Τίτλος:
Estrogenic and cytotoxic potentials of compounds isolated from Millettia macrophylla Benth (Fabaceae): Towards a better understanding of its underlying mechanisms
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
Background: Millettia macrophylla was previously reported to have estrogenic effects and to prevent postmenopausal osteoporosis in Wistar rats. So, the study deals with the identification of its secondary metabolites and the evaluation of their estrogenicity and cytotoxicity toward tumoural cells. Thus, 13 known compounds were obtained from successive chromatographic columns and identified by NMR data compared to those previously reported. Methods: In vitro estrogenicity of the isolates and the phenolic fraction (PF) of M. macrophylla were performed by E-screen and reporter gene assays, while their cytotoxicity was evaluated by Alamar Blue (resazurin) assay. A 3-days uterotrophic assay and the ability of PF to alleviate hot flushes in ovariectomized adult rats were tested in vivo. Results: Seven of the 13 secondary metabolites turned to be estrogenic. Only two exhibited cytotoxic effects on MCF-7 and MDA-MB-231 with CC50 values of 110 μM and 160 μM, respectively. PF induced a significant (p < 0.01) MCF-7 cells proliferation and transactivated both ERα and ERβ in the reported gene assay at 10-2 μg/mL. In vivo, PF acted more efficiently than the methanol crude extract, resulting to a significant (p < 0.01) increase in the uterine wet weight, uterine protein level, uterine and vaginal epithelial height at the dose of 10 mg/kg BW. In addition, PF reduced the average duration and frequency of hot flushes induced in rat. Conclusion: These aforementioned results indicate that PF is a good candidate for the preparation of an improved traditional medicine able to alleviate some menopausal complaints such as vaginal dryness and hot flushes. Graphical abstract: Estrogenic and cytotoxic potentials of compounds isolated from Millettia macrophylla Benth. (Fabaceae): towards a better understanding of its underlying mechanism © 2016 The Author(s).
Συγγραφείς:
Zingue, S.
Tchoumtchoua, J.
Ntsa, D.M.
Sandjo, L.P.
Cisilotto, J.
Nde, C.B.M.
Winter, E.
Awounfack, C.F.
Ndinteh, D.T.
Clyne, C.
Njamen, D.
Halabalaki, M.
Creczynski-Pasa, T.B.
Περιοδικό:
BMC Complementary and Alternative Medicine
Εκδότης:
BioMed Central Ltd.
Λέξεις-κλειδιά:
afromorsin; daidzein; dihydrocoumestrol dimethylether; estradiol benzoate; estrogen receptor alpha; estrogen receptor beta; flemichapparin B; formononetin; genistein; lupenone; lupeol; methanol; Millettia macrophylla extract; palmitic acid; phenol derivative; pisatin; plant extract; secundiferol 1; stigmastenone; unclassified drug; variabilin; estrogen; plant extract, animal experiment; animal tissue; Article; cell proliferation; controlled study; drug cytotoxicity; drug dose comparison; drug mechanism; drug structure; endometrium; estrogen activity; female; hot flush; human; human cell; in vivo study; mass spectrometry; MCF 7 cell line; MDA MB 231 cell line; Millettia; Millettia macrophylla; nonhuman; nuclear magnetic resonance spectroscopy; ovariectomy; phytochemistry; rat; reporter gene; resazurin assay; traditional medicine; transactivation; ultra performance liquid chromatography; uterus weight; vagina epithelium; animal; cell survival; chemistry; cytology; drug effects; MCF-7 cell line; tumor cell line; uterus; vagina, Animals; Cell Line, Tumor; Cell Survival; Estrogens; Female; Humans; MCF-7 Cells; Millettia; Ovariectomy; Plant Extracts; Rats; Uterus; Vagina
DOI:
10.1186/s12906-016-1385-5
