Abstract
The dried vine stems of Spatholobus suberectus are commonly used in traditional Chinese medicine for treating gynecological and cardiovascular diseases. In this study, five new compounds named spasuberol A (2), homovanillyl-4-oxo-nonanoate (5), spasuberol C (6), spasuberoside A (14), and spasuberoside B (15), together with ten known compounds (1, 3, 4, 7–13), were isolated from the dried vine stems of S. suberectus. Their chemical structures were analyzed using spectroscopic assays. This is the first study interpreting the detailed structural information of 4. The anti-inflammatory activity of these compounds was evaluated by reducing nitric oxide overproduction in RAW264.7 macrophages stimulated by lipopolysaccharide. Compounds 1 and 8–10 showed strong inhibitory activity with half maximal inhibitory concentration (IC50) values of 5.69, 16.34, 16.87, and 6.78 μM, respectively, exhibiting higher activity than the positive drug l-N6-(1-iminoethyl)-lysine (l-NIL) with an IC50 value of 19.08 μM. The IC50 values of inhibitory activity of compounds 2 and 4–6 were 46.26, 40.05, 45.87, and 28.29 μM respectively, which were lower than l-NIL, but better than that of positive drug indomethacin with an IC50 value of 55.44 μM. Quantitative real-time polymerase chain reaction analysis revealed that assayed compounds with good anti-inflammatory activity, such as 1, 6, 9, and 10 at different concentrations, can reduce the messenger RNA (mRNA) expression of some pro-inflammatory cytokines such as tumor necrosis factor α (TNF-α), nitric oxide synthase (iNOS), and cyclooxygenase 2 (COX-2). The anti-inflammatory activity and the possible mechanism of the compounds mentioned in this paper were studied preliminarily.
Highlights
Spatholobi caulis (SPC), belonging to family Leguminosae, is the dried vine stem of Spatholobus suberectus Dunn, distributed in Fujian Province and the Guangxi Zhuang autonomous region of China
On the basis of the current struggle to discover more natural products as valuable resources for lead compounds for drug and pesticide design, the present study aims to identify more anti-inflammatory compounds in SPC, and further investigate the possible mechanism of nitric oxide (NO) inhibitory action of these isolated compounds using real-time quantitative polymerase chain reaction
Fr.1C was subjected to silica gel column chromatography (SGCC) to get three fractions (Fr.1C1–3) with CHCl3-MeOH (40:1, v/v) as the elution phase, and compound 3 was isolated from Fr.1C3 using MeCN-H2 O (35:65, v/v, 8 mL/min) as the elution that flowed through RPSP-HPLC
Summary
Spatholobi caulis (SPC), belonging to family Leguminosae, is the dried vine stem of Spatholobus suberectus Dunn, distributed in Fujian Province and the Guangxi Zhuang autonomous region of China. SPC is an important ingredient of traditional Chinese medicine (TCM) recorded in the Pharmacopoeia of the People’s Republic of China [1], with demonstrated blood-activating and stasis-dissolving efficacy. In clinical practice, it is always used for treating rheumatic arthralgia, irregular menstruation, and paralysis in many Chinese formulas such as Jinkui Shenqi pills and Fukeqianjin. On the basis of the current struggle to discover more natural products as valuable resources for lead compounds for drug and pesticide design, the present study aims to identify more anti-inflammatory compounds in SPC, and further investigate the possible mechanism of NO inhibitory action of these isolated compounds using real-time quantitative polymerase chain reaction (qPCR)
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