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Compounds from the Petroleum Ether Extract of Wedelia chinensis with Cytotoxic, Anticholinesterase, Antioxidant, and Antimicrobial Activities.

ABSTRACT: Wedelia chinensis is a folk medicine used in many Asian countries to treat various ailments. Earlier investigations reported that the petroleum ether extract of the plant has potential biological activity, but the compounds responsible for activity are not yet completely known. Therefore, the current work was designed to isolate and characterize the compounds from the petroleum ether extract and to study their bioactivities. Four compounds including two diterepenes (-) kaur-16α-hydroxy-19-oic acid (1) and (-) kaur-16-en-19-oic acid (2), and two steroids β-sitosterol (3), and cholesta-5,23-dien-3-ol (4) were isolated and characterized. Among the compounds, the diterpenes were found to have more biological activities than the steroidal compounds. Compound 1 showed the highest cytotoxicity with LC₅₀ of 12.42 ± 0.87 μg/mL. Likewise, it possesses good antioxidant activity in terms of reducing power. On the contrary, compound 2 exerted the highest antiacetylcholinesterase and antibutyrylcholinesterase activity. Both the diterpenes showed almost similar antibacterial and antifungal activity. The identification of diterpenoid and steroid compounds with multifunctional activities suggests that W. chinensis may serve as an important source of bioactive compounds which should be further investigated in animal model for therapeutic potential in the treatment of different chronic diseases.

SUBMITTER: Khan MAR

PROVIDER: S-EPMC9865212 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature

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Compounds from the Petroleum Ether Extract of <i>Wedelia chinensis</i> with Cytotoxic, Anticholinesterase, Antioxidant, and Antimicrobial Activities.

Khan Md Abdur Rashid MAR Islam Md Aminul MA Biswas Kushal K Al-Amin Md Yusuf MY Ahammed Md Salim MS Manik Md Imran Nur MIN Islam K M Monirul KMM Kader Md Abdul MA Alam Ahm Khurshid AK Zaman Shahed S Sadik Golam G

Molecules (Basel, Switzerland) 20230113 2

<i>Wedelia chinensis</i> is a folk medicine used in many Asian countries to treat various ailments. Earlier investigations reported that the petroleum ether extract of the plant has potential biological activity, but the compounds responsible for activity are not yet completely known. Therefore, the current work was designed to isolate and characterize the compounds from the petroleum ether extract and to study their bioactivities. Four compounds including two diterepenes (-) kaur-16α-hydroxy-19 ...[more]

PMID: 36677851

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Project description:Ruta chalepensis is an herb used to treat various ailments, and its potential cytotoxic effects on different tumor cell lines have been extensively studied. The present study aimed to evaluate the cytotoxic activity of R. chalepensis methanol extract (RCME), sub-partitions obtained from solvents of increasing polarity, and major compounds, as well as their hemolytic, anti-hemolytic, and antioxidant potential. The in vitro cytotoxic activity against the human hepatocarcinoma (HEP-G2) and the murine lymphoma cell line (L5178Y-R) was evaluated using the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction assay, whereas selectivity indices (SIs) were determined by comparing cytotoxicity against normal African green monkey kidney cells (VERO) and human peripheral blood mononuclear cells (PBMC). Hemolytic and anti-hemolytic activities were evaluated on human erythrocytes. The most effective cytotoxic treatment was evaluated for nitric oxide release by J774A.1 macrophages. Antioxidant activity of R. chalepensis material was also determined. Results showed that RCME produced significant (p < 0.05) cytotoxicity in HEP-G2 (IC50 = 1.79 µg/mL) and L5178Y-R (IC50 = 1.60 µg/mL) cells and exhibited high SIs (291.50 and 114.80, respectively). In addition, the n-hexane fraction (RCHF) showed an IC50 of 18.31 µg/mL in HEP-G2 cells and an SI of 9.48 in VERO cells, whereas the chloroform fraction (RCCF) evidenced an IC50 of 1.60 µg/mL in L5178Y-R cells and an SI of 34.27 in PBMC cells. Chalepensin (CHL), rutamarin (RTM), and graveolin (GRV), which are major components of R. chalepensis, showed high activity against L5178Y-R cells, with IC50 of 9.15, 15.13 and SI of 45.08 µg/mL, respectively. In addition, CHL, RTM, and GRV showed SIs of 24.76, 9.98, and 3.52, respectively, when compared with PBMC cells. RCME at concentrations of 125 µg/mL and 250 µg/mL, significantly (p < 0.05) decreased nitrite production in J774A.1 cells, when exposed to lipopolysaccharide. This study demonstrated that RCME showed significant cytotoxic activity against HEP-G2 and L5178Y-R cells, without affecting normal VERO, PBMC, and J774A.1 cells.

Project description:BackgroundBergenia ciliata is a medicinal plant used for the treatment of diarrhea, vomiting, fever, cough, diabetes, cancer, pulmonary disorders and wound healing.MethodsIn this study, Bergenia ciliata crude extract, subfractions, and isolated compounds were evaluated for their antioxidant and anticholinesterase potential. The free radical scavenging capacities of the extracts determined using DPPH and ABTS assays. The anticholinesterase potentials were determined using acetylcholine esterase and butyryl choline esterase enzymes. To determine the phytochemical composition, the extracts were subjected to HPLC analysis and silica gel column isolation. Based on HPLC fingerprinting results, the ethyl acetate fraction was found to have more bioactive compounds and was therefore subjected to silica gel column isolation. As a result, three compounds; pyrogallol, rutin, and morin were isolated in the pure state. The structures of the isolated compounds were elucidated using spectroscopic techniques like 1H-NMR, IR and UV-Visible.ResultsThe crude extract showed maximum anticholinesterase (acetylcholinesterase = 90.22 ± 1.15% and butyrylcholinesterase = 88.22 ± 0.71%) and free radical scavenging (87.37 ± 2.45 and 83.50 ± 0.70% respectively against DPPH and ABTS radicals) potentials. The total phenolic contents (expressed as equivalent of gallic acid; mgGAE/g) were higher in ethyl acetate fraction (80.96 ± 1.74) followed by crude extract (70.65 ± 0.86) while the flavonoid contents (expressed as quercetin equivalent; mgQE/g) and were higher in crude extract (88.40 ± 1.12) followed by n-butanol fraction (60.10 ± 1.86). The isolated bioactive compounds pyrogallol, rutin, and morin were found active against ABTS and DPPH free radicals. Amongst them, pyrogallol was more active against both free radicals. Reasonable anticholinesterase activities were recorded for pyrogallol against selected enzymes.ConclusionThe extracts and isolated compounds showed antioxidant and acetylcholinesterase inhibitory potentials. It was concluded that this plant could be helpful in the treatment of oxidative stress and neurological disorders if used in the form of extracts.

Project description:BackgroundWedelia chinensis has been reported as a folk medicine for the treatment of different diseases including neurodegenerative disease. Although the plant has been studied well for diverse biological activities, the effect of this plant in neurological disorder is largely unknown. The present study was undertaken to evaluate the cholinesterase inhibitory and antioxidant potential of W. chinensis.MethodsThe extract and fractions of the plant were evaluated for acetylcholinesterase and butyrylcholinesterase inhibitory activity by modified Ellman method. The antioxidant activity was assessed in several in vitro models/assays such as reducing power, total antioxidant capacity, total phenolic and flavonoid content, scavenging of 2,2'-diphenyl-1-picrylhydrazyl (DPPH) free radical and hydroxyl radical, and inhibition of brain lipid peroxidation. Chromatographic and spectroscopic methods were used to isolate and identify the active compound from the extract.ResultsAmong the fractions, aqueous fraction (AQF) and ethylacetate fraction (EAF) exhibited high inhibition against acetylcholinesterase (IC50: 40.02 ± 0.16 μg/ml and 57.76 ± 0.37 μg/ml) and butyrylcholinesterase (IC50: 31.79 ± 0.18 μg/ml and 48.41 ± 0.05 μg/ml). Similarly, the EAF and AQF had high content of phenolics and flavonoids and possess strong antioxidant activity in several antioxidant assays including DPPH and hydroxyl radical scavenging, reducing power and total antioxidant activity. They effectively inhibited the peroxidation of brain lipid in vitro with IC50 values of 45.20 ± 0.10 μg/ml and 25.53 ± 0.04 μg/ml, respectively. A significant correlation was observed between total flavonoids and antioxidant and cholinesterase inhibitory activity. Activity guided chromatographic separation led to the isolation of a major active compound from the EAF and its structure was elucidated as apigenin by spectral analysis.ConclusionsThe potential ability of W. chinensis to inhibit the cholinesterase activity and peroxidation of lipids suggest that the plant might be useful for the management of AD.

Project description:BackgroundAngelica shikokiana is a Japanese medicinal herb that is included among food and drug preparations protecting against cancer; however, there is no previous report about the cytotoxicity of A. shikokiana or its bioactive compounds.ObjectiveThis study was designed to investigate the cytotoxic activities of A. shikokiana methanol extract (AME) and its isolated compounds and to identify the molecular mechanisms of the cytotoxicity.Materials and methodsCytotoxicity and selectivity was investigated by measuring the IC50 values on five cancer cell lines; human hepatocellular carcinoma, rhabdomyosarcoma (RD), colorectal carcinoma, human epithelioma and human breast adenocarcinoma and one normal cell line; human lung fibroblasts. The effects on tubulin polymerization and histone deacetylase 8 (HDAC8), were examined to determine the mechanism of cytotoxicity. Docking study was designed to examine the binding affinity to the target molecules.ResultsMethanol extract and some of its isolated coumarins and flavonoids showed potent, selective cytotoxicity against cancer cell lines. AME and all isolated compounds inhibited tubulin polymerization. Angelicin and kaempferol-3-O-rutinoside were the most active compounds. Phenolic compounds and furanocoumarins showed binding affinity to colchicine binding site rather than the vinblastine binding site of tubulin microtubules. On the other side, quercetin, kaempferol, luteolin, chlorogenic acid, and methyl chlorogenate exhibited the strongest activity against HDAC8 and the highest affinity to trichostatin A binding site.ConclusionThese findings provide the first scientific evidence of the cytotoxicity of AME through inhibition of tubulin polymerization and HDAC8 activity through its coumarin and flavonoid content.SummaryThe present study provides for the first time a clue for the cytotoxic activities of the AME. Our results indicate that the cytotoxic activities are partially related to the ability of AME to inhibit tubulin polymerization and HDAC8 activity. Isolated compounds; Angelicin and kaempferol-3-O-rutinoside showed the strongest inhibition of tubulin polymerization through binding to colchicine binding domain of tubulin microtubules. Phenolic compounds; quercetin, luteolin, kaempferol, chlorogenic acid and methyl chlorogenate exhibited a strong inhibition of HDAC8 through binding to TSA binding site. This, however, further detailed pharmacological and in vivo studies should be the next step in evaluating the cytotoxic activities of AME and its active compounds that are currently ongoing. Abbreviations used: AME: Methanol extract of the aerial part of A. shikokiana, HDACs: Histone deacetylases,HDAC8: Histone deacetylase 8.

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Compounds from the Petroleum Ether Extract of Wedelia chinensis with Cytotoxic, Anticholinesterase, Antioxidant, and Antimicrobial Activities.

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Compounds from the Petroleum Ether Extract of <i>Wedelia chinensis</i> with Cytotoxic, Anticholinesterase, Antioxidant, and Antimicrobial Activities.

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