大葉南蛇藤及光果南蛇藤之生物活性成份研究

Studies on the Bioactive Constituents of Celastrus kusanoi and C. punctatus

李怜誼(Ling-Yi Lee)

指導教授 ： 林忠男

高雄醫學大學/藥學院/藥學研究所/碩士(2009年)

摘要

本研究乃將大葉南蛇藤 (Celastrus kusanoi) 與光果南蛇藤 (Celastrus punctatus) 的莖分別進行成份分離及生物活性探討。由大葉南蛇藤的CHCl3萃取液中分離得到一個新化合物，3β-trans-(3,4-dihydroxycinnamoyloxy)
-11α-hydroxy-urs-12-ene (2) 以及五個已知物分別為3β-hydroxy-5,8-epidioxyergosta-6,22-diene (1)、cholest-5-ene-3β,4β-diol (3)、nimbidiol (4)、β-sitosterol (5)、β-sitosterol-3-O-β-D-glucopyranoside (6)。由光果南蛇藤的CHCl3萃取液中得到三個已知物，分別為β-amyrin (7)、β-sitosterol (8) 和β-amyrin palmitate (9)，並進行生物活性試驗。探討β-amyrin (7) 和β-amyrin palmitate (9) 這類五環三萜類 (pentacyclic triterpenes) 化合物對於NTUB1人類膀胱癌細胞毒殺活性、誘導或抑制活性氧分子 (Reactive Oxygen Species，ROS) 作用及腫瘤細胞週期停滯 (cell cycle arrest) 研究。結果顯示β-amyrin palmitate (9) 脂溶性大，實驗過程會析出，故不採計其結果。而β-amyrin (7) 有細胞毒殺的活性，進一步探討發現β-amyrin (7) 有誘導ROS的產生及使NTUB1細胞週期停滯在G1 phase產生細胞凋亡作用。同時發現β-amyrin (7) 與抗癌藥物cisplatin併用時，有助於提升cisplatin細胞毒殺的效果，未來在臨床治療上與cisplatin併用，也許可減少cisplatin治療時所帶來的副作用。這個結果開啟了日後對於三萜類藥物開發的興趣，作為未來有潛力的抗癌藥物。

關鍵字

大葉南蛇藤 ； 光果南蛇藤

並列摘要

A new terpenoid, 3β-trans-(3,4-dihydroxycinnamoyloxy)
-11α-hydroxy-urs-12-ene (2) and five known compounds, 3β-hydroxy-5,8-epidioxyergosta-6,22-diene (1), cholest-5-ene-3β,4β-diol (3), nimbidiol (4), β-sitosterol (5) and β-sitosterol-3-O-β-D-glucopyranoside (6) were isolated from the stems of Celastrus kusanoi by chromatography with silica gel column and determined by spectroscopic methods. Three known compounds, β-amyrin (7), β-sitosterol (8) and β-amyrin palmitate (9) were isolated from the stems of Celastrus punctatus, another plant of the genus Celastrus. In pharmacological studies, β-amyrin (7), a pentacyclic triterpene, revealed significant cytotoxic activity and induced ROS (Reactive Oxygen Species). In cell cycle distribution assay, β-amyrin (7) was arrested NTUB1 cells in G1 phase. The cytotoxic activity of β-amyrin (7) may have the relationship with inducing production of ROS and cell cycle arrest. β-Amyrin (7) also enhanced the cytotoxic activity of cisplatin. Combination of cisplatin and β-amyrin (7) will improve clinical response and lower the side effect of cisplatin. This finding opens interesting perspects for further exploration of the triterpenoids as potential anticancer drugs.

並列關鍵字

Celastrus kusanoi ； C. punctatus

參考文獻

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