無患子與五倍子活性成分之研究

Studies on the Bioactive Constituents from Sapindus mukorossi and Galla Chinensis

黃慧琪(Hui-Chi Huang)

指導教授 ： 吳永昌

共同指導教授 ： 郭曜豪(Yao-Haur Kuo)

高雄醫學大學/藥學院/藥學研究所/博士(2006年)

摘要

以抗癌、抗菌和殺福壽螺進行一系列台灣產天然物之活性篩選，發現無患子果實甲醇萃取物和五倍子(羅氏鹽膚木的蟲癭)乙醇萃取物皆具有有效的抗菌作用，無患子果實甲醇萃取物對害蟲殺福壽螺具有殺螺作用，而無患子蟲癭乙醇萃取物則具有抗血小板凝集作用與抗癌作用，因此分別進行無患子果實、蟲癭與五倍子其化學成分和生物活性成分之研究。
由無患子的果實中分離純化得到六個新化合物，三十五個為已知化合物。Oleanane-type saponins的化合物對福壽螺具有有效的防治作用，在濃度10 ppm下其致死率為70~90 %。除此之外，此類化合物也具有效的抗發炎作用。
無患子蟲癭分離純化得到二十二個新化合物和三十六個已知化合物。所分離之化合物進行抗血小板試之體外篩選生物活性研究，發現tirucallane-type saponins的新化合物不會引起血小板細胞毒性 (LDH leakage, <14.71 %, conc. 30 ?嵱) 之下，能夠有效地抑制platelet-activity factor (PAF), arachidonic acid (AA), thrombin (THB) 和U46619所誘導的血小板凝集反應；其中獲致的十個新dammarane type saponins的化合物，部份具有抗癌作用。
五倍子中分離純化得到二十一個為已知化合物，所分離之化合物目前正進行抗菌和抗發炎作用試驗。
由上述植物中共發現二十八個新化合物和九十二個已知化合物，其皆藉由一維、二維核磁共振光譜等物理數據和部份以化學方法確認其化學結構。

關鍵字

無患子 ； 五倍子 ； 蟲癭 ； 殺福壽螺活性 ； 抗血小板凝集 ； 抗菌和抗發炎作用

並列摘要

As a series of studies on the chemical constituents and biological activities (anti-canacer, anti-molluscoid, and anti-bacteria) of Taiwanese plants, the methanolic extracts of the fruits of Sapindus mukorossi and the EtOH extract of Galla Chinensis (the galls of Rhus chinensis) had antibacterial activity and the EtOH extract of the fruits of S. mukorssii showed the effect of causing death of Pomacea canaliculata (Lamarck), as well as the EtOH extract of the galls of S. mukorossi showed anti-platelet aggregation activity and cytotoxicity against several human tumor cell lines.
Investigation of the methanolic extract of fruits of S. mukorossi led to the isolation of six new saponins and thirty-five known compounds. The bioassay for preventive activity test against Pomacea canaliculata revealed that Oleanane-type saponins had 70~90 % inhibition at a concentration of 10 ppm. In addition, the oleanane-type saponins also show significant anti-inflammatory activity.
Twenty-two new compounds together with thirty-six known compounds were isolated from the galls of S. mukorossii. Biological evaluation showed that tirucallane-type saponins, had potent anti-platelet aggregation [induced by platelet-activity factor (PAF), arachidonic acid (AA), thrombin (THB) and U46619] and
no obvious cytotoxicity (measured by LDH leakage, <14.71 %, conc. 30 ?嵱).
Subsequent purification of Galla Chinensis yielded twenty-one known isolates including flavanoids, triterpenes, and tannins. The evaluation in anti-bacteria and anti-inflammatory activity for these isolates is still under progress.
The structural elucidation of these twenty-eight new and ninety-two known compounds are based on spectroscopic analyses (mainly 1D and 2D NMR techniques), as well as by chemical evidences.

並列關鍵字

Sapindus mukorossi ； Galla Chinensis ； Galls ； anti-molluscoid ； anti-platelet aggregation ； anti-bacteria and anti-inflammatory activity

參考文獻

第九章 參考文獻

1. Chen, C.H., Flora of Taiwan, editorial committee of the flora of Taiwan, second edition, Taiwan, 3, 599-608, 1993

2. Nakayama, K., Saponins of pericarps of Chinese Sapindus delavayi (Pyi-shiau-tzu), a source of natural surfactants, Chem. Pharm. Bull., 34, 2209-2213, 1986.

3. Wong, W., Acyclic sesquiterpene oligoglycosides from pericarps of Sapindus delavayi, Phytochemistry, 30, 2699-2702, 1991.

4. Kasai, R., Nishi, M., Mizutani, K., Miyahara, I., Moriya, T., Miyahara, K. and Tanaka, O., Trifolioside II, an acyclic sesquiterpene oligoside from pericarps of Sapindus trifoliatus, Phytochemistry, 27, 2209-2211, 1988.