臺灣公立成功大學(xué)化學(xué)系教授吳天賞從植物中抽取生物堿合成antofine后,實驗發(fā)現(xiàn)可有效毒殺人類癌細胞,,但這項研究僅止于實驗室,距離臨床實驗還要一段時間,。
專精于中草藥的吳天賞,,從厚桂殼及棱果榕分離抽取合成antofine后實驗發(fā)現(xiàn),antofine對人類肺癌細胞,、乳癌細胞,、鼻咽癌細胞、多重抗藥性鼻咽癌細胞的癌細胞株,,具有極佳的細胞毒殺活性,。
吳天賞表示,antofine對腫瘤細胞生長有很強的抑制作用,,對當(dāng)前開發(fā)抗癌藥物是一個新契機,,且是新的先導(dǎo)抗癌藥物,若是再繼續(xù)研發(fā),,可能發(fā)展出抗癌新藥,。
吳天賞的這項研究,已在今年的愛思唯爾期刊《生物有機醫(yī)藥化學(xué)》雜志刊登,。(生物谷Bioon.com)
生物谷推薦原始出處:
Bioorganic & Medicinal Chemistry,,doi:10.1016/j.bmc.2008.04.032 ,Chung-Ren Su,,Tian-Shung Wu
Total synthesis of phenanthroindolizidine alkaloids (±)-antofine, (±)-deoxypergularinine, and their dehydro congeners and evaluation of their cytotoxic activity
Chung-Ren Sua, Amooru G. Damua, Po-Cheng Chiangb, Kenneth F. Bastowb, Susan L. Morris-Natschkeb, Kuo-Hsiung Leeb and Tian-Shung Wua, ,
aDepartment of Chemistry, National Cheng Kung University, Tainan 701, Taiwan, ROC
bNatural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, United States
Due to their limited natural abundance and significant biochemical effects, we synthesized the alkaloids (±)-antofine (1a), (±)-deoxypergularinine (1b), and their dehydro congeners (2 and 3) starting from the corresponding phenanthrene-9-carboxaldehydes. We also evaluated their in vitro cytotoxic activity. Compounds 1a and 1b showed significant potency against various human tumor cell lines, including a drug-resistant variant, with EC50 values ranging from 0.16 to 16 ng/mL. Structure–activity correlations of these alkaloids and some of their synthetic intermediates were also ascertained. The non-planar structure between the two major moieties, phenanthrene and indolizidine, plays a crucial role in the cytotoxic activity of phenanthroindolizidines. Increasing the planarity and rigidity of the indolizidine moiety significantly reduced potency. A methoxy group at the 2-position (1a) was more favorable for cytotoxic activity than a hydrogen atom