3-乙酰基-11-酮-β-乳香酸的抗炎作用及其衍生物的化学修饰(1)
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[摘要] 乳香酸(Bas)是乳香提取物中的活性成分，乳香酸在治疗炎症方面的疾病如类风湿关节炎、慢性支气管炎、哮喘以及慢性发炎性肠道疾病(溃疡性结肠炎和克罗恩病)已经显示出显著的药理活性。数据表明，3-乙酰基-11-酮-β-乳香酸(AKBA)被认为在各种乳香酸中是最强大的。AKBA被发现和确认为5-脂肪氧合酶(5-LOX)强大的抑制剂;AKBA的其他药理活性研究发现，它还充当了p38-MAP激酶强大的抑制剂。为了得到更多的AKBA，它的衍生物BA、KBA、ABA经过一系列化学修饰乙酰化和烯丙基氧化转化为AKBA，从而AKBA的量根据乳香树种和相应树脂质量从0.1%~3.0%上升到25%~35%。
[关键词] 3-乙酰基-11-酮-β-乳香酸；抗炎；5-脂肪氧合酶；p38-MAP激酶
[中图分类号] R961 [文献标识码]A[文章编号]1674-4721(2011)06(a)-015-03
Anti-inflammatory actions and chemical modification of derivatives of 3–acetyl–11–keto–β–boswellic acid
LIU Shaojun1，LIU Lina2
1.Benxi Guangyuan Bio-Technology Co., Ltd., Liaoning Province, Benxi117000, China; 2. Doctor-room, Beijing Fengtai Kandan Middle School, Beijing 100070, China
[Abstract] Boswellic acids (BAs) are active components in extracts of the resin of Boswellia serrata, BAs for the treatment of inflammatory diseases like rheumatoid arthritis, chronic bronchitis, asthma as well as chronic inflammatory bowel diseases (ulcerative colitis and Crohn’s disease) have showed significant pharmacological activity. The data suggests that of the various boswellic acids, 3–acetyl–11–keto–β–boswellic acid (AKBA), is considered the most powerful. AKBA was discovered and identified as very potent 5-LOX inhibitor. Other pharmacological properties of AKBA have been studied and it was found that it also acts as potent inhibitor of the p38-MAP kinases. In order to get more AKBA, its derivatives BA, KBA, ABA through a sequence of chemical modification of acetylation and allylic oxidation were transformed into AKBA, thereby increasing the amount of AKBA from 0.1%-3.0% up to 25%-35%, depending on the Boswellia species and the quality of the corresponding resin.
[Key words] AKBA; Anti-inflammatoriy; 5-lipoxygenase; p38-MAP kinase
乳香酸(boswellic acids，Bas)是传统中药乳香的有效活性成分，在多种动物实验中显示有明显的抗炎作用。乳香酸的药理活性与结构关系即构效关系的研究中发现，3-乙酰基-11-酮-β-乳香酸(AKBA)与其他衍生物相比显示更强大的药理活性[1-2]。鉴于此，将抗炎活性较低的AKBA衍生物进行化学修饰将其转化为具有显著抗炎活性的AKBA，从而大大提高了AKBA的含量，同时也提高了乳香酸的抗炎活性。
1 抗炎活性
现代药理研究表明，乳香酸的抗炎活性具有起效浓度低，毒副作用小，抗炎作用广泛等特点。乳香酸在对一系列炎症疾病的尝试中发现，它不仅对具有红、肿、热、痛典型炎症特征的疾病如风湿性、类风湿关节炎、骨关节炎、滑囊炎、肌腱炎等有效；同样对非典型的炎症如哮喘和炎症性肠道疾病包括溃疡性结肠炎、克罗恩病以及比较罕见的胶原性结肠炎等均显示很强的药理活性。
1.1降低水肿
Norihiro B等[3]研究证实：从乳香中提取及半合成的18个单体成分抑制花生四烯酸所致的炎性水肿 ......
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