Division of Ethnopharmacology, Entomology Research Institute, Loyola College (University of Madras), Chennai, Tamil Nadu, 600034, India.
GLR Laboratories Private Limited, Mathur, Chennai, 600068, India.
J Ethnopharmacol. 2019 Dec 5;245:112170. doi: 10.1016/j.jep.2019.112170. Epub 2019 Aug 18.
The interest on herbal health supplements for obesity is increasing globally. Our previous ethnobotanical survey in Tiruvallur district, Tamil Nadu, India indicated the use of Spermacoce hispida L. seeds for the treatment of obesity.
This study was aimed to validate the traditional claim and to identify the antihyperlipidemic principle in the seeds of Spermacoce hispida using bioassay guided fractionation method.
Bioassay monitored fractionation of the aqueous extract from Spermacoce hispida seeds was carried out using triton WR 1339 induced hyperlipidemic animals. It yielded deacetylasperulosidic acid (DAA) as the active ingredient. Pharmacokinetic properties of DAA were predicted using DataWarrior and SwissADME tools. In vitro antiobesity and antihyperlipidemic effects of DAA were evaluated in 3T3L1 preadipocytes and HepG2 cells, respectively. The chronic antihyperlipidemic efficacy of DAA was evaluated in high fat diet fed rats.
DAA did not show any mutagenic and tumorigenic properties. It bound with PPARα with comparable ligand efficiency as fenofibrate. The treatment with DAA significantly lowered the proliferation of matured adipocytes, but not preadipocytes. The treatment of steatotic HepG2 cells with DAA significantly decreased the LDH leakage by 43.03% (P < 0.05) at 50 μM concentration. In triton WR 1339 induced hyperlipidemic animals, the treatment with 50 mg/kg dose significantly lowered the TC, TG and LDL-c levels by 40.27, 46.00 and 63.65% respectively. In HFD fed animals, the treatment at 10 mg/kg decreased BMI and AC/TC ratio without altering SRBG. It also improved serum lipid, transaminases and phosphatases levels of HFD fed animals. The treatment lowered adipocyte hypertrophy and steatosis of hepatocytes.
This preliminary report supported the traditional use of Spermacoce hispida for the treatment of obesity. Further detailed investigations on the long term safety, efficacy and molecular mode of action of Spermacoce hispida and DAA will throw more light on their usefulness for the management of obesity.
全球范围内，人们对草药保健品治疗肥胖的兴趣日益增加。我们之前在印度泰米尔纳德邦蒂鲁瓦卢尔区进行的民族植物学调查表明，使用了水蜈蚣 Spermacoce hispida L. 的种子来治疗肥胖症。
本研究旨在验证传统说法，并使用基于生物测定的分离方法确定 Spermacoce hispida 种子中的抗高血脂原理。
使用 Triton WR 1339 诱导的高脂血症动物监测水蜈蚣种子水提物的生物测定导向分离，得到了去乙酰asperulosidic 酸 (DAA) 作为有效成分。使用 DataWarrior 和 SwissADME 工具预测 DAA 的药代动力学性质。在 3T3L1 前脂肪细胞和 HepG2 细胞中分别评估 DAA 的体外抗肥胖和抗高血脂作用。在高脂肪饮食喂养的大鼠中评估 DAA 的慢性抗高血脂疗效。
DAA 没有显示出任何致突变和致癌特性。它与 PPARα 结合的配体效率与非诺贝特相当。DAA 治疗显著降低成熟脂肪细胞的增殖，但对前脂肪细胞没有影响。用 DAA 处理脂肪变性的 HepG2 细胞可使 LDH 漏出量显著降低 43.03%（P < 0.05），浓度为 50 µM。在 Triton WR 1339 诱导的高脂血症动物中，用 50 mg/kg 剂量治疗可使 TC、TG 和 LDL-c 水平分别降低 40.27%、46.00%和 63.65%。在 HFD 喂养的动物中，用 10 mg/kg 剂量治疗可降低 BMI 和 AC/TC 比值，而不改变 SRBG。它还改善了 HFD 喂养动物的血清脂质、转氨酶和磷酸酶水平。治疗降低了脂肪细胞肥大和肝细胞脂肪变性。
本初步报告支持使用水蜈蚣治疗肥胖症的传统用途。对 Spermacoce hispida 和 DAA 的长期安全性、疗效和分子作用模式进行更详细的研究，将为它们在肥胖症管理中的应用提供更多的依据。
