Anti-proliferation activity of terpenoids isolated from Euphorbia kansui in human cancer cells and their structure-activity relationship / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
; (6): 766-774, 2017.
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| ID: wpr-812058
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WPRO
ABSTRACT
Euphorbia kansui is a commonly used traditional Chinese medicine for the treatment of edema, pleural effusion, and asthma, etc. According to the previous researches, terpenoids in E. kansui possess various biological activities, e.g., anti-virus, anti-allergy, antitumor effects. In this work, twenty five terpenoids were isolated from E. kansui, including thirteen ingenane- and eight jatrophane-type diterpenoids (with two new compounds, kansuinin P and Q) and four triterpenoids. Eighteen of them were analyzed by MTS assay for in vitro anticancer activity in five human cancer cell lines. Structure-activity relationship for 12 ingenane-type diterpenoids in colorectal cancer Colo205 cells were preliminary studied. Significant anti-proliferation activities were observed in human melanoma cells breast cancer MDA-MB-435 cells and Colo205 cells. More than half of the isolated ingenane-type diterpenoids showed inhibitory activities in MDA-MB-435 cells. Eight ingenane- and one jatrophane-type diterpenoids possessed much lower IC values in MDA-MB-435 cells than positive control staurosporine. Preliminary structure-activity relationship analysis showed that substituent on position 20 was important for the activity of ingenane-type diterpenoids in Colo205 cells and substituent on position 3 contributed more significant biological activity of the compounds than that on position 5 in both MDA-MB-435 and Colo205 cells.
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Asunto principal:
Farmacología
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Relación Estructura-Actividad
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Terpenos
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Medicamentos Herbarios Chinos
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Estructura Molecular
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Química
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Euphorbia
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Línea Celular Tumoral
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Proliferación Celular
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Quimioterapia
Límite:
Humans
Idioma:
En
Revista:
Chinese Journal of Natural Medicines (English Ed.)
Año:
2017
Tipo del documento:
Article