Programa de Pós-Graduação em Ciências Farmacêuticas, Brazil.
Facultad de Química, Universidad Autónoma de Yucatán (UADY), Mérida, Yucatán, Mexico.
J Ethnopharmacol. 2016 May 26;184:30-41. doi: 10.1016/j.jep.2016.02.046. Epub 2016 Mar 2.
Chrysophyllum cainito L. (Sapotaceae), commonly known as caimito or star apple, is a neotropical tree valued for its ornamental quality and edible fruits. Besides its culinary use, the leaves are also popularly used to treat diabetes mellitus and several inflammatory diseases.
This study aimed to complement previous data obtained about the anti-hypersensitivity effects of the crude methanol extract (CME), CHCl3 fraction and isolated compounds obtained from C. cainito.
The CME, CHCl3 fraction and two isolated triterpenes identified as 3β-Lup-20(29)-en-3-yl acetate (1) and Lup-20(29)-en-3β-O-hexanoate (2) were evaluated regarding their effects using clinical pain models, such as post-operative, inflammatory and neuropathic pain. Acute inflammatory pain models induced by PGE2, epinephrine, LPS and CFA were also used to improve the knowledge about the mechanism of action.
The animals treated with the CME and submitted to PGE2, epinephrine, LPS or CFA had the mechanical hypersensitivity significantly reduced. When repeatedly administered, the CME enhanced the mechanical withdrawal threshold of mice submitted to post-operative pain model, CFA-induced chronic inflammatory pain and two different models of neuropathic pain. In turn, the CHCl3 fraction presented anti-hypersensitivity effect against epinephrine- or LPS-induced hypersensitivity, with a more prominent activity in both the neuropathic pain models. The compound 1 seems to present the same profile of the CHCl3, whereas compound 2 exhibited activity similar to the CME.
This data suggests that the CME effect involves interference in the production, release or action of some chemical mediators, such as PGE2, sympathetic amines, cytokines, etc. Part of these effects was observed with the CHCl3 fraction, emphasizing the prominent inhibition of neuropathic pain. The results also demonstrated that part of the CME effects are due to the presence of the triterpenes 1 and 2, but it is important to mention that we cannot discard the effects of countless other compounds presented in the crude extract, acting in a synergic way.
番石榴（番石榴科），俗称西印度樱桃或星苹果，是一种新热带地区的树木，因其观赏品质和可食用的果实而受到重视。除了烹饪用途外，叶子也常用于治疗糖尿病和几种炎症性疾病。
本研究旨在补充之前关于番石榴粗甲醇提取物（CME）、CHCl3 馏分和从番石榴中分离得到的化合物的抗过敏作用的研究数据。
评估 CME、CHCl3 馏分和两种分离的三萜，鉴定为 3β-Lup-20(29)-en-3-yl 乙酸酯（1）和 Lup-20(29)-en-3β-O-己酸酯（2），在临床疼痛模型中的作用，如术后、炎症和神经病理性疼痛。还使用 PGE2、肾上腺素、LPS 和 CFA 诱导的急性炎症疼痛模型来提高对作用机制的认识。
用 CME 处理并接受 PGE2、肾上腺素、LPS 或 CFA 的动物的机械性过敏反应显著减轻。当重复给药时，CME 增强了接受术后疼痛模型、CFA 诱导的慢性炎症性疼痛和两种不同神经病理性疼痛模型的小鼠的机械性退缩阈值。相反，CHCl3 馏分对肾上腺素或 LPS 诱导的过敏具有抗过敏作用，在两种神经病理性疼痛模型中表现出更明显的活性。化合物 1 似乎具有与 CHCl3 相同的作用谱，而化合物 2 表现出与 CME 相似的活性。
这些数据表明，CME 的作用涉及对某些化学介质（如 PGE2、交感胺、细胞因子等）的产生、释放或作用的干扰。这些作用的一部分是用 CHCl3 馏分观察到的，强调了对神经病理性疼痛的显著抑制。结果还表明，CME 作用的一部分是由于三萜 1 和 2 的存在，但值得注意的是，我们不能排除粗提物中存在的无数其他化合物的协同作用。
