is one of the largest genera in the plant kingdom that belongs to the Moraceae family. This review aimed to summarize the medicinal uses, phytochemistry, and pharmacological actions of two major ...species from this genus, namely
and
. These species can be found abundantly in most Asian countries, including Malaysia. The chemical analysis report has shown that
species contained a wide range of phytoconstituents, including phenols, flavonoids, alkaloids, tannins, saponins, terpenoids, glycosides, sugar, protein, essential and volatile oils, and steroids. Existing studies on the pharmacological functions have revealed that the observed
species possessed a broad range of biological properties, including antioxidants, antidiabetic, anti-inflammatory, anticancer, antitumor and antiproliferative, antimutagenic, antimicrobial, anti-helminthic, hepatoprotective, wound healing, anticoagulant, immunomodulatory activities, antistress, toxicity studies, and mosquitocidal effects. Apart from the plant parts and their extracts, the endophytes residing in these host plants were discussed as well. This study also includes the recent applications of the
species and their plant parts, mainly in the nanotechnology field. Various search engines and databases were used to obtain the scientific findings, including Google Scholar, ScienceDirect, PMC, Research Gate, and Scopus. Overall, the review discusses the therapeutic potentials discovered in recent times and highlights the research gaps for prospective research work.
(
) is an
herbal shrub traditionally consumed to treat various diseases including diabetes in Malaysia. This study was designed to evaluate the α-glucosidase inhibitory activity of
leaves extracts, ...and to identify the metabolites responsible for the bioactivity.
Crude extract obtained from the dried leaves using 80% methanolic solution was further partitioned using different polarity solvents. The resultant extracts were investigated for their α-glucosidase inhibitory potential followed by metabolites profiling using the gas chromatography tandem with mass spectrometry (GC-MS).
Multivariate data analysis was developed by correlating the bioactivity, and GC-MS data generated a suitable partial least square (PLS) model resulting in 11 bioactive compounds, namely, palmitic acid, phytol, hexadecanoic acid (methyl ester), 1-monopalmitin, stigmast-5-ene, pentadecanoic acid, heptadecanoic acid, 1-linolenoylglycerol, glycerol monostearate, alpha-tocospiro B, and stigmasterol. In-silico study via molecular docking was carried out using the crystal structure
isomaltase (PDB code: 3A4A). Interactions between the inhibitors and the protein were predicted involving residues, namely LYS156, THR310, PRO312, LEU313, GLU411, and ASN415 with hydrogen bond, while PHE314 and ARG315 with hydrophobic bonding.
The study provides informative data on the potential α-glucosidase inhibitors identified in
leaves, indicating the plant's therapeutic effect to manage hyperglycemia.
The present study has been aimed to investigate the antioxidant and antidiabetic activities of Christia vespertilionis leaves extracts. The analysis of the extracts obtained using different solvents ...revealed that ethyl acetate: methanol extract as the most potential in 2, 2- diphenyl-1-picrylhydrazyl (DPPH) radical scavenging while hexane: ethyl acetate exhibited highest ferric reducing antioxidant power (FRAP) capacity and α-glucosidase inhibition. The infrared analysis displayed the presence of O-H, C-H, C=O, C=C, C-O, and N-H predominantly in the extracts reflecting some of the compounds reported previously; quercetin 3-O-glucoside, oleanolic acid methyl ester, β-sitosterol, stigmasterol, geraniol and 2’-hydroxygenistein. The latter two displayed competitive mode of inhibition in both the yeast and human protein receptors. Conclusively, C. vespertilionis leaves contain potent antioxidants and α-glucosidase inhibitors; thus, further studies can enhance its use in pharmaceutical applications.
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•Christia vespertilionis leaf possess antioxidant and antidiabetic activities.•Functional groups corresponding to the plant's compounds were identified.•In silico study predicted the interaction between the compounds and the protein.
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•The 80% ethanol extract of M. charantia fruit exhibited the most antioxidant activity.Brevifolincarboxylic acid is a new antioxidant compound reported in Momordica charantia ...fruit.3-Malonylmomordicin I and goyaglycoside G are possessing anti-oxidant activity.
Momordica charantia fruit is claimed to have healthy benefit. Despite this potential claim, the phytochemical study of this fruit is still lacking. Thus, this study aimed to evaluate the antioxidants profile of Momordica charantia (Cucurbitaceae) fruit. The antioxidant activity of the ethanolic extracts of various polarities was evaluated and the metabolites that are responsible for its activity were identified using metabolomics approach. Six different mixture of ethanol in water that are 0%, 20%, 40%, 60%, 80%, and 100% (v/v) was extracted using dveseeded fruit sample. Liquid chromatography-mass spectrometry-quadrupole time of flight and multivariate data analysis was used to identify the metabolites that were either antioxidants or pro-oxidants. The 80% ethanol extract exhibited the most antioxidant activity when tested in both 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) antioxidant assays. This extract showed the most intense LC-MS signals represented to ascorbic acid, margarolic acid, brevifolincarboxylic acid, quercetin 3-O-glycoside, kuguacin H, cucurbitacin E, 3-malonylmomordicin I, and goyaglycoside G correlating to the anti-oxidant activity. This study reports for the first time the existence of brevifolincarboxylic acid in this fruit, and the antioxidant activity of 3-malonylmomordicin I and goyaglycoside G. In addition, the loading plots revealed the unknown compounds possessing the antioxidant activity which are potential to be isolated in the future study.
The present study used in vitro and in silico techniques, as well as the metabolomics approach to characterise α-glucosidase inhibitors from different fractions of Clinacanthus nutans. C. nutans is a ...medicinal plant belonging to the Acanthaceae family, and is traditionally used to treat diabetes in Malaysia. n-Hexane, n-hexane: ethyl acetate (1:1, v/v), ethyl acetate, ethyl acetate: methanol (1:1, v/v), and methanol fractions were obtained via partitioning of the 80% methanolic crude extract. The in vitro α-glucosidase inhibitory activity was analyzed using all the fractions collected, followed by profiling of the metabolites using liquid chromatography combined with mass spectrometry. The partial least square (PLS) statistical model was developed using the SIMCA P+14.0 software and the following four inhibitors were obtained: (1) 4,6,8-Megastigmatrien-3-one; (2) N-Isobutyl-2-nonen-6,8-diynamide; (3) 1′,2′-bis(acetyloxy)-3′,4′-didehydro-2′-hydro-β, ψ-carotene; and (4) 22-acetate-3-hydroxy-21-(6-methyl-2,4-octadienoate)-olean-12-en-28-oic acid. The in silico study performed via molecular docking with the crystal structure of yeast isomaltase (PDB code: 3A4A) involved a hydrogen bond and some hydrophobic interactions between the inhibitors and protein. The residues that interacted include ASN259, HID295, LYS156, ARG335, and GLY209 with a hydrogen bond, while TRP15, TYR158, VAL232, HIE280, ALA292, PRO312, LEU313, VAL313, PHE314, ARG315, TYR316, VAL319, and TRP343 with other forms of bonding.
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•The antidiabetic potential of various extracts of C. nutans leaf has been evaluated.•Multivariate data analysis identified 4 α-glucosidase inhibiting compounds.•In silico study predicted the protein-inhibitors interaction.
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•The C. nutans n-hexane fraction is harmful with the LC50 of 75.49 μg/mL.•The mortality rate increased as the fraction concentration increased.•Morphological defects such as less ...pigmentation, dented tail, oedema malformed yolk sac was detected at the median lethal concentration.•GC–MS analysis revealed the presence of sterols, fatty acids and some of its derivatives in the n-hexane fraction.
Clinacanthus nutans, an herbal shrub belonging to the Acanthaceae family, is traditionally used as a functional food to treat various ailments in Malaysia and Indonesia. Although the polar fraction of this plant shows non-toxic effect, the toxicity of the non-polar extract is not reported so far. The present study aimed to assess the toxic effect and determine the lethal concentration of this non-polar fraction using zebrafish embryos. The n-hexane fraction was partitioned from the crude extract of C. nutans obtained using 80% methanolic solution. After spawning of the adult male and female zebrafish, the eggs were collected, transferred into a 96-well plate and incubated with the n-hexane fraction at concentrations of 15.63 μg/ml, 31.25 μg/ml, 62.5 μg/ml, 125 μg/ml, 250 μg/ml and 500 μg/ml in 2% DMSO. The survival and sublethal endpoint were assessed, the mortality and hatchability rates were calculated based on microscopic observation, while the heartbeat rate was measured using DanioScope software. The median lethal concentration (LC50) of the C. nutans n-hexane fraction, which was determined using probit analysis, was calculated to be 75.49 μg/mL, which is harmful. Moreover, gas chromatography-mass spectrometry (GC–MS) analysis revealed the presence of palmitic acid, phytol, hexadecanoic acid, 1-monopalmitin, stigmast-5-ene, pentadecanoic acid, heptadecanoic acid, 1-linolenoylglycerol and stigmasterol in the n-hexane fraction.
The best described pharmacological property of flavonoids is their capacity to act as potent antioxidant that has been reported to play an important role in the alleviation of diabetes mellitus. ...Flavonoids biochemical properties are structure dependent; however, they are yet to be thoroughly understood. Hence, the main aim of this work was to investigate the antioxidant and antidiabetic properties of some structurally related flavonoids to identify key positions responsible, their correlation, and the effect of methylation and acetylation on the same properties. Antioxidant potential was evaluated through dot blot, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, ABTS+ radical scavenging, ferric reducing antioxidant power (FRAP), and xanthine oxidase inhibitory (XOI) assays. Antidiabetic effect was investigated through α-glucosidase and dipeptidyl peptidase-4 (DPP-4) assays. Results showed that the total number and the configuration of hydroxyl groups played an important role in regulating antioxidant and antidiabetic properties in scavenging DPPH radical, ABTS+ radical, and FRAP assays and improved both α-glucosidase and DPP-4 activities. Presence of C-2-C-3 double bond and C-4 ketonic group are two essential structural features in the bioactivity of flavonoids especially for antidiabetic property. Methylation and acetylation of hydroxyl groups were found to diminish the in vitro antioxidant and antidiabetic properties of the flavonoids.
•Phaleria macrocarpa is widely used as a remedy to reduce blood glucose levels.•GC–MS is a distinctive method dominating the metabolomics research area.•Chemometric analysis can be applied to resolve ...large data sets.
Phaleria macrocarpa is a medicinal plant widely available in Malaysia. The plant parts have been traditionally used as an antidiabetic remedy. This study aimed to identify the putative inhibitors of the α-glucosidase enzyme from P. macrocarpa using a gas chromatography-mass spectrometry (GC–MS)-based metabolomics approach and further subjected them to in silico molecular docking analysis to elucidate the possible mechanism of action. This study assessed the inhibitory potential of P. macrocarpa fruit extracts (aqueous, 20 %, 40 %, 60 %, 80 %, and 100 % ethanol) against the α-glucosidase enzyme using GC–MS and chemometric analysis. Orthogonal partial least squares (OPLS) combined with GC–MS analysis were applied to correlate the inhibition of enzyme activity to the metabolites profile of P. macrocarpa. All the potential inhibitors identified were further docked to the yeast (Saccharomyces cerevisiae) protein crystal structure (PDB3A4A). The generated score scatter plot of OPLS showed a recognizable separation of all the extracts into six different clusters. GC–MS, incorporated with multivariate data analysis techniques, was used to identify significant chemical markers. Methyl α-d-glucopyranoside, squalene, palmitic acid, myo-inositol and isoquinoline metabolites were identified as putative inhibitors against α-glucosidase activity from P. macrocarpa. In conclusion, the GC–MS-based metabolomics approach identified potential chemical markers of P. macrocarpa that could be utilized in the development of herbal based medicine.
Momordica charantia is widely consumed edible fruit. The food and pharmaceutical industries use it as a natural antioxidant. However, the quality control of M. charantia-based medicinal products is ...questionable due to the complexity of metabolites in this fruit. Hence, this study has developed a statistical model in predicting the antioxidant value through the 2, 2-diphenyl-1 picrylhydrazyl radical scavenging activity and ferric reducing antioxidant power based on infrared spectroscopy with attenuated total reflectance. This technique was reliably used for quality control. Six ethanol extracts (0, 20, 40, 60, 80, and 100% in water) of this plant's fruit were prepared. The radical scavenging and ferric reducing antioxidant power activities were measured and the chemical profiling of the extracts was fingerprinted by infrared spectroscopy between 4,000 and 600 cm
−1
at a resolution of 4 cm
−1
. Statistical analysis was developed by correlating the bioactivity and infrared spectra of each extract using orthogonal partial least square discriminant analysis. The C-N, C˭O, C-O, C-H, and OH infrared signals were positively correlated with biological activity. The antioxidant activity of the fruit of M. charantia may be due to the presence of several antioxidants that work synergistically.
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