Institute of Food Science and Nutrition Bahauddin Zakariya University Multan, 60800, Pakistan; Institute for Molecular Bioscience, The University of Queensland, Brisbane, QLD, Australia.
Institute of Food Science and Nutrition Bahauddin Zakariya University Multan, 60800, Pakistan.
J Ethnopharmacol. 2021 May 10;271:113805. doi: 10.1016/j.jep.2021.113805. Epub 2021 Jan 16.
Syzygium cumini (L.) Skeels is an important medicinal plant utilized in the health care systems of Pakistan, India, Sri Lanka, and Bangladesh. S. cumini have been used to treat renal issues, indigestion, diabetes, dysentery, and employed in folk medicine to treat inflammations. It is known to anticipate antioxidant, anti-inflammatory, anticancer, anti-diabetic, anti-bacterial, antifungal, activities, and radioprotective activities.
We examined the in vitro anti-inflammatory activities of S. cumini fruit extracts, evaluated using membrane stabilization, egg albumin denaturation, and bovine serum albumin denaturation assays. In vivo anti-inflammatory activity was also assessed, using murine models of carrageenan, formaldehyde, and PGE induced paw edema. Fractionation of active extracts was performed using HPLC, followed by LC-ESI-MS/MS analysis to identify the bioactive compounds responsible for anti-inflammatory activity.
The crude methanolic extract showed stronger in vitro and in vivo anti-inflammatory activities compared to other extracts. The most potent effects were observed in the formaldehyde induced paw edema assay wherein methanolic extract and standard indomethacin induced 72% and 88% inhibition against paw edema volume in comparison to control (normal saline) respectively. In the bovine serum albumin denaturation assay the methanolic extract induced 82% inhibition against denaturation as compared to control (phosphate buffer) while standard diclofenac sodium induced 98% inhibition. In contrast, 50% v/v MeOH:HO or 100% dichloromethane extracts displayed moderate to weak effects in the anti-inflammatory models. HPLC fractionation provided 6 active sub-fractions, four (MF2, MF3, MF6, MF7) from the 100% methanolic extract and two (HAF1, HAF3) from the 50% methanolic extract. The MF2, MF7, and HAF1 sub-fractions displayed potent activity in all studied in vitro assays. LC-ESI-MS-MS analysis tentatively identified delphinidin 3-glucoside, peonidin-3,5-diglucoside, gallic acid, liquitrigenin, scopoletin, umbelliferon, and rosmanol from the 100% methanolic fractions. Myricetin, catechin, quinic acid, chlorogenic acid, ellagic acid, gallic acid, and caffeic acid were identified in the 50% methanolic fractions.
These results demonstrate that S. cumini fruit extracts are a rich source of bioactive compounds that are worthy of further investigation as leads for anti-inflammatory drug discovery.
Syzygium cumini(L.)Skeels 是一种重要的药用植物,在巴基斯坦、印度、斯里兰卡和孟加拉国的医疗保健系统中得到应用。S. cumini 被用于治疗肾脏问题、消化不良、糖尿病、痢疾,并在民间医学中用于治疗炎症。它已知具有抗氧化、抗炎、抗癌、抗糖尿病、抗菌、抗真菌活性以及放射防护活性。
我们检查了 S. cumini 果实提取物的体外抗炎活性,使用膜稳定性、卵清蛋白变性和牛血清白蛋白变性测定进行评估。还使用角叉菜胶、甲醛和 PGE 诱导的爪肿胀的小鼠模型评估了体内抗炎活性。使用 HPLC 对活性提取物进行分级,然后使用 LC-ESI-MS/MS 分析鉴定负责抗炎活性的生物活性化合物。
与其他提取物相比,粗甲醇提取物显示出更强的体外和体内抗炎活性。在甲醛诱导的爪肿胀测定中观察到最强的效果,其中甲醇提取物和标准吲哚美辛分别诱导 72%和 88%的抑制作用,与对照(生理盐水)相比。在牛血清白蛋白变性测定中,甲醇提取物诱导 82%的变性抑制作用,与对照(磷酸盐缓冲液)相比,而标准双氯芬酸钠诱导 98%的抑制作用。相比之下,50%v/v MeOH:HO 或 100%二氯甲烷提取物在抗炎模型中显示出中等至弱的作用。HPLC 分级提供了 6 个活性亚级分,其中 4 个(MF2、MF3、MF6、MF7)来自 100%甲醇提取物,2 个(HAF1、HAF3)来自 50%甲醇提取物。MF2、MF7 和 HAF1 亚级分在所有研究的体外测定中均显示出强大的活性。LC-ESI-MS-MS 分析推测从 100%甲醇级分中鉴定出矢车菊素 3-葡萄糖苷、芍药素-3,5-二葡萄糖苷、没食子酸、甘草素、伞形花内酯、独活素和罗斯马林。在 50%甲醇级分中鉴定出杨梅素、儿茶素、奎宁酸、绿原酸、鞣花酸、没食子酸和咖啡酸。
这些结果表明,S. cumini 果实提取物是生物活性化合物的丰富来源,值得进一步研究,作为抗炎药物发现的先导化合物。