306 plant species. 127 plant species had at least one COVID-19 related pharmacological activity. Of these plant species, the number of herbal entities used for each indication was: pain/aches (87), fever (2), pneumonia (9), breathing/asthma problems (5), coughing (11), diarrhoea (1), immunosuppression (8), blood issues (10), fatigue (2), heart problems (11), inflammation (8), rheumatism (10) and viral diseases (12). Thirty (30) species were used for more than one disease and Azedarachta indica topped the list (6 of the 13 COVID-19 related diseases). The majority of the species had phytochemicals known to have antiviral activity or mechanisms of actions linked to COVID-19 and consequent diseases' treatment pathways. Conclusion: Medicinal plants are a promising source of compounds that can be used for drug development of COVID-19 related diseases. This review highlights potential targets for the World Health Organization and other research entities to explore in order to assist in controlling the pandemic.


Assuntos
COVID-19 , Plantas Medicinais , Antivirais/uso terapêutico , Humanos , Malaui , Compostos Fitoquímicos , SARS-CoV-2
9.
Curr Top Med Chem ; 21(12): 1067-1095, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33966619

RESUMO

BACKGROUND: Type 2 diabetes (adult onset diabetes) is the most common type of diabetes, accounting for around 90% of all diabetes cases with insulin resistance and insulin secretion defect. The key goal of anti-diabetic therapy is to increase the development of insulin, immunity and/or decrease the amount of blood glucose. While many synthetic compounds have been produced as antidiabetic agents, due to their side effects and limited effectiveness, their usefulness has been hindered. METHODS: This systematic review investigated the bioactive compounds reported to possess activities against type 2 diabetes. Three (3) databases, PubMed, ScienceDirect and Google Scholar were searched for research articles published between January 2010 and October 2020. A total of 6464 articles were identified out of which 84 articles were identified to be elligible for the study. RESULT AND DISCUSSION: From the data extracted, it was found that quercetin, Kaempferol, Rosmarinic acid, Cyanidin, Rutin, Catechin, Luteolin and Ellagic acid were the most cited bioactive compounds which all falls within the class of polyphenolic compounds. The major sources of these bioactive compounds includes citrus fruits, grapes, onions, berries, cherries, broccoli, honey, apples, green tea, Ginkgo biloba, St. John's wort, green beans, cucumber, spinach, tea, Rosmarinus officinalis, Aloe vera, Moringa oleifera, tomatoes, potatoes, oregano, lemon balm, thyme, peppermint, Ocimum basilicum, red cabbage, pears, olive oil and walnut.


Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
10.
J Ethnopharmacol ; 271: 113913, 2021 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-33571616

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The growing challenge to access conventional analgesics, contraindications, and adverse effects could have led individuals to use Schkuhria pinnata (Lam.) Kuntze ex Thell. (Compositae), as an alternative traditional therapeutic strategy for pain. However, evidence of its safety and efficacy is scarce. AIM OF THE STUDY: This study evaluated the anti-nociceptive effect of the ethanol extract of the aerial parts of S. pinnata in mice. METHODS: The mice were randomly assigned to nine groups: (1) vehicle; (2) acetylsalicylic acid (intraperitoneally 150 mg/kg); (3) pentazocine (intramuscularly 1.0 mg/kg); (4 a & b) orally 100 mg/kg extract; (5 a & b) orally 200 mg/kg extract; (6 a & b) orally 400 mg/kg extract. We used an acetic acid-induced writhing model and a tail-flick test. The number of writhes and time taken for the tail to flick was recorded. A one-way analysis of variance followed by Tamhane T2 post hoc was used for multiple comparisons. RESULTS: Compared to a vehicle (59.0 ± 2.68), S. pinnata ethanol extract at a dose of 200 and 400 mg/kg, p.o reduced writhes to 42.5 ± 1.12 and 27.0 ± 2.62, (p < 0.05) respectively. Similarly, the pain threshold of mice increased dose-dependently; doses of 200 and 400 mg/kg, increased time to 5.33 ± 0.42 and 8.67 ± 0.21 min, (p < 0.05) respectively. The extract had an EC50 of 348.8 mg/kg and acute toxicity established an LD50 of 1224.8 (95% CI: 952.2-1575.3). CONCLUSION: S. pinnata ethanol extract had anti-nociceptive activity by central and peripheral mechanisms that could justify its traditional use in pain management. Further studies could now focus on identifying active fractions and pure isolated compounds responsible for anti-nociceptive activity.


Assuntos
Analgésicos/farmacologia , Asteraceae/química , Componentes Aéreos da Planta/química , Extratos Vegetais/farmacologia , Ácido Acético/toxicidade , Administração Oral , Analgésicos/administração & dosagem , Analgésicos/toxicidade , Animais , Comportamento Animal/efeitos dos fármacos , Modelos Animais de Doenças , Etanol/química , Flavonoides/análise , Camundongos , Dor/induzido quimicamente , Dor/tratamento farmacológico , Limiar da Dor/efeitos dos fármacos , Fenóis/análise , Extratos Vegetais/administração & dosagem , Extratos Vegetais/toxicidade
11.
Front Pharmacol ; 12: 682794, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-35002686

RESUMO

Background: Viruses cause various human diseases, some of which become pandemic outbreaks. This study synthesized evidence on antiviral medicinal plants in Africa which could potentially be further studied for viral infections including Coronavirus disease 2019 (COVID-19) treatment. Methods: PUBMED, CINAHIL, Scopus, Google Scholar, and Google databases were searched through keywords; antiviral, plant, herb, and Africa were combined using "AND" and "OR". In-vitro studies, in-vivo studies, or clinical trials on botanical medicine used for the treatment of viruses in Africa were included. Results: Thirty-six studies were included in the evidence synthesis. Three hundred and twenty-eight plants were screened for antiviral activities of which 127 showed noteworthy activities against 25 viral species. These, were Poliovirus (42 plants), HSV (34 plants), Coxsackievirus (16 plants), Rhinovirus (14plants), Influenza (12 plants), Astrovirus (11 plants), SARS-CoV-2 (10 plants), HIV (10 plants), Echovirus (8 plants), Parvovirus (6 plants), Semiliki forest virus (5 plants), Measles virus (5 plants), Hepatitis virus (3 plants), Canine distemper virus (3 plants), Zika virus (2 plants), Vesicular stomatitis virus T2 (2 plants). Feline herpesvirus (FHV-1), Enterovirus, Dengue virus, Ebola virus, Chikungunya virus, Yellow fever virus, Respiratory syncytial virus, Rift Valley fever virus, Human cytomegalovirus each showed sensitivities to one plant. Conclusion: The current study provided a list of African medicinal plants which demonstrated antiviral activities and could potentially be candidates for COVID-19 treatment. However, all studies were preliminary and in vitro screening. Further in vivo studies are required for plant-based management of viral diseases.

12.
Front Microbiol ; 12: 794631, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34987491

RESUMO

Antimicrobial peptides (AMPs) constitute a broad range of bioactive compounds in diverse organisms, including fish. They are effector molecules for the innate immune response, against pathogens, tissue damage and infections. Still, AMPs from African Catfish, Clarias gariepinus, skin mucus are largely unexplored despite their possible therapeutic role in combating antimicrobial resistance. In this study, African Catfish Antimicrobial peptides (ACAPs) were identified from the skin mucus of African Catfish, C. gariepinus. Native peptides were extracted from fish mucus scrapings in 10% acetic acid (v/v) and ultra-filtered using 5 kDa molecular weight cut-off membrane. The extract was purified using C18 Solid-Phase Extraction. The antibacterial activity was determined using the Agar Well Diffusion method and broth-dilution method utilizing Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922). Thereafter, Sephadex G-25 gel filtration was further utilized in bio-guided isolation of the most active fractions prior to peptide identification using Orbitrap Fusion Lumos Tribrid Mass Spectrometry. The skin mucus extracted from African Catfish from all the three major lakes of Uganda exhibited antimicrobial activity on E. coli and S. aureus. Lake Albert's C. gariepinus demonstrated the best activity with the lowest MIC of 2.84 and 0.71 µg/ml on S. aureus and E. coli, respectively. Sephadex G-25 peak I mass spectrometry analysis (Data are available via ProteomeXchange with identifier PXD029193) alongside in silico analysis revealed seven short peptides (11-16 amino acid residues) of high antimicrobial scores (0.561-0.905 units). In addition, these peptides had a low molecular weight (1005.57-1622.05 Da) and had percentage hydrophobicity above 54%. Up to four of these AMPs demonstrated α-helix structure conformation, rendering them amphipathic. The findings of this study indicate that novel AMPs can be sourced from the skin mucus of C. gariepinus. Such AMPs are potential alternatives to the traditional antibiotics and can be of great application to food and pharmaceutical industries; however, further studies are still needed to establish their drug-likeness and safety profiles.

13.
Sci Afr ; 12: e00824, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37215382

RESUMO

Mycobacterium tuberculosis remains one of the world's contributors to mortality. With the emergence of SARS-CoV-2 coinfections, patients with TB are predisposed to being more heavily weighed down by COVID-19 disease and its opportunistic coinfections. The severity of the disease coupled with drug resistance on the currently used drugs warrants for the search for alternative remedies from synthetic agents, semisynthetics and natural products that include plants. Africa is rich in plant diversity with a promise as sources of drug agents, one of which is Eichhornia crassipes. This work aimed at isolating a fatty acid and dock it to ß-ketoacyl-ACP synthase for possible anti-TB drug development prospects using computational tools. (9z,12z)-Octadeca-9,12-dienoic acid was isolated from Eichhornia crassipes for the first time using chromatographic techniques and identified using 1D and 2D NMR spectroscopic methods (1H NMR, COSY, HSQC, HMBC and 13C NMR). The compound was then docked to ß-ketoacyl-ACP synthase (KasA), an essential member of the b-ketoacyl synthases encoded in the M. tuberculosis genome in comparison with its co-crystallized ligand JSF-3285, also for the first time. (9z,12z)-Octadeca-9,12-dienoic acid interacted with only phenylalanine239 and proline201 while JSF-3285 interacted with proline201, glutamine120, alanine119, leucine116, glutamine199, histadine345, phenylalanine239, glycine240 and glycine200. (9z,12z)-Octadeca-9,12-dienoic acid had a ligand efficiency of 0.24, compared to the co-crystallized ligand's 0.36. The compound was too flexible and elongated with -4.72 KCalmol-1 binding energy. Despite some unfavourable physico-chemical properties, the compound still provides reliable interactions that only require logical structural modifications by the addition of polar regions amongst others to increase interactions and ligand efficiency, which can consequently stand to be a better potential drug lead. For the first time, plant-based (9z,12z)-Octadeca-9,12-dienoic acid isolated from Eichhornia crassipes was shown to interact fairly well with ß-ketoacyl-ACP synthase and proved to be a potential starting material from which anti-tubercular drugs can be designed.

14.
Front Bioeng Biotechnol ; 8: 604041, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33344436

RESUMO

Antimicrobial resistance remains a great threat to global health. In response to the World Health Organizations' global call for action, nature has been explored for novel and safe antimicrobial candidates. To date, fish have gained recognition as potential source of safe, broad spectrum and effective antimicrobial therapeutics. The use of computational methods to design antimicrobial candidates of industrial application has however, been lagging behind. To fill the gap and contribute to the current fish-derived antimicrobial peptide repertoire, this study used Support Vector Machines algorithm to fish out fish-antimicrobial peptide-motif candidates encrypted in 127 peptides submitted at the Antimicrobial Peptide Database (APD3), steered by their physico-chemical characteristics (i.e., positive net charge, hydrophobicity, stability, molecular weight and sequence length). The best two novel antimicrobial peptide-motifs (A15_B, A15_E) with the lowest instability index (-28.25, -22.49, respectively) and highest isoelectric point (pI) index (10.48 for each) were selected for further analysis. Their 3D structures were predicted using I-TASSER and PEP-FOLD servers while ProSA, PROCHECK, and ANOLEA were used to validate them. The models predicted by I-TASSER were found to be better than those predicted by PEP-FOLD upon validation. Two I-TASSER models with the lowest c-score of -0.10 and -0.30 for A15_B and A15_E peptide-motifs, respectively, were selected for docking against known bacterial-antimicrobial target-proteins retrieved from protein databank (PDB). Carbapenam-3-carboxylate synthase (PDB ID; 4oj8) yielded the lowest docking energy (-8.80 and -7.80 Kcal/mol) against motif A15_B and A15_E, respectively, using AutoDock VINA. Further, in addition to Carbapenam-3-carboxylate synthase, these peptides (A15_B and A15_E) were found to as well bind to membrane protein (PDB ID: 1by3) and Carbapenem synthetase (PDB: 1q15) when ClusPro and HPEPDOCK tools were used. The membrane protein yielded docking energy scores (DES): -290.094, -270.751; coefficient weight (CW): -763.6, 763.3 for A15_B and A15_E) whereas, Carbapenem synthetase (PDB: 1q15) had a DES of -236.802, -262.75 and a CW of -819.7, -829.7 for peptides A15_B and A15_E, respectively. Motif A15_B of amino acid positions 2-19 in Pleurocidin exhibited the strongest in silico antimicrobial potentials. This segment could be a good biological candidate of great application in pharmaceutical industries as an antimicrobial drug candidate.

15.
SAGE Open Med ; 8: 2050312120959178, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32999721

RESUMO

OBJECTIVES: The main aim of this study was to estimate relative proportions of medication use according to different pregnancy risk categories (A, B, C, D, X) among pregnant women attending antenatal care (ANC) visits at Shashemene Referral Hospital. METHODS: A hospital-based retrospective cross-sectional study was conducted at Shashemene referral hospital from February 2016 to February 2017. Structured data collection form was used to capture data from patient medication cards. SPSS version 16.0 was used to analyze the results after entering and importing from MS-Excel. RESULTS: A total of 317 pregnant women cards were collected and assessed during the study period in May, 2017. Most, 208(65.6%), of the pregnant women were in their second trimester of pregnancy followed by third trimester, 78(24.6%). Tetanus prevention in pregnancy, 274(86.4%), was the most common reason for drug use. Number of medications prescribed was highest, 384(68.2%), in second trimester followed by third trimester, 130(23.1%). More than half, 305(54.2%), of the drugs prescribed were under category C, tetanus toxoid (TT) vaccine alone accounting for 274 (89.8%) of them, followed by 36.8% from category A. CONCLUSION: Vaccines, vitamins and minerals were the most frequently prescribed medications. The overall drug use condition during pregnancy in this study was inappropriate as more than half of the prescribed medications were from category C. On the other hand, category X medications were not prescribed.

16.
Artigo em Inglês | MEDLINE | ID: mdl-32508941

RESUMO

Eichhornia crassipes has been reported to have various medicinal properties including anticancer activities. The plant was collected from the Shire river in Malawi, and two cytotoxic compounds, benzene-1,4-diol and nonanedioic acid, were isolated and characterized for the first time in the leaves and roots of the plant. 1H NMR, COSY, HSQC, HMBC, 13-C, and LCMS spectroscopic experimental techniques were used to identify the compounds in their pure forms. In silico experiments showed that both compounds do not have AMES toxicity and do not inhibit cytochrome P450 enzymes, but nonanedioic acid acts as a CYP2D6 substrate. This work showed that Eichhornia crassipes can be considered to have a role as a source of potential hits and leads to drug development that can be rationally optimized for drugs.

17.
Syst Rev ; 9(1): 7, 2020 01 08.
Artigo em Inglês | MEDLINE | ID: mdl-31915054

RESUMO

BACKGROUND: Studies on several preclinical models of type 2 diabetes mellitus have been conducted to establish the hypoglycemic activity of Momordica charantia L. Concerned with appropriateness of these models, we designed a systematic review to establish the efficacy and safety of M. charantia L. in preclinical models of type 2 diabetes mellitus. METHODS: Review authors will search without language restriction in MEDLINE/PubMed, Web of Science, Embase, Scopus, and CINAHL databases through April 2019. Search filters will be applied to enhance search efficiency. The authors will search for gray literature in Google and Google Scholar, OpenGrey, and ProQuest Dissertations & Theses. Two authors will evaluate full texts, extract data, and asses risk of bias independently. The review will include randomized or non-randomized studies that assessed the efficacy or safety of M. charantia L. with vehicle control group. The primary endpoint will be fasting blood glucose level. We will use Egger's test to assess publication biases. Chi-square test and I2 will be used to assess heterogeneity in effect size of the primary outcome. Using RevMan software version 5.3, the authors will perform a meta-analysis of quantitative data. DISCUSSION: The strength of evidence will be rated as high, moderate, low, or very low using GRADE framework for animal studies. This systematic review will potentially improve research practice by identifying risks of bias and design features that compromise translatability and contribute to evidence-based clinical trial design. SYSTEMATIC REVIEW REGISTRATION: PROSPERO CRD42019119181.


Assuntos
Diabetes Mellitus Tipo 2 , Hipoglicemiantes , Modelos Animais , Momordica charantia , Segurança do Paciente , Fitoterapia , Animais , Humanos , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Preparações de Plantas/uso terapêutico , Metanálise como Assunto , Revisões Sistemáticas como Assunto
18.
Front Pharmacol ; 11: 608672, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33597879

RESUMO

Echinops kebericho Mesfin is traditionally used for the treatment of various infectious diseases. This study investigated antibacterial activity of the essential oil (EO) and the different fractions of ethanol extract. The most active component was isolated and identified. Isolation and purification was accomplished using chromatographic techniques while identification was done by spectroscopic method. Minimum inhibitory concentration (MIC) was determined using the broth micro-dilution method. In bioactive-guided isolation, percent inhibition was determined using optical density (OD) measurement. The MICs of the essential oil ranged from 78.125 µg/ml to 625 µg/ml, and its activity was observed against methicillin-resistant Staphylococcus aureus (MRSA, NCTC 12493). Ethyl acetate fraction showed high activity against MRSA (NCTC 12493), MIC = 39.075 µg/ml followed by Enterococcus faecalis (ATCC 49532), MIC = 78.125 µg/ml and was least active against Klebsiella pneumoniae (ATCC 700603), MIC = 1,250 µg/ml. MIC of hexane fraction ranged from 156.2 µg/ml to Escherichia coli (ATCC 49532) to 1,250 µg/ml to E. coli (NCTC 11954). The MICs of chloroform fraction ranged from 312.5 to 2500 µg/ml; while butanol fraction could be considered pharmacologically inactive as its MIC value was 2,500 µg/ml for all and no activity against E. coli (NCTC 11954). Dehydrocostus lactone was successfully isolated and identified whose MIC was 19.53 µg/ml against MRSA. Dehydrocostus lactone isolated from E. kebericho M. showed noteworthy antibacterial activity which lends support to ethnopharmacological use of the plant. Further optimization should be done to improve its antibacterial activities and pharmacokinetic profile.

19.
Complement Ther Med ; 47: 102224, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31780027

RESUMO

OBJECTIVE: This study summarized evidence on the efficacy and safety of essential oils (EOs) in the treatment of topical infections. DESIGN AND SETTING: Systematic review of clinical trials conducted and reported in accordance with the Preferred Reporting Items for Systematic Reviews and Meta-analysis (PRISMA) guideline. Electronic databases of the Cochrane, PubMed, EMBASE, Web of Science, and Scopus were searched from inception to November 2018. INTERVENTION: Essential oil of any type, standard treatment and placebo. MAIN OUTCOME MEASURES: Outcomes of the study include total acne count, acne severity index, reduction in total acne surface area, number of non-inflammatory acne lesions and inflammatory acne lesions, microbial cure rate, microbial decolonization rate, and new microbial emergence. RESULTS: Non-significant but higher proportion of MRSA was cleared in EOs group (69% [95%CI: 34%, 96%]) compared to routine care (45% [95%CI: 36%, 53%]). Essential oils significantly lowered level of new MRSA emergence (9% [95% CI: 5%, 14%], I2 = 86.59%) compared to routine care (53% [95%CI: 30%, 75%], I2 = 86.59%). Four of the five studies on acne treatment showed equal or superior efficacy of EOs and the remaining one showed inferior efficacy to a control. In treatment of topical fungal infections, efficacy of essential oils were non-inferior compared to a standard treatment but superior to a placebo. CONCLUSION: Essential oils could be considered as alternative treatment for acne, decolonization of MRSA, and topical fungal infections, yet the low quality and heterogeneity among the studies calls for further studies.


Assuntos
Acne Vulgar/tratamento farmacológico , Anti-Infecciosos Locais/uso terapêutico , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Óleos Voláteis/uso terapêutico , Humanos , Ensaios Clínicos Controlados Aleatórios como Assunto
20.
J Ethnopharmacol ; 231: 311-324, 2019 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-30385422

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Momordica charantia Linnaeus (Cucurbitaceae) has been extensively used traditionally as food and herbal medicine for type 2 diabetes mellitus in Asia, Brazil, and east Africa. In vitro and in vivo studies suggest its glycemic control potential; however, clinical studies produced conflicting results. AIM OF THE STUDY: To evaluate the efficacy of M. charantia preparations in lowering elevated plasma glucose level in prediabetes and type 2 diabetes mellitus patients. METHODS: Electronic search of the Cochrane library, PubMed®, CINAHL, and SCOPUS databases was done from 1st January 1960-30th April 2018 without language restriction. Two independent reviewers extracted data and assessed risk of bias of articles. Revman var. 5.3 software was used for data synthesis in meta-analysis. Heterogeneity was assessed using Chi-square and I2 tests. Treatment effect was estimated using mean difference at follow up in outcome measures between M. charantia preparations and placebo or oral hypoglycemic agents control group. The protocol of this study has a registration number PROSPERO CRD42018083653. RESULTS: Ten studies of type 2 diabetes mellitus (n = 1045) were included in the meta-analysis. They had 4-16 weeks follow up and overall moderate to high risk of bias. Compared to placebo, M. charantia monoherbal formulation significantly reduces FPG, PPG and HBA1c with mean difference of - 0.72 mmol/L, (95% CI: -1.33, -0.12), I2 = 14%, - 1.43 mmol/L, (95% CI: -2.18, -0.67), I2 = 0, - 0.26%, (95% CI: -0.49, -0.03), I2 = 0 respectively. M. charantia also lowered FPG in prediabetes (mean difference -0.31 mmol/L, n = 52); the evidence was downgraded to low quality because the study had unclear risk of bias and inadequate sample size. No serious adverse effects were reported. CONCLUSION: M. charantia adjunct preparations improved glycemic control in T2DM patients. However, this conclusion is based on low to very low quality evidences for the primary outcomes and sparse data for several safety outcomes, thus, warrant further research. Particularly needed are the researches that focus on standardizing M. charantia formulation and determine its efficacy and safety in clinical trials with adequate sample size, designed with random sequence generation, allocation concealment of intervention and blinding of both research personnel and participants.


Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Momordica charantia , Preparações de Plantas/uso terapêutico , Humanos , Fitoterapia , Ensaios Clínicos Controlados Aleatórios como Assunto
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