Ammon H P T
Department of Pharmacology and Toxicology, Institute of Pharmaceutical Sciences, University of Tuebingen, Auf der Morgenstelle 8, 72076, Tuebingen, Germany.
, Im Kleeacker 30, 72072, Tuebingen, Germany.
Adv Exp Med Biol. 2016;928:291-327. doi: 10.1007/978-3-319-41334-1_13.
Boswellic acids, which are pentacyclic triterpenes belong to the active pharmacological compounds of the oleogum resin of different Boswellia species. In the resin, more than 12 different boswellic acids have been identified but only KBA and AKBA received significant pharmacological interest. Biological Activity: In an extract of the resin of Boswellia species multiple factors are responsible for the final outcome of a therapeutic effect, be it synergistic or antagonistic. Moreover, the anti-inflammatory actions of BAs are caused by different mechanisms of action. They include inhibition of leukotriene synthesis and to a less extend prostaglandin synthesis. Furthermore inhibition of the complement system at the level of conversion of C3 into C3 and C3. A major target of BAs is the immune system. Here, BEs as well as BAs including KBA and AKBA, have been shown to decrease production of proinflammatory cytokines including IL-1, IL-2, IL-6, IFN-γ and TNF-α which finally are directed to destroy tissues such as cartilage, insulin producing cells, bronchial, intestinal and other tissues. NFĸB is considered to be the target of AKBA. The complex actions of BEs and BAs in inflamed areas may be completed by some effects that are localized behind the inflammatory process as such tissue destruction. In this case, in vitro- and animal studies have shown that BAs and BEs suppress proteolytic activity of cathepsin G, human leucocyte elastase, formation of oxygen radicals and lysosomal enzymes.
Whereas KBA is absorbed reaching blood levels being close to in vitro IC AKBA which is more active in in vitro studies than KBA, but undergoes much less absorption than KBA. However, absorption of both is increased more than twice when taken together with a high-fat meal.Clinical Studies There are a variety of chronic inflammatory diseases which respond to treatment with extracts from the resin of Boswellia species. Though, the number of cases is small in related clinical studies, their results are convincing and supported by the preclinical data. These studies include rheumatoid arthritis, osteoarthritis, chronic colitis, ulcerative colitis, collagenous colitis, Crohn's disease and bronchial asthma. It can not be expected that there is cure from these diseases but at least improvement of symptoms in about 60-70 % of the cases. Side Effects The number and severity of side effects is extremely low. The most reported complaints are gastrointestinal symptoms. Allergic reactions are rare. And most authors report, that treatment with BEs is well tolerated and the registered side effects in BE- and placebo groups are similar.
乳香酸是五环三萜类化合物，属于不同乳香属植物油胶树脂的活性药理成分。在树脂中，已鉴定出12种以上不同的乳香酸，但只有酮基乳香酸（KBA）和乙酰基乳香酸（AKBA）受到了显著的药理关注。
在乳香属植物树脂提取物中，多种因素决定了治疗效果的最终结果，可能是协同作用或拮抗作用。此外，乳香酸的抗炎作用由不同的作用机制引起。它们包括抑制白三烯合成，对前列腺素合成的抑制作用较小。此外，在C3转化为C3和C3的水平上抑制补体系统。乳香酸的一个主要靶点是免疫系统。在这里，乳香提取物（BEs）以及包括KBA和AKBA在内的乳香酸已被证明可减少促炎细胞因子的产生，包括白细胞介素-1（IL-1）、白细胞介素-2（IL-2）、白细胞介素-6（IL-6）、干扰素-γ（IFN-γ）和肿瘤坏死因子-α（TNF-α），这些细胞因子最终会导致软骨、胰岛素产生细胞、支气管、肠道和其他组织等组织的破坏。核因子κB（NFĸB）被认为是AKBA的靶点。BEs和乳香酸在炎症区域的复杂作用可能由一些位于炎症过程（如组织破坏）之后的局部效应来完成。在这种情况下，体外和动物研究表明，乳香酸和BEs可抑制组织蛋白酶G、人白细胞弹性蛋白酶的蛋白水解活性、氧自由基的形成和溶酶体酶。
KBA可被吸收，达到接近体外半数抑制浓度（IC）的血药浓度。AKBA在体外研究中比KBA更具活性，但吸收比KBA少得多。然而，与高脂餐一起服用时两者的吸收均增加两倍以上。
有多种慢性炎症性疾病对乳香属植物树脂提取物治疗有反应。尽管相关临床研究中的病例数量较少，但其结果令人信服，并得到临床前数据的支持。这些研究包括类风湿性关节炎、骨关节炎、慢性结肠炎、溃疡性结肠炎、胶原性结肠炎、克罗恩病和支气管哮喘。无法期望这些疾病能被治愈，但至少约60%-70%的病例症状会有所改善。
副作用的数量和严重程度极低。最常报告的不适是胃肠道症状。过敏反应罕见。大多数作者报告，BEs治疗耐受性良好，BE组和安慰剂组记录的副作用相似。
