State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, 210009, China.
J Nat Med. 2013 Oct;67(4):856-61. doi: 10.1007/s11418-013-0745-4. Epub 2013 Jan 29.
Two new compounds, (2R)-7,3'-dihydroxy-6,4'-methoxyflavan (1) and (3R)-7,4'-dihydroxy-2'-methoxyisoflavan (2), along with 12 known flavonoids (3-14), were isolated from the vine stems of Millettia nitida var. hirsutissima. The structures of the isolated compounds were elucidated based on spectroscopic analyses and comparison of literature data. All of the isolates were evaluated for their effects on in-vitro anticoagulative assay and on nitric oxide (NO) production in lipopolysaccharide (LPS)-activated RAW264.7 macrophages. As a result, all compounds showed weak antiplatelet aggregation activities and compounds 4, 5, 7, 8 and 9 demonstrated antithrombin activity with a good dose-effect relationship from 5 to 100 μg mL⁻¹ in rabbit plasma. Compounds 8, 9, 10 and 14 exhibited inhibitory effects on LPS-induced NO production in RAW264.7 macrophages with IC₅₀ values of 4.79 ± 0.20, 8.23 ± 0.35, 5.23 ± 0.11 and 6.30 ± 0.30 μg mL⁻¹, respectively.
从密花豆的藤茎中分离得到了两个新化合物（2R）-7,3'-二羟基-6,4'-甲氧基黄烷（1）和（3R）-7,4'-二羟基-2'-甲氧基异黄酮（2），以及 12 个已知的类黄酮（3-14）。通过光谱分析和文献数据比较，确定了分离得到的化合物的结构。对所有分离得到的化合物进行了体外抗凝活性和脂多糖（LPS）激活的 RAW264.7 巨噬细胞中一氧化氮（NO）产生的抑制作用评价。结果表明，所有化合物均表现出较弱的抗血小板聚集活性，化合物 4、5、7、8 和 9 在 5 至 100 μg mL⁻¹浓度范围内对兔血浆中的抗凝血酶活性呈良好的剂量效应关系。化合物 8、9、10 和 14 对 LPS 诱导的 RAW264.7 巨噬细胞中 NO 产生具有抑制作用，IC₅₀值分别为 4.79 ± 0.20、8.23 ± 0.35、5.23 ± 0.11 和 6.30 ± 0.30 μg mL⁻¹。
