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青蒿为菊科草本植物黄花蒿(Artemisia annua L.)。广布于我国广东、广西、云南、四川、山东等省,均有大量野生,资源丰富。 青蒿首载于《神农本草经》及马王堆出土的《五十二病方》,晋·葛洪《肘后备急方》。此后,宋元明清各医籍本草均以复方青蒿汤、截疟青蒿丸、青蒿散以及青蒿别甲煎等治疟记载。民间常取青蒿叶的鲜汁治疗疟疾。除此之外,中医还用于解暑热、祛虚热、健胃、止血、杀虫等方面。 我国从中分离出抗疟有效单体——青蒿素。对恶性性疟、脑型疟及抗氯喹疟原虫有特效。经过结构修饰,经催化氢化生成无抗疟作用的氢化青蒿素,与钠硼氢反应生成抗疟效价更高的双氢蒿素,从此出发,选择反应条件温和的三类反应,制备了三十多个青蒿素衍生物。其中水溶性青蒿酯钠,油溶性蒿甲醚抗疟效价均较青蒿索强6倍左右。化学结构见下:
Artemisia annua is the asteraceae herb Artemisia annua L. Widely distributed in our country Guangdong, Guangxi, Yunnan, Sichuan, Shandong and other provinces, have a large number of wild, rich in resources. Artemisia is first placed on “Shen Nong’s Materia Medica” and Mawangdui “Fifty-two Diseases”, Jin Gehong “elbow backup emergency.” Since then, the Song, Yuan Ming and Qing dynasties of Materia Medica are Compound Artemisia decoction, cut off Malaria Artemisia annua, Artemisia annua and Artemisia annua and other treatment of Malaria record. Often take fresh leaves of Artemisia annua malaria treatment. In addition, Chinese medicine is also used to relieve heat, remove heat, stomach, hemostasis, insecticidal and so on. China isolated from the effective anti-malarial monomer - artemisinin. On the falciparum malaria, cerebral malaria and chloroquine resistant Plasmodium have special effects. After structural modification, the hydrogenated artemisinin without antimalarial activity was generated by catalytic hydrogenation and reacted with sodium borohydride to produce the artemisinin with higher antimalarial potency. Based on these, three types of reactions with mild reaction conditions were selected and prepared More than thirty artemisinin derivatives. Among them, the water-soluble sodium artemethane and the oil-soluble artemether antimalarial potency were 6 times stronger than that of Artemisia annua. See below for the chemical structure: