Bioorganic Chemistry Division, Indian Institute of Integrative Medicine (CSIR), Srinagar, 190005, Jammu and Kashmir, India.
Bioorganic Chemistry Division, Indian Institute of Integrative Medicine (CSIR), Srinagar, 190005, Jammu and Kashmir, India.
Chem Biol Interact. 2015 Oct 5;240:180-98. doi: 10.1016/j.cbi.2015.08.015. Epub 2015 Aug 29.
Arglabin belongs to guaianolide class of sesquiterpene lactones, isolated from Artemisia species. The molecule bears a 5,7,5-tricyclic ring system having five contiguous stereo centers in which the two five membered rings are trans-annulated. Arglabin shows promising antitumor activity against different tumor cell lines. The antitumor activity of arglabin proceeds through its inhibition of farnesyl transferase which leads to the activation of RAS proto-oncogene, a process that is believed to play a pivotal role in 20-30% of all human tumors. It actually inhibits the incorporation of farnesyl pyrophosphate into human H-ras proteins by the enzyme farnesyl transferase (FTase). The present review is an attempt to summarize the chemistry and biology of this molecule since its isolation in 1982. It embodies the isolation, structure elucidation, stereo chemical description, structural classification, chemical synthesis, structural modifications and antitumor evaluation reported till date.
阿格雷宾属于倍半萜内酯类化合物，从蒿属植物中分离得到。该分子具有 5,7,5-三环体系，其中两个五元环反式稠合，具有五个连续的立体中心。阿格雷宾对不同肿瘤细胞系表现出有希望的抗肿瘤活性。阿格雷宾的抗肿瘤活性通过其抑制法呢基转移酶来进行，这导致 RAS 原癌基因的激活，这一过程被认为在所有人类肿瘤的 20-30%中起着关键作用。它实际上抑制了法尼基焦磷酸与人类 H-ras 蛋白的酶法尼基转移酶 (FTase) 的结合。自 1982 年分离以来，本综述试图总结该分子的化学和生物学特性。它包含了迄今报道的分离、结构阐明、立体化学描述、结构分类、化学合成、结构修饰和抗肿瘤评价。
