Identification and Antiproliferative Activity Evaluation of a Series of Triterpenoids Isolated from Flueggea virosa (Roxb. ex Willd.)

Abstract

Problem statement: Medicinal plants derived anticancer were now being subjects of many research groups especially, the secondary metabolite triterpenoids trees which had enormous potential to inspire and influence modern antiproliferative research. The study aimed to investigate the chemical constitution and their potential use as antiproliferative activity of purified compounds derived from F. virosa. Approach: The F. virosa was selected and percolated with hexane, ethyl acetate, acetone and methanol. The extracts were purified and elucidated chemical structures. Furthermore, the isolated compounds were tested for biological activity. The bioassays were performed on two cancer cell lines, adriamycin-sensitive erythroleukemia cells (K562) and adriamycin-resistant erythroleukemia cells (K562/Adr) which overexpressed P-glycoprotein (MDR1/ABCB1). Results: Friedelin (1), epifriedelanol (3), stigmasterol (4) and betulinic acid (5) were isolated from the leaves and twigs of F. virosa. The molecular structures of these compounds were determined using several spectroscopic methods. The compounds i.e., 1, a chemically modified compound 1 heptanolide (2), 3 and 4 showed a limited cytotoxic activity towards human cancer cell lines mainly due to a low aqueous solubility which prevented their use in cell viability assays. Interestingly, compound 5 exhibited a high cytotoxicity characterized by an effective concentration value (IC 50 ) equal to 9.7±2.1 µg.mL −1 (21.2±4.6 µM) and 7.1±0.7 µg.mL −1 (15.5±1.5 µM) for K562and K562/Adr, respectively. Moreover, the antiproliferative activity of compound 5 was independent of the multidrug resistance phenotype exhibited by the K562/Adr cell line suggesting that compound 5 was not the effluxes out of the K562/Adr cells by MDR1 (ABCB1). Conclusion: The results clearly showed that the betulinic acid of the four isolated compounds from F. virosa could be considered as high potential source of cytotoxic activity.

Anti-Syncytium (MC99+1A2) and Anti-Bacterial Activities from Twigs and Stems of Ficus dubia

“…= 284285 °C (lit. 281283 °C) [17,18,19]; IR (KBr), ν max : 3474 (OH stretching), 2932, 2853, 1385 cm -1 ; 13 C and 1 H NMR data, see Table 4.…”

Anticancer activity of ethyl acetate and n-butanol extracts from rhizomes of Agapetes megacarpa W.W. Smith

“…Several constituent have been identified from A. obouata (Chen et al, 1990), A. hosseana (Deng and Chen, 1991) and A. neriifolia (Xuan, 2006). Among those, the anticancer activities for β-sitosterol (Awad et al, 2003;Park et al, 2007;Zhao et al, 2009), friedelanol (Kundu et al, 2000) and friedelin (Monkodkaew et al, 2009;Ding et al, 2010) have been shown. Those compounds were reported as cytotoxic to some cancer cells in vitro.…”

Isolation and Characterisation of Bergenin From Ethyl Acetate Extract of Flueggea Virosa Leaves

“…It has grey or brown bark that is smooth, fissured or rough [1]. Flueggea virosa is found throughout the tropical regions of Africa and Asia where it is often found along water courses and in fallow, disturbed lands up to 2300 m above sea level [2]. Different parts of the plant are used to treat many diseases like diabetes, HIV -AIDS and related infection, arrhythmia, malaria, fever, hepatitis and epilepsy [3].…”