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

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 ß-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.

Isolation of two new triterpene glycoside from the fruits of Terminalia arjuna and their in vitro and in silico studies.

Two new triterpene glycoside, Arjunoglycoside VI (1) and Arjunursglycoside I (2) alone with five previously known analogues (3-7) were isolated from methanolic extract of the fruits of Terminalia arjuna. The structures were elucidated by extensive spectroscopic studies (1 D and 2 D NMR and mass). Compound 1 and 2 showed moderate activity on α-chymotrypsin enzyme inhibition with IC50 values 53.8 ± 1.39 and 64.27 ± 1.27 µg/mL respectively. Molecular docking was performed for compound 1 and 2 with the 1CGI co crystals of α-chymotrypsin enzyme protein of Bovine from protein data bank showed -7.7 and -7.6 kcal/mol binding energy, respectively.

Evaluation of cholinesterase inhibitory and antioxidant activity of Wedelia chinensis and isolation of apigenin as an active compound.

BACKGROUND: Wedelia 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. METHODS: The 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. RESULTS: Among 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. CONCLUSIONS: The 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.

New ursane triterpene from the fruits of Terminalia arjuna.

A new ursane triterpene, torment (2 alpha,3 beta,19 alpha-trihydroxyurs-12-en) (1), was isolated from the fruits of Terminalia arjuna along with four known ursane and oleane triterpenes. The structures were established on the basis of extensive NMR (1D & 2D) and MS (EI & ESI) studies. Tormentic acid (2), 19 alpha-hydroxy asiatic acid (3) and olean-12-en-2 alpha,3 beta-diol (4) were isolated for the first time from this species. Compounds 1 and 2 lacked significant enzyme inhibition, cytotoxicity, immunomodulatory and antiglycation activities.