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1.
Nutrients ; 15(15)2023 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-37571339

RESUMO

This research investigated the antihypertensive effects of tamarind products and compared their potentials based on an animal model's data verified by molecular docking, multitarget interactions, and dynamic simulation assays. GC-MS-characterized tamarind products were administered to cholesterol-induced hypertensive albino rat models. The two-week-intervened animals were dissected to collect their serum and organs and respectively subjected to analyses of their hypertension-linked markers and tissue architectures. The lead biometabolites of tamarinds interacted with eight target receptors in the molecular docking and dynamic simulation studies and with multitarget in the network pharmacological analyses. The results show that the serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), C-reactive protein (CRP), troponin I, and lipid profiles were maximally reinstated by the phenolic-enriched ripened sour tamarind extract compared to the sweet one, but the seed extracts had a smaller influence. Among the tamarind's biometabolites, ϒ-sitosterol was found to be the best ligand to interact with the guanylate cyclase receptor, displaying the best drug-likeliness with the highest binding energy, -9.3 Kcal. A multitargeted interaction-based degree algorithm and a phylogenetic tree of pathways showed that the NR3C1, REN, PPARG, and CYP11B1 hub genes were consistently modulated by ϒ-sitosterol to reduce hypertension and related risk factors. The dynamic simulation study showed that the P-RMSD values of ϒ-sitosterol-guanylate cyclase were stable between 75.00 and 100.00 ns at the binding pocket. The findings demonstrate that ripened sour tamarind extract may be a prospective antihypertensive nutraceutical or supplement target affirmed through advanced preclinical and clinical studies.


Assuntos
Hipertensão , Tamarindus , Ratos , Animais , Antioxidantes/farmacologia , Tamarindus/química , Sitosteroides , Anti-Hipertensivos/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Simulação de Dinâmica Molecular , Simulação de Acoplamento Molecular , Ligantes , Filogenia , Hipertensão/tratamento farmacológico , Guanilato Ciclase
3.
J Ethnopharmacol ; 308: 116189, 2023 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-36791925

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Diarrhea is one of the leading causes of preventable death in developing countries, mainly caused by bacterial infections and traditional therapies are very common in diarrheal incidences. Meda Pata (Litsea glutionsa) has a long history of use as traditional medicine for diarrhea, dysentery, and spasm in Bangladesh, India, and some other Asian countries. AIM OF THE STUDY: This research reports the antidiarrheal effects of Meda Pata (Litsea glutinosa leaf extract, LGLEx) in animal models. The work has been supported by in silico molecular docking study to verify the effects. MATERIALS AND METHODS: The antidiarrheal effect of LGLEx was investigated in castor oil-induced diarrhea, magnesium sulfate-induced diarrhea, and gastrointestinal motility test models. Antidiarrheal effects were supported by a molecular docking study through an interaction between LGLEx's GC-MS analyzed imidazole-containing compounds and muscarinic acetylcholine receptor (PDB: 4U14) and 5-HT3 receptor (PDB: 5AIN). RESULTS: LGLEx potentially reduced the diarrheal incidences in in vivo assays reducing gastrointestinal motility. The maximum diarrheal inhibition was obtained in the castor oil-induced model (62.63%) and and BaSO4-induced model (73.14%), which were statistically significant (P < 0.05) when compared to the reference drug loperamide. In the castor-oil and BaSO4-induced models, peristaltic movement was reduced by 25.96% and 32.17%, respectively. Biochemical markers particularly IgE, C-reactive proteins, and serum electrolytes were significantly (P < 0.0) restored in treated groups. A Molecular docking analysis revealed that two compounds (1-Ethyl-2-hydroxymethylimidazole and 1,6-Anhydro-beta-D-glucofuranose demonstrated the highest binding affinity with target receptors muscarinic acetylcholine receptor (PDB: 4U14) and 5-HT3 receptor (PDB: 5AIN) confirming their drug likeliness. The findings indicate a high potential antidiarrheal impact that warrants further investigation for its therapeutic application.


Assuntos
Antidiarreicos , Litsea , Animais , Ratos , Antidiarreicos/farmacologia , Óleo de Rícino , Simulação de Acoplamento Molecular , Receptores 5-HT3 de Serotonina , Extratos Vegetais/farmacologia , Diarreia/tratamento farmacológico
4.
Cardiovasc Toxicol ; 23(1): 32-45, 2023 01.
Artigo em Inglês | MEDLINE | ID: mdl-36626070

RESUMO

Lasia spinosa (L.) Thwaites is a medicinal plant of enormous traditional use with insufficient scientific evidence. This research screened the antioxidative effect of L. spinosa extracts by measuring the total phenolic content, total flavonoid content, DPPH free radical scavenging activity, ABTS scavenging activity, Iron-chelating activity, and Ferric reducing power followed by an evaluation of in vivo cardioprotective effect in doxorubicin-induced Wistar Albino rats. Phytochemical characterization was made by Gas Chromatography-Mass Spectroscopic analysis. L. spinosa showed an excellent antioxidative effect while methanol leaf extract (LSM) was found to be more potent than ethyl acetate leaf extract (LSE) in scavenging the free radicals. Intraperitoneal injection of doxorubicin caused a significant (P < 0.001) increase in lactate dehydrogenase (LDH), creatine kinase (CK-MB), C-reactive protein (CRP), and Cardiac troponin I. Pretreatment with orally administrated (LSM100 and LSM200 mg/kg b.w.) daily for 10 days showed a decrease in the cardiac markers, lipid profiles, especially triglycerides (TG), total cholesterol (TC), low-density lipoprotein (LDL), and an increase of high-density lipoprotein (HDL) compared to the disease control group. LSM200 was found to significantly (P < 0.05) decrease the levels of CK-MB and LDH. It also restored TC, TG, and LDL levels compared to the doxorubicin-induced cardiac control group. The protective role of LSM was further confirmed by histopathological examination. This study thus demonstrates that L. spinosa methanol extract could be approached as an alternative supplement for cardiotoxicity, especially in the chemical-induced toxicity of cardiac tissues.


Assuntos
Cardiotoxicidade , Extratos Vegetais , Animais , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Doxorrubicina/toxicidade , Metanol , Modelos Animais , Extratos Vegetais/farmacologia , Ratos
5.
Biomed Pharmacother ; 143: 112215, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34649346

RESUMO

Orchids are basically ornamental, and biological functions are seldom evaluated. This research investigated the effects of Acampe ochracea methanol extract (AOME) in ameliorating the paracetamol (PCM) induced liver injury in Wistar albino rats, evaluating its phytochemical status through UPLC-qTOF-MS analysis. With molecular docking and network pharmacology, virtual screening verified the inevitable interactions between the UPLC-qTOF-MS-characterized compounds and hepatoprotective drug receptors. The AOME has explicit a dose-dependent decrease of liver enzymes acid phosphatase (ACP), aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), gamma-glutamyl transferase (GGT), lactate dehydrogenase (LDH), total bilirubin, as well as an increase of serum total protein and antioxidant enzymes catalase (CAT), superoxide dismutase (SOD), glutathione reductase (GSH) with a virtual normalization (p < 0.05-p < 0.001) and the values were almost equivalent to the reference drug silymarin. After pretreatment with AOME, PCM-induced malondialdehyde (MDA) levels were considerably decreased (p < 0.001). Histopathological examinations corroborated the functional and biochemical findings. The AOME upregulated the genes involved in antioxidative (CAT, SOD, ß-actin, PON1, and PFK1) and hepatoprotective mechanisms in PCM intoxicated rats. An array of 103 compounds has been identified from AOME through UPLC-qTOF-MS analysis. The detected compounds were substantially related to the targets of several liver proteins and antioxidative enzymes, according to an in silico study. Virtual prediction by SwissADME and admetSAR showed that AOME has drug-like, non-toxic, and potential pharmacological activities in hepatic damage. Furthermore, VEGFA, CYP19A1, MAPK14, ESR1, and PPARG genes interact with target compounds impacting the significant biological actions to recover PCM-induced liver damage.


Assuntos
Antioxidantes/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Fígado/efeitos dos fármacos , Orchidaceae , Estresse Oxidativo/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Acetaminofen , Animais , Antioxidantes/isolamento & purificação , Antioxidantes/farmacocinética , Aromatase/genética , Aromatase/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/genética , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Modelos Animais de Doenças , Receptor alfa de Estrogênio/genética , Receptor alfa de Estrogênio/metabolismo , Regulação da Expressão Gênica , Fígado/metabolismo , Fígado/patologia , Masculino , Proteína Quinase 14 Ativada por Mitógeno/genética , Proteína Quinase 14 Ativada por Mitógeno/metabolismo , Simulação de Acoplamento Molecular , Farmacologia em Rede , Orchidaceae/química , Estresse Oxidativo/genética , PPAR gama/genética , PPAR gama/metabolismo , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacocinética , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacocinética , Mapas de Interação de Proteínas , Ratos Wistar , Transdução de Sinais , Fator A de Crescimento do Endotélio Vascular/genética , Fator A de Crescimento do Endotélio Vascular/metabolismo
6.
Oxid Med Cell Longev ; 2021: 9711176, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34367469

RESUMO

The purpose of this study was to look into the effects of green coconut mesocarp juice extract (CMJE) on diabetes-related problems in streptozotocin- (STZ-) induced type 2 diabetes, as well as the antioxidative functions of its natural compounds in regulating the associated genes and biochemical markers. CMJE's antioxidative properties were evaluated by the standard antioxidant assays of 1,1-diphenyl-2-picrylhydrazyl (DPPH), superoxide radical, nitric oxide, and ferrous ions along with the total phenolic and flavonoids content. The α-amylase inhibitory effect was measured by an established method. The antidiabetic effect of CMJE was assayed by fructose-fed STZ-induced diabetic models in albino rats. The obtained results were verified by bioinformatics-based network pharmacological tools: STITCH, STRING, GSEA, and Cytoscape plugin cytoHubba bioinformatics tools. The results showed that GC-MS-characterized compounds from CMJE displayed a very promising antioxidative potential. In an animal model study, CMJE significantly (P < 0.05) decreased blood glucose, serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), creatinine, uric acid, and lipid levels and increased glucose tolerance as well as glucose homeostasis (HOMA-IR and HOMA-b scores). The animal's body weights and relative organ weights were found to be partially restored. Tissue architectures of the pancreas and the kidney were remarkably improved by low doses of CMJE. Compound-protein interactions showed that thymine, catechol, and 5-hydroxymethylfurfural of CMJE interacted with 84 target proteins. Of the top 15 proteins found by Cytoscape 3.6.1, 8, CAT and OGG1 (downregulated) and CASP3, COMT, CYP1B1, DPYD, NQO1, and PTGS1 (upregulated), were dysregulated in diabetes-related kidney disease. The data demonstrate the highly prospective use of CMJE in the regulation of tubulointerstitial tissues of patients with diabetic nephropathy.


Assuntos
Antioxidantes/farmacologia , Cocos/química , Diabetes Mellitus Experimental/complicações , Nefropatias Diabéticas/prevenção & controle , Regulação da Expressão Gênica/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Glicemia/análise , Nefropatias Diabéticas/etiologia , Nefropatias Diabéticas/patologia , Masculino , Estresse Oxidativo , Ratos , Ratos Wistar , alfa-Amilases/antagonistas & inibidores
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