The Center for Research on Botanical Dietary Supplements, Interdepartmental Graduate Program in Nutritional Sciences, Department of Food Science and Human Nutrition, Iowa State University, Ames, IA 50011, United States.
Phytochemistry. 2011 Nov;72(16):2015-23. doi: 10.1016/j.phytochem.2011.07.016. Epub 2011 Aug 17.
Hypericum perforatum (St. John's wort) is an herb widely used as supplement for mild to moderate depression. Our prior studies established synergistic anti-inflammatory activity associated with 4 bioactive compounds in a fraction of a H. perforatum ethanol extract. Whether these 4 compounds also contributed to the ethanol extract activity was addressed in the research reported here. Despite the popularity of H. perforatum, other Hypericum species with different phytochemical profiles could have their anti-inflammatory potentials attributed to these or other compounds. In the current study, ethanol extracts of different Hypericum species were compared for their inhibitory effect on LPS-induced prostaglandin E2 (PGE2) and nitric oxide (NO) production in RAW 264.7 mouse macrophages. Among these extracts, those made from H. perforatum and H. gentianoides demonstrated stronger overall efficacy. LC-MS analysis established the 4 compounds were present in the H. perforatum extract and pseudohypericin in all active fractions. The 4 compounds accounted for a significant part of the extract's inhibitory activity on PGE2, NO, tumor necrosis factor-α (TNF-α), and interleukin-1β (IL-1β) in RAW 264.7 as well as peritoneal macrophages. Pseudohypericin was the most important contributor of the anti-inflammatory potential among the 4 compounds. The lipophilic fractions of H. gentianoides extract, which did not contain the previously identified active constituents, decreased PGE2 and NO potently. These fractions were rich in acylphloroglucinols, including uliginosin A that accounted for a proportion of the anti-inflammatory activity observed with the active fractions. Overall, the current study established that a different group of major anti-inflammatory constituents were present in H. gentianoides, while showing that the previously identified 4 compound combination was important for H. perforatum's anti-inflammatory potential.
贯叶金丝桃（贯叶连翘）是一种被广泛用作轻度至中度抑郁症补充剂的草药。我们之前的研究确定了在贯叶金丝桃乙醇提取物的一个部分中与 4 种生物活性化合物相关的协同抗炎活性。在本研究中，研究了这些 4 种化合物是否也对乙醇提取物的活性有贡献。尽管贯叶金丝桃很受欢迎，但具有不同植物化学特征的其他金丝桃属植物的抗炎潜力可能归因于这些或其他化合物。在当前的研究中，比较了不同金丝桃属植物的乙醇提取物对 LPS 诱导的 RAW 264.7 小鼠巨噬细胞中前列腺素 E2（PGE2）和一氧化氮（NO）产生的抑制作用。在这些提取物中，来自贯叶金丝桃和金丝桃的提取物表现出更强的整体功效。LC-MS 分析确定 4 种化合物存在于贯叶金丝桃提取物中，伪金丝桃素存在于所有活性部分中。4 种化合物在 RAW 264.7 及腹腔巨噬细胞中对 PGE2、NO、肿瘤坏死因子-α（TNF-α）和白细胞介素-1β（IL-1β）的抑制活性占提取物的很大一部分。伪金丝桃素是 4 种化合物中抗炎潜力的最重要贡献者。金丝桃属植物提取物的亲脂部分不含先前鉴定的活性成分，但能强烈降低 PGE2 和 NO。这些部分富含酰基间苯三酚，其中包括 uliginosin A，它占活性部分观察到的抗炎活性的一部分。总体而言，本研究确定了金丝桃属植物中存在不同的主要抗炎成分，同时表明先前鉴定的 4 种化合物组合对贯叶金丝桃的抗炎潜力很重要。
