Department of Pharmacognosy, Faculty of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Pharmacognosy, College of Pharmacy, Mansoura University, El-Mansoura 35516, Egypt.
Molecules. 2018 Jul 28;23(8):1892. doi: 10.3390/molecules23081892.
Extensive phytochemical analysis of different root fractions of Courb. (Euphorbiaceae) has resulted in the isolation and identification of 22 secondary metabolites. 6-hydroxy-8-methoxycoumarin-7--β-d-glycopyranoside () and 2-hydroxymethyl -methyltryptamine () were isolated and identified as new compounds along with the known diterpenoid (, , , and ), triterpenoid ( and ), flavonoid (, , , , and ), coumarinolignan (⁻), coumarin (), pyrimidine (), indole (, ), and tyramine-derived molecules (⁻). The anti-inflammatory, analgesic, and antipyretic activities were evaluated for fifteen of the adequately available isolated compounds (⁻, ⁻, , , , , and ). Seven (, , , , , and of the tested compounds showed a significant analgesic effect ranging from 40% to 80% at 10 mg/kg in two in vivo models. Compound could also prove its analgesic property (67.21%) when it was evaluated on a third in vivo model at the same dose. The in vitro anti-inflammatory activity was also recorded where all compounds showed the ability to scavenge nitric oxide (NO) radical in a dose-dependent manner. However, eight compounds (, , , , , , , and ) out of the fifteen tested compounds exhibited considerable in vivo anti-inflammatory activity which reached 64.91% for compound at a dose of 10 mg/kg. Moreover, the tested compounds exhibited an antipyretic effect in a yeast-induced hyperthermia in mice. The activity was found to be highly pronounced with compounds , , , , , and which decreased the rectal temperature to about 37 °C after 2 h of the induced hyperthermia (~39 °C) at a dose of 10 mg/kg. This study could provide scientific evidence for the traditional use of as an anti-inflammatory, analgesic, and antipyretic.
对 Courb.（大戟科）不同根部分的广泛植物化学分析导致了 22 种次生代谢物的分离和鉴定。6-羟基-8-甲氧基香豆素-7--β-d-吡喃葡萄糖苷（）和 2-羟甲基-甲基色胺（）被分离并鉴定为新化合物，以及已知的二萜（，，，和），三萜（和），类黄酮（，，，，和），香豆素木脂素（⁻），香豆素（），嘧啶（），吲哚（，）和酪氨酸衍生分子（⁻）。对十五种充分可用的分离化合物（⁻，⁻，，，，和）进行了抗炎、镇痛和退热活性评价。在所测试的化合物中，有七种（，，，，，和）在两种体内模型中，在 10mg/kg 时表现出 40%至 80%的显著镇痛作用。在相同剂量下，化合物也在第三个体内模型中证明了其镇痛作用（67.21%）。体外抗炎活性也有记录，所有化合物均表现出以剂量依赖方式清除一氧化氮（NO）自由基的能力。然而，在所测试的 15 种化合物中，有八种（，，，，，，，和）化合物表现出相当大的体内抗炎活性，化合物在 10mg/kg 剂量下达到 64.91%。此外，所测试的化合物在酵母诱导的发热的小鼠中表现出退热作用。在诱导发热（约 39°C）后 2 小时，在 10mg/kg 剂量下，化合物、、、、、和可将直肠温度降低到约 37°C，活性非常显著。本研究可为作为抗炎、镇痛和退热的传统用途提供科学依据。
