Flavonoids from Millettia nitida var. hirsutissima with their anticoagulative activities and inhibitory effects on NO pr
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Flavonoids from Millettia nitida var. hirsutissima with their anticoagulative activities and inhibitory effects on NO production Xiao-Lin Liao • Jian-Guang Luo • Ling-Yi Kong
Received: 30 October 2012 / Accepted: 15 January 2013 Ó The Japanese Society of Pharmacognosy and Springer Japan 2013
Abstract Two new compounds, (2R)-7,30 -dihydroxy-6,40 methoxyflavan (1) and (3R)-7,40 -dihydroxy-20 -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 lg 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 lg mL-1, respectively. Keywords Millettia nitida var. hirsutissima Leguminosae Flavonoids Antithrombin Antiplatelet aggregation RAW264.7 macrophages
provinces of South China, and has been used as a substitute for the traditional Chinese medicine Ji-Xue-Teng (the vine stems of Spatholobus suberectus) for thousands of years. It has been used to treat blood stasis syndromes including anemia, menoxenia, inflammation of peripheral blood vessels and thrombotic changes in vessels by promoting blood circulation and also to treat rheumatic arthritis [1–3]. Previous chemical investigations on this plant have identified flavonoids as major components, which are also responsible for the pharmacological properties of this medicinal herb [4]. Flavonoids demonstrate a significant potential as new pharmacological agents [5, 6]. Recently, some flavonoids have been reported to exert anticoagulative and anti-inflammatory activities [6, 7]. In order to further clarify the actual bioactive components of this medicinal plant, the present investigation was focused on the isolation and bioactivity of the flavonoids in the vine stems of M. nitida var. hirsutissima. As a result, a new flavan (1) and a new isoflavan (2) were isolated, along with 12 known flavonoids (3–14). Furthermore, the anticoagulative activities of the isolates were investigated by using platelet aggregation and thrombin time (TT) methods, and the inhibitory effects of the isolates on NO production in LPS-induced RAW264.7 macrophages were also evaluated.
Introduction Millettia nitida var. hirsutissima (Leguminosae) is a perennial herb distributed in Jiangxi, Fujian and Guangxi
Results and discussion Chemistry
X.-L. Liao J.-G. Luo L.-Y. Kong (&) State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China
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