Department of Biomedical Science, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, UPM Serdang 43400, Selangor, Malaysia.
Integrative Pharmacogenomics Institute (iPROMISE), Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam Campus, Bandar Puncak Alam Selangor 42300, Malaysia.
Biomolecules. 2020 Feb 12;10(2):280. doi: 10.3390/biom10020280.
leaf has been reported to exert antinociceptive activity. The present study elucidates the possible mechanisms of antinociception modulated by the methanol extract of leaves (MEDL) using various mouse models. The extract (25, 150, and 300 mg/kg) was administered orally to mice for 30 min priot to subjection to the acetic acid-induced writhing-, hot plate- or formalin-test to establish the antinociceptive profile of MEDL. The most effective dose was then used in the elucidation of possible mechanisms of action stage. The extract was also subjected to the phytochemical analyses. The results confirmed that MEDL exerted significant ( < 0.05) antinociceptive activity in those pain models as well as the capsaicin-, glutamate-, bradykinin- and phorbol 12-myristate 13-acetate (PMA)-induced paw licking model. Pretreatment with naloxone (a non-selective opioid antagonist) significantly ( < 0.05) reversed MEDL effect on thermal nociception. Only l-arginine (a nitric oxide (NO) donor) but not N(ω)-nitro-l-arginine methyl ester (l-NAME; a NO inhibitor) or 1-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ; a specific soluble guanylyl cyclase inhibitor) significantly ( < 0.05) modified MEDL effect on the writhing test. Several polyphenolics and volatile antinociceptive compounds were detected in MEDL. In conclusion, MEDL exerted the opioid/NO-mediated antinociceptive activity, thus, justify as a potential source for new analgesic agents development.
叶子已被报道具有镇痛活性。本研究使用各种小鼠模型阐明了 叶子甲醇提取物（MEDL）调制的镇痛作用的可能机制。将提取物（25、150 和 300 mg/kg）口服给予小鼠 30 分钟，然后使其经受乙酸引起的扭体、热板或福马林试验，以建立 MEDL 的镇痛作用特征。然后使用最有效剂量来阐明作用机制阶段。还对提取物进行了植物化学分析。结果证实，MEDL 在这些疼痛模型以及辣椒素、谷氨酸、缓激肽和佛波醇 12-肉豆蔻酸 13-乙酸酯（PMA）诱导的爪舔模型中表现出显著的（<0.05）镇痛活性。纳洛酮（一种非选择性阿片受体拮抗剂）预处理显著（<0.05）逆转了 MEDL 对热痛觉的作用。只有 l-精氨酸（一氧化氮（NO）供体）而不是 N（ω）-硝基-l-精氨酸甲酯（l-NAME；NO 抑制剂）或 1-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮（ODQ；一种特异性可溶性鸟苷酸环化酶抑制剂）显著（<0.05）改变了 MEDL 在扭体试验中的作用。在 MEDL 中检测到几种多酚和挥发性镇痛化合物。总之，MEDL 发挥了阿片类药物/NO 介导的镇痛作用，因此， justifies 作为开发新的镇痛剂的潜在来源。
