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1.
Nat Prod Res ; : 1-9, 2024 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-38300810

RESUMO

Three new dihydrochalcones: artoserichalcone A-C (1-3), were isolated from the leaves of Artocarpus sericicarpus. The structures of compounds were determined based on NMR spectrum (1H, 13C, and 2D) and HRESIMS spectroscopic analysis. Compounds (1) and (3) showed active antimalarial activity with IC50 values of 16.90 and 13.56 µM, respectively. Meanwhile, compound (2) with an IC50 value of 63.01 µM was categorised as a moderate antimalarial substance. The cytotoxicity against Huh7, HepG2, BHK-21, and Vero cells showed that compounds (1-3) with CC50 values > 20 µg/mL could be considered non-cytotoxic. Compounds (1-3) exhibited antimalarial activity against Plasmodium falciparum and non-toxic as an antimalarial agent.

2.
Sci Rep ; 14(1): 3823, 2024 02 15.
Artigo em Inglês | MEDLINE | ID: mdl-38360784

RESUMO

Zebrafish have been utilized for many years as a model animal for pharmacological studies on diabetes and obesity. High-fat diet (HFD), streptozotocin and alloxan injection, and glucose immersion have all been used to induce diabetes and obesity in zebrafish. Currently, studies commonly used both male and female zebrafish, which may influence the outcomes since male and female zebrafish are biologically different. This study was designed to investigate the difference between the metabolites of male and female diabetic zebrafish, using limonene - a natural product which has shown several promising results in vitro and in vivo in treating diabetes and obesity-and provide new insights into how endogenous metabolites change following limonene treatment. Using HFD-fed male and female zebrafish, we were able to develop an animal model of T2D and identify several endogenous metabolites that might be used as diagnostic biomarkers for diabetes. The endogenous metabolites in males and females were different, even though both genders had high blood glucose levels and a high BMI. Treatment with limonene prevented high blood glucose levels and improved in diabesity zebrafish by limonene, through reversal of the metabolic changes caused by HFD in both genders. In addition, limonene was able to reverse the elevated expression of AKT during HFD.


Assuntos
Diabetes Mellitus , Hiperglicemia , Animais , Feminino , Masculino , Hipoglicemiantes/farmacologia , Limoneno , Peixe-Zebra/metabolismo , Glicemia/metabolismo , Espectroscopia de Prótons por Ressonância Magnética , Obesidade/metabolismo , Dieta Hiperlipídica , Hiperglicemia/complicações
3.
Data Brief ; 52: 109895, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38161655

RESUMO

This article presents two types of phytochemical data obtained from Brucea javanica (L.) Merr. roots, a medicinal plant belonging to the Simaroubaceae family. The high-resolution LC-MS dataset comprised the chemical profile of dichloromethane extract, which was utilised to annotate 35 chemical constituents. For annotations, the measured spectral data were compared with the in-silico spectral data generated from 920 molecular structures previously reported in Simaroubaceae. Indole alkaloids, quassinoids, aliphatics and lignan were the chemical groups identified in the root extract. The second dataset provides NMR spectra (1H, 13C, COSY, HMQC and HMBC) for the six indole alkaloids previously detected in LC-MS analysis and isolated through centrifugal partition chromatography. The chemical structures of all compounds were confirmed based on NMR data as bruceolline J (compound 7), canthin-6-one-N-oxide (compound 10), bruceolline E (compound 15), 5-methoxycanthin-6-one (compound 16), canthin-6-one (compound 20), and 1­hydroxy-11-methoxycanthin-6-one (compound 22). This phytochemical data was generated to support an ongoing anti-cancer and anti-dengue study.

4.
Nat Prod Res ; 38(1): 10-15, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-35862620

RESUMO

Phytochemical investigation of methanolic extract of L. rubiginosa using modern chromatographic techniques has led to the isolation of three new triterpenoid saponins, lepiginosides A-C (1-3), a new farnesyl glycoside, lepiginoside D (4), together with lepisantheside B (5) and gleditsoside C (6). The characterization and structural elucidation of the isolated compounds were established by extensive spectroscopic data analysis and comparison with literature data. Moreover, the antibacterial activity against seven bacteria, but none is active.


Assuntos
Glicosídeos Cardíacos , Sapindaceae , Saponinas , Triterpenos , Glicosídeos/farmacologia , Saponinas/química , Sapindaceae/química , Triterpenos/química , Estrutura Molecular
5.
Pharmaceuticals (Basel) ; 16(5)2023 May 07.
Artigo em Inglês | MEDLINE | ID: mdl-37242494

RESUMO

BACKGROUND: In recent years, the potential role of probiotics has become prominent in the discoveries of neurotherapy against neurodegenerative diseases, such as Alzheimer's and Parkinson's diseases. Lactic acid bacteria (LAB) exhibit neuroprotective properties and exert their effects via various mechanisms of actions. This review aimed to evaluate the effects of LAB on neuroprotection reported in the literature. METHODS: A database search on Google Scholar, PubMed, and Science Direct revealed a total of 467 references, of which 25 were included in this review based on inclusion criteria which comprises 7 in vitro, 16 in vivo, and 2 clinical studies. RESULTS: From the studies, LAB treatment alone or in probiotics formulations demonstrated significant neuroprotective activities. In animals and humans, LAB probiotics supplementation has improved memory and cognitive performance mainly via antioxidant and anti-inflammatory pathways. CONCLUSIONS: Despite promising findings, due to limited studies available in the literature, further studies still need to be explored regarding synergistic effects, efficacy, and optimum dosage of LAB oral bacteriotherapy as treatment or prevention against neurodegenerative diseases.

6.
J Complement Integr Med ; 20(2): 365-371, 2023 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-36750417

RESUMO

OBJECTIVES: The objective of this study is to determine the activity of Garcinia cowa Roxb. n-hexane, ethyl acetate, and butanol fractions as an immunomodulator in vitro and obtain the fraction that has the potential as an immunomodulator. METHODS: Raw 264.7 macrophages were used to asses G. cowa Roxb. immunomodulatory activity. The MTT assay was chosen to measure cell viability to evaluate the cytotoxic effect on cells. ELISA method was used to measure the concentration of Interleukin-6 (IL-6) and Tumor Necrosis Factor Alpha (TNF-α) secreted by cells after being treated with G. cowa Roxb. fraction. The neutral red uptake assay determined the effect of Garcinia cowa Roxb. on the phagocytic activity. RESULTS: After Raw 264.7 macrophages were given the Hexan fraction (Hex) at concentrations of 12.5 and 25 µg/mL, there was a decrease in the concentration of IL-6, TNF-α, and the phagocytosis index of cells. Administration of the Ethyl Acetate fraction (EtOAc) at concentrations of 12.5 and 25 µg/mL on cells caused a decrease in IL-6 and TNF-α levels but did not affect the phagocytosis index. There was an increase in the level of TNF-α and the phagocytosis index after being given the Butanol fraction (BuOH) with concentrations of 12.5 and 25 µg/mL but there was a slight decrease in the level of IL-6. CONCLUSIONS: Both Hex and EtOAc fractions could suppress immune responses through decreasing IL-6, TNF-α, and slightly decreased phagocytic activity. BuOH fraction could stimulate immunomodulatory activities through enhanced TNF-α levels and phagocytic index, but less potent in enhancing IL-6 production. The BuOH fraction could be developed as an immunostimulant.


Assuntos
Garcinia , Extratos Vegetais , Extratos Vegetais/farmacologia , Extratos Vegetais/análise , Interleucina-6 , Fator de Necrose Tumoral alfa , Fatores Imunológicos/farmacologia
7.
Artigo em Inglês | MEDLINE | ID: mdl-36336330

RESUMO

Depression is a common mental disorder that can adversely affect psychosocial function and quality of life. However, the exact aetiology and pathogenesis of depression are still unclear. Stress plays a major role in the pathogenesis of depression. The use of currently prescribed antidepressants has many side effects. Centella asiatica (C. asiatica) has shown promising antidepressant activity in rodent models. Here, we developed a reserpine-induced zebrafish stress-like model and performed behavioural analysis, cortisol measurement and 1H-Nuclear Magnetic Resonance (1H NMR) spectroscopy-based metabolomics analysis to test the anti-stress activity of ethanolic extract of C. asiatica (RECA). A significant increase in total distance travelled (F(8,8) = 8.905, p = 0.0054) and a reduction in freezing duration (F(9, 9) = 10.38, p = 0.0018) were found in the open field test (OFT). Asiaticoside, one of tested C.asiatica's triterpenoid gives a significant increase in contact duration (F(5,5) = 142.3, (p = 0.0330) at 2.5 mg/kg). Eight biomarkers were found, i.e. ß-hydroxyisovaleric acid, leucine, threonine, scylloinositol, lactate, betaine, valine, choline and l-fucose, to be responsible for the class separation between stress and RECA-treated groups. Metabolic pathway alteration in zebrafish brain upon treatment with RECA was identified as valine, leucine and isoleucine biosynthesis, while alanine, aspartate, glutamate and glycerophospholipid metabolism was involved after fluoxetine treatment.


Assuntos
Centella , Triterpenos , Animais , Peixe-Zebra , Reserpina/toxicidade , Centella/química , Leucina , Qualidade de Vida , Espectroscopia de Ressonância Magnética , Aminoácidos de Cadeia Ramificada , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Valina
8.
J Tradit Complement Med ; 12(6): 556-566, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36325238

RESUMO

Background and aim: The present study investigates Plectranthus scutellarioides (L.) R.Br. as potential antibacterial oral rinse against bacteria associated with peri-implantitis to prevent the initial infection as well as disease progression. Experimental procedure: Phytochemical screening was done on P. scutellarioides lyophilized extract to identify the presence of chemical constituent by using mass-based identification. The extract was screened for its antibacterial activity against 4 Gram-positive aerobes (early colonizer) and 5 Gram-negative facultative anaerobes as well as obligate anaerobes (late colonizer) using disc diffusion method. The extract was tested for minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), its cytotoxicity effects on human gingival fibroblast cell (HnGF) as well as bacteria morphological changes by scanning electron microscopy (SEM). Results and conclusion: Four flavonoid compounds were identified namely quercetin-3-glucoside, quercitrin, quercetin 3-(6″-acetylglucoside) and quercetin 3-O-acetyl-rhamnoside. The sensitivity test revealed that P. scutellarioides extract was effective against all the bacteria tested. MIC concentrations for the Gram-positive aerobes were in the range of 1.56-12.50 mg/mL, and the MBC concentrations were within 3.13-12.50 mg/mL. For Gram-negative obligate anaerobes, the MIC concentration were within 3.13-12.50 mg/mL and MBC within 6.25-200.00 mg/mL. The ethanolic extract did not have any cytotoxic effect on HnGF cells at the tested concentrations. SEM images showed bacterial cell wall disruption for all the bacteria tested. The results showed that P. scutellarioides extract exerts its antibacterial property by disrupting the cell wall of all the bacteria tested. Hence, P. scutellarioides may benefit from further investigations on its safety for oral use as an adjunctive treatment for peri-implantitis.

9.
Phytochem Anal ; 33(8): 1235-1245, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36192845

RESUMO

INTRODUCTION: Ficus deltoidea Jack (Moraceae) is a plant used in Malaysia to treat various ailments, including diabetes. The presence of several varieties raises essential questions regarding which is the potential bioactive variety and what are the bioactive metabolites. OBJECTIVES: Here, we explored the phytochemical diversity of the seven varieties from Peninsular Malaysia using Nuclear Magnetic Resonance (NMR) and Liquid Chromatography-Mass Spectrometry (LC-MS) analyses and correlated it with the α-glucosidase inhibitory activity. METHODOLOGY: The Nuclear Overhauser Effect Spectroscopy (NOESY) One-Dimensional (1D)-NMR and LC-MS data were processed, annotated, and correlated with in vitro α-glucosidase inhibitory using multivariate data analysis. RESULTS: The α-glucosidase results demonstrated that different varieties have varying inhibitory effects, with the highest inhibition rate being F. deltoidea var. trengganuensis and var. kunstleri. Furthermore, diverse habitats and plant ages could also influence the inhibitory rate. The heat map from NMR and LC-MS profiles showed unique patterns according to varying levels of α-glucosidase inhibition rate. The Partial Least Squares (PLS) model constructed from both NMR and LC-MS further confirmed the correlation between the α-glucosidase inhibition rate of F. deltoidea varieties and its metabolite profiles. The Variable Influence on Projection (VIP) and correlation coefficient (p(corr)) values values were used to determine the highly relevant metabolites for explaining the anticipated inhibitory action. CONCLUSION: NMR and LC-MS annotations allow the identification of flavan-3-ols and proanthocyanidins as the key bioactive factors. Our current results demonstrated the value of multivariate data analysis to predict the quality of herbal materials from both biological and chemical aspects.


Assuntos
Ficus , Ficus/química , alfa-Glucosidases , Cromatografia Líquida , Extratos Vegetais/química , Espectrometria de Massas em Tandem , Metabolômica , Espectroscopia de Ressonância Magnética , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/química
10.
J Pharm Biomed Anal ; 210: 114579, 2022 Feb 20.
Artigo em Inglês | MEDLINE | ID: mdl-35016031

RESUMO

Ficus deltoidea var angustifolia (FD-A) reduces blood pressure in spontaneously hypertensive rats (SHR) but the mechanism remains unknown. Changes in urine metabolites following FD-A treatment in SHR were, therefore, examined to identify the mechanism of its antihypertensive action. Male SHR were given either FD-A (1000 mg kg-1 day-1) or losartan (10 mg kg-1 day-1) or 0.5 mL of ethanolic-water (control) daily for 4 weeks. Systolic blood pressure (SBP) was measured every week and urine spectra data acquisition, on urine collected after four weeks of treatment, were compared using multivariate data analysis. SBP in FD-A and losartan treated rats was significantly lower than that in the controls after four weeks of treatment. Urine spectra analysis revealed 24 potential biomarkers with variable importance projections (VIP) above 0.5. These included creatine, hippurate, benzoate, trimethylamine N-oxide, taurine, dimethylamine, homocysteine, allantoin, methylamine, n-phenylacetylglycine, guanidinoacetate, creatinine, lactate, glucarate, kynurenine, ethanolamine, betaine, 3-hydroxybutyrate, glycine, lysine, glutamine, 2-hydroxyphenylacetate, 3-indoxylsulfate and sarcosine. From the profile of these metabolites, it seems that FD-A affects urinary levels of metabolites like taurine, hypotaurine, glycine, serine, threonine, alanine, aspartate and glutamine. Alterations in these and the pathways involved in their metabolism might underlie the molecular mechanism of its antihypertensive action.


Assuntos
Ficus , Hipertensão , Animais , Anti-Hipertensivos/farmacologia , Pressão Sanguínea , Hipertensão/tratamento farmacológico , Masculino , Extratos Vegetais/farmacologia , Ratos , Ratos Endogâmicos SHR
11.
Front Plant Sci ; 12: 791205, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-35003181

RESUMO

Glutathione (GSH; γ-glutamyl-cysteinyl-glycine), a low-molecular-weight thiol, is the most pivotal metabolite involved in the antioxidative defense system of plants. The modulation of GSH on the plant in response to environmental stresses could be illustrated through key pathways such as reactive oxygen species (ROS) scavenging and signaling, methylglyoxal (MG) detoxification and signaling, upregulation of gene expression for antioxidant enzymes, and metal chelation and xenobiotic detoxification. However, under extreme stresses, the biosynthesis of GSH may get inhibited, causing an excess accumulation of ROS that induces oxidative damage on plants. Hence, this gives rise to the idea of exploring the use of exogenous GSH in mitigating various abiotic stresses. Extensive studies conducted borne positive results in plant growth with the integration of exogenous GSH. The same is being observed in terms of crop yield index and correlated intrinsic properties. Though, the improvement in plant growth and yield contributed by exogenous GSH is limited and subjected to the glutathione pool [GSH/GSSG; the ratio of reduced glutathione (GSH) to oxidized glutathione (GSSG)] homeostasis. Therefore, recent studies focused on the sequenced application of GSH was performed in order to complement the existing limitation. Along with various innovative approaches in combinatory use with different bioactive compounds (proline, citric acid, ascorbic acid, melatonin), biostimulants (putrescine, Moringa leaf extract, selenium, humic acid), and microorganisms (cyanobacteria) have resulted in significant improvements when compared to the individual application of GSH. In this review, we reinforced our understanding of biosynthesis, metabolism and consolidated different roles of exogenous GSH in response to environmental stresses. Strategy was also taken by focusing on the recent progress of research in this niche area by covering on its individualized and combinatory applications of GSH prominently in response to the abiotic stresses. In short, the review provides a holistic overview of GSH and may shed light on future studies and its uses.

12.
Mol Divers ; 25(2): 995-1009, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-32301032

RESUMO

The ß-glucuronidase, a lysosomal enzyme, catalyzes the cleavage of glucuronosyl-O-bonds. Its inhibitors play a significant role in different medicinal therapies as they cause a decrease in carcinogen-induced colonic tumors by reducing the level of toxic substances present in the intestine. Among those inhibitors, bisindole derivatives had displayed promising ß-glucuronidase inhibition activity. In the current study, hydrazone derivatives of bisindolymethane (1-30) were synthesized and evaluated for in vitro ß-glucuronidase inhibitory activity. Twenty-eight analogs demonstrated better activity (IC50 = 0.50-46.5 µM) than standard D-saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 µM). Compounds with hydroxyl group like 6 (0.60 ± 0.01 µM), 20 (1.50 ± 0.10 µM) and 25 (0.50 ± 0.01 µM) exhibited the most potent inhibitory activity, followed by analogs with fluorine 21 (3.50 ± 0.10 µM) and chlorine 23 (8.20 ± 0.20 µM) substituents. The presence of hydroxyl group at the aromatic side chain was observed as the main contributing factor in the inhibitory potential. From the docking studies, it was predicted that the active compounds can fit properly in the binding groove of the ß-glucuronidase and displayed significant binding interactions with essential residues.


Assuntos
Glicoproteínas , Hidrazonas , Indóis , Glucuronidase/antagonistas & inibidores , Glucuronidase/química , Glicoproteínas/síntese química , Glicoproteínas/química , Hidrazonas/síntese química , Hidrazonas/química , Indóis/síntese química , Indóis/química , Simulação de Acoplamento Molecular
13.
Food Res Int ; 137: 109547, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-33233172

RESUMO

Fruit of salak (Salacca zalacca) is traditionally used and commercialized as an antidiabetic agent. However, the scientific evidence to prove this traditional use is lacking. This research was aimed to evaluate the metabolic changes of obese-diabetic (OBDC) rats treated with S. zalacca fruit extract using proton-nuclear magnetic resonance (1H NMR)-based metabolomics approach. This research presents the first report on the in vitro antidiabetic effect of S. zalacca fruits extract using this approach. The obtained results indicated that the administration of 400 mg/kg bw of 60% ethanolic S. zalacca extract for 6 weeks significantly decreased the blood glucose level and normalized the blood lipid profile of the OBDC rats. The potential biomarkers in urine were 2-oxoglutarate, alanine, leucine, succinate 3-hydroxybutyrate, taurine, betaine, allantoin, acetate, dimethylamine, creatine, creatinine, glucose, phenyl-acetylglycine, and hippurate. Based on the data obtained, the 60% ethanolic extract could not fully improved the metabolic complications of diabetic rats. The extract of S. zalacca fruit was able to decrease the ketones bodies as 3-hydroxybutyrate and acetoacetate. It also improved energy metabolism, involving glucose, acetate, lactate, 2-hydroxybutyrate, 2-oxoglutarate, citrate, and succinate. Moreover, it decreased metabolites from gut microflora, including choline. This extract had significant effect on amino acid metabolism, metabolites from gut microflora, bile acid metabolism and creatine. The result can further support the traditional claims of S. zalacca fruits in management of diabetes. This finding might be valuable in understanding the molecular mechanism and pharmacological properties of this medicinal plant for managing diabetes mellitus.


Assuntos
Diabetes Mellitus Experimental , Frutas , Metabolômica , Animais , Diabetes Mellitus Experimental/tratamento farmacológico , Espectroscopia de Ressonância Magnética , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Espectroscopia de Prótons por Ressonância Magnética , Ratos , Ratos Sprague-Dawley
14.
J Food Biochem ; 44(12): e13535, 2020 12.
Artigo em Inglês | MEDLINE | ID: mdl-33103260

RESUMO

Coffee is rich in antioxidant and has been shown to confer various health benefits. Here, we investigated the effect of single-dose coffee consumption in healthy human subjects. About 30 healthy volunteers were recruited and given a serving of sugar free black coffee. Urine and fecal samples were collected and analyzed. Significant changes in urinary metabolites relating to coffee, gut microbial and host energy metabolisms were observed post-coffee consumption. Clear sex differences were also observed in the urinary metabolic profiles pre- and post-coffee consumption. Sex differences in richness and composition of gut microbiota were observed, however, the effect of single-dose coffee consumption on host gut microbiota were unremarkable. These findings indicated that single-dose coffee consumption affects sex-specific host metabolic responses that relates to gut-microbe and energy metabolism. This study demonstrated the utility of systems biology tools to unravel complexity of host-diet biology and gut microbial responses. PRACTICAL APPLICATIONS: This study demonstrated that integrated systems biology approach enabled efficient extractions of host biochemical and microbial information that allows food industry to ascertain the impact of diet and longitudinal assessment of potential functional food in humans.


Assuntos
Microbioma Gastrointestinal , Adulto , Café , Dieta , Fezes , Feminino , Humanos , Masculino , Caracteres Sexuais
15.
J Integr Neurosci ; 19(2): 217-227, 2020 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-32706186

RESUMO

Centella asiatica is notable for its wide range of biological activities beneficial to human health, particularly its cognitive enhancement and neuroprotective effects. The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors are ionotropic glutamate receptors mediating fast excitatory neurotransmission essential in long-term potentiation widely thought to be the cellular mechanism of learning and memory. The method of whole-cell patch-clamp was used to study the effect of the acute application of Centella asiatica extract on the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor-mediated spontaneous excitatory postsynaptic currents in the entorhinal cortex of rat brain slices. The respective low dose of test compounds significantly increased the amplitude of spontaneous excitatory postsynaptic currents while having no significant effects on the frequency. The findings suggested that Centella asiatica extract increased the response of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors at the postsynaptic level, revealing the potential role of Centella asiatica in modulating the glutamatergic responses in the entorhinal cortex of rat brain slices to produce cognitive enhancement effects.


Assuntos
Córtex Entorrinal/efeitos dos fármacos , Potenciais Pós-Sinápticos Excitadores/efeitos dos fármacos , Nootrópicos/farmacologia , Receptores de AMPA/efeitos dos fármacos , Triterpenos/farmacologia , Animais , Centella , Nootrópicos/administração & dosagem , Técnicas de Patch-Clamp , Extratos Vegetais , Ratos , Triterpenos/administração & dosagem
16.
Bioorg Chem ; 99: 103819, 2020 06.
Artigo em Inglês | MEDLINE | ID: mdl-32325334

RESUMO

Leishmaniasis has affected a wider part of population around the globe. Most often, the existing regiments to battle against leishmaniasis are inadequate and limited. In our ongoing efforts to develop new leishmanicidal agents, we have synthesized a series of novel and symmetrical bis-Schiff base-disulfide hybrids 1-27. Intermediate disulfide was synthesized from corresponding 2-aminothiol followed by reacting the coupled adduct with various aromatic aldehydes. All these compounds showed outstanding inhibition when compared with standard (Table 1). Out of twenty seven analogues, twenty two analogues i.e. 1-5, 7-13, 17-21, 23-27 analogues showed excellent inhibitory potential with EC50 values ranging from 0.010 ± 0.00 to 0.096 ± 0.01 µM while five compounds i.e. 6, 14-16, and 22 showed good inhibitory potential with EC50 values ranging from 0.10 ± 0.00 to 0.137 ± 0.01 µM when compared with the standard Amphotericin B. Structure-activity relationship has been established while molecular docking studies were performed to pin the binding interaction of active molecules. This study will help to develop new antileishmanial lead compounds.


Assuntos
Antiprotozoários/farmacologia , Dissulfetos/farmacologia , Leishmania/efeitos dos fármacos , Antiprotozoários/síntese química , Antiprotozoários/química , Dissulfetos/química , Relação Dose-Resposta a Droga , Simulação de Acoplamento Molecular , Estrutura Molecular , Testes de Sensibilidade Parasitária , Bases de Schiff/química , Bases de Schiff/farmacologia , Relação Estrutura-Atividade
17.
Appl Biochem Biotechnol ; 192(1): 1-21, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32215848

RESUMO

Patients are turning into herbs for the management of diabetes, which cause increasing in the demand of plant-based alternative medicines. Ficus deltoidea or locally known as "Mas Cotek" in Malaysia is a famous herbal plant. However, many varieties of F. deltoidea existed with varied antidiabetic activities inspire us to evaluate in vivo antidiabetic activity of the most available varieties of F. deltoidea. Therefore, antihyperglycemic effect of different varieties of F. deltoidea at dose 250 mg/kg was evaluated on streptozotocin-nicotinamide-induced diabetic rats and further assessed their urinary metabolites using proton nuclear magnetic resonance (1H-NMR). The hyperglycemic blood level improved towards normoglycemic state after 30 days of treatment with standardized extracts of F. deltoidea var. trengganuensis, var. kunstleri, and var. intermedia. The extracts also significantly managed the biochemical parameters in diabetic rats. Metabolomics results showed these varieties were able to manage the altered metabolites of diabetic rats by shifting some of the metabolites back to their normal state. This knowledge might be very important in suggesting the use of these herbs in long-term treatment for diabetes. The most potential variety can be recommended, which may be useful for further pharmacological studies and herbal authentication processes.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/urina , Ficus/química , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Animais , Glicemia/análise , Cromatografia Líquida de Alta Pressão , Etanol , Espectroscopia de Ressonância Magnética , Masculino , Metaboloma , Niacinamida , Extratos Vegetais/química , Folhas de Planta/química , Ratos , Ratos Sprague-Dawley , Estreptozocina
18.
Artigo em Inglês | MEDLINE | ID: mdl-32047522

RESUMO

This study aimed to determine the total phenolic content, DPPH scavenging, α-glucosidase, and nitric oxide (NO) inhibition of Gynura procumbens and Cleome gynandra extracts obtained with five different ethanolic concentrations. The findings showed that the 100% ethanolic extract of G. procumbens had the highest phenolic content and the lowest IC50 values for DPPH scavenging and NO inhibition activity compared to the properties of the other extracts. For C. gynandra, the 20% and 100% ethanolic extracts had comparably high total phenolic contents, and the latter possessed the lowest IC50 value in the NO inhibition assay. In addition, the 20% ethanolic extract of C. gynandra had the lowest IC50 value in the DPPH scavenging assay. However, none of the extracts from either herb had the ability to inhibit α-glucosidase enzyme. Pearson correlation analysis indicated a strong relationship between the phenolic content and DPPH scavenging activity in both herb extracts. A moderately strong relationship was also observed between the phenolic content and NO inhibition in G. procumbens extracts and not in C. gynandra extracts. The UHPLC-ESI-Orbitrap-MS revealed major phenolics from the groups of hydroxycinnamic acids, hydroxybenzoic acids, and flavonoid derivatives from both herbs, which could be the key contributors to their bioactivities. Among the identified metabolites, 24 metabolites were tentatively assigned for the first time from both species of studied herbs. These two herbs could be recommended as prospective natural products with valuable medicinal properties.

19.
BMC Complement Med Ther ; 20(1): 56, 2020 Feb 17.
Artigo em Inglês | MEDLINE | ID: mdl-32066426

RESUMO

BACKGROUND: Ficus deltoidea (FD) has been shown to have antidiabetic, anti-inflammatory, antinociceptive and antioxidant properties. However, its effects on key events in the pathogenesis of atherosclerosis are unknown. AIM: To investigate the endothelial activation, inflammation, monocyte-endothelial cell binding and oxidative stress effects of four FD varieties. METHODS: Human coronary artery endothelial cells (HCAEC) were incubated with different concentrations of aqueous ethanolic extracts of FD var. trengganuensis (FDT), var. kunstleri (FDK), var. deltoidea (FDD) and var. intermedia (FDI), together with LPS. Protein and gene expression of vascular cell adhesion molecule-1 (VCAM-1), intercellular cell adhesion molecule-1 (ICAM-1), endothelial-leukocyte adhesion molecule-1 (E-selectin), interleukin-6 (IL-6), Nuclear factor-κB (NF-κB) p50 and p65 and endothelial nitric oxide synthase (eNOS) were measured using ELISA and QuantiGene plex, respectively. Adhesion of monocyte to HCAEC and formation of reactive oxygen species (ROS) were detected by Rose Bengal staining and 2'-7'-dichlorofluorescein diacetate (DCFH-DA) assay. RESULTS: FDK exhibited the highest inhibition of biomarkers in relation to endothelial activation and inflammation, second in reducing monocyte binding (17.3%) compared to other varieties. FDK (25.6%) was also the most potent at decreasing ROS production. CONCLUSION: FD has anti-atherogenic effects, possibly mediated by NF-κB and eNOS pathways; with FDK being the most potent variety. It is potentially beneficial in mitigating atherogenesis.


Assuntos
Células Endoteliais/efeitos dos fármacos , Ficus/química , NF-kappa B/metabolismo , Óxido Nítrico Sintase Tipo III/metabolismo , Extratos Vegetais/farmacologia , Adesão Celular/efeitos dos fármacos , Células Cultivadas , Vasos Coronários/citologia , Humanos , Inflamação , Monócitos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos
20.
J Ethnopharmacol ; 254: 112657, 2020 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-32045683

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Malaria, a devastating infectious disease which was initially recognized as episodic fever, is caused by parasitic protozoan of the genus Plasmodium. Medicinal plants with ethnobotanical information to treat fever and/or malaria has been the key element in identifying potential plant candidates for antimalarial screening. Goniothalamus lanceolatus Miq. (Annonaceae) is used as a folk remedy, particularly to treat fever and skin diseases. AIM OF THE STUDY: In this context, supported with previous preliminary data of its antiplasmodial activity, this study was undertaken to determine the in vitro antiplasmodial and cytotoxicity activities of G. lanceolatus crude extracts and its major compounds. MATERIALS AND METHODS: The in vitro antiplasmodial activity was determined by parasite lactate dehydrogenase (pLDH) assay on chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum. The cytotoxicity activity was evaluated using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay on hepatocellular carcinoma (HepG2) and normal liver (WRL-68) cell lines. RESULTS: The root methanol extract possessed potent antiplasmodial activity against both P. falciparum 3D7 and K1 strains (IC50 = 2.7 µg/ml, SI = 140; IC50 = 1.7 µg/ml, SI = 236). Apart from the DCM extract of stem bark and root that were found to be inactive (IC50 > 50 µg/ml) against 3D7 strain, all other tested crude extracts exhibited promising (5< IC50 < 15 µg/ml) to moderate (15< IC50 < 50 µg/ml) antiplasmodial activity against both strain. Additionally, only compound C (Parvistone D) exerted promising antiplasmodial activity against 3D7 strain (IC50 = 7.5 µM, SI = 51) whereas compound A, B and D showed moderate antiplasmodial activity against the same strain (20 < IC50 < 100 µM). Interestingly, when tested on K1 strain, compound A, C and D exhibited promising antiplasmodial activity (2 < IC50 < 20 µM) while compound B exhibited moderate activity (IC50 = 26.9 µM). Cytotoxicity study showed that all tested crude extracts and compounds were non-toxic on WRL-68 and HepG2 cell lines (CC50 > 30 µg/ml, CC50 > 10 µM, respectively), except for the hexane and DCM extracts of root, which exerted mild cytotoxicity on HepG2 cell line (IC50 < 30 µg/ml). CONCLUSIONS: This study suggests that the root methanol extract and compound C (Parvistone D) obtained from G. lanceolatus are highly potential for exploitation as source of antimalarial agents. Parvistone D is identified as one of the bioactive styryl lactones found in the plant extract. It is also noteworthy, that the extract and compound were more active against chloroquine-resistant (K1) strain of P. falciparum. Further studies are being carried out to assess their toxicity profile and antimalarial efficacy in animal model.


Assuntos
Sobrevivência Celular/efeitos dos fármacos , Goniothalamus/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Linhagem Celular Tumoral , Células do Cúmulo , Relação Dose-Resposta a Droga , Etnofarmacologia , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Casca de Planta/química , Extratos Vegetais/química , Raízes de Plantas/química
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