The antiangiogenic activity of Kushecarpin D, a novel flavonoid isolated from Sophora flavescens Ait.

AIMS: Kushecarpin D (KD) is a novel flavonoid isolated from the traditional Chinese herbal medicine Kushen (the dried root of Sophora flavescens Ait). As part of our continuous effort to explore Chinese traditional medicinal herbs and to identify novel natural anticancer products, the antiangiogenic properties of KD were examined in vitro using a human umbilical vein endothelial cell line (ECV304). MAIN METHODS: The SRB and Trypan Blue exclusion assays were used to evaluate the effect of KD on cell proliferation. The antiangiogenic activities of KD were evaluated through studies of cell migration, cell adhesion, and tube formation. DCFH-DA and DHE fluorescent assays were used to detect the reactive oxygen species (ROS) levels. Catalase activity was detected using the colorimetric ammonium molybdate method. Cell cycle and apoptosis were measured using flow cytometry and the Hoechst 33258 staining assay. KEY FINDINGS: The results indicated that KD showed antiangiogenic activity via inhibitory effects on cell proliferation, cell migration, cell adhesion, and tube formation. ROS levels were down-regulated and catalase activity was up-regulated after treatment with KD. The cell cycle was arrested at the G2/M phase, while no apoptosis was observed using the Hoechst 33258 staining assay or following the flow cytometric analysis of the sub-G1 proportion. SIGNIFICANCE: The antiangiogenic properties of KD, in combination with its anti-proliferative effect and ability to induce cell cycle arrest without inducing apoptosis, make it a good candidate for development as antitumor agent. However, further studies are essential to elucidate its mechanism of action.

A novel flavonoid isolated from Sophora flavescens exhibited anti-angiogenesis activity, decreased VEGF expression and caused G0/G1 cell cycle arrest in vitro.

Kushen, the dried root of Sophora flavescens Ait, is a traditional Chinese herbal medicine. Kushen alkaloids have been developed in China as anticancer drugs, and more potent antitumor activities have been identified in kushen flavonoids than in kushen alkaloids. In this study, the anti-angiogenic properties of (2S)-7,2',4'-triihydroxy-5-methoxy-8-dimethylallyl flavanone (Compound 1, a novel flavonoid isolated from Kushen), were examined using the human umbilical vein endothelial cell line (ECV304) in vitro. The results indicated that compound 1 shows anti-angiogenesis activity via inhibitory effects on cell proliferation, cell migration, cell adhesion, and tube formation. Further studies indicated that compound 1 blocks cell cycles in the G0/G1 phase without inducing apoptosis, and down regulates vascular endothelial growth factor (VEGF) expression. The free radical scavenging activity of compound 1 was found through 2',7'-dichlorofluorescin diacetate (DCFH-DA) incubation assay in cells. The anti-angiogenic properties of compound 1 and its antiproliferative effect on endothelial cells without causing apoptosis make it a good candidate for development as a agent against development of tumors.

Alkaloids from Sophora flavescens Aition.

Although the quinolizidine alkaloids and flavonoids, the main active components of the traditional Chinese medicine Sophora flavescens, have been largely investigated, a new matrine alkaloid derivative 9alpha-hydroxy-7,11-dehydromatrine (1) and a rare 1,4-diazaindan-type alkaloid flavascensine (17), together with 15 known alkaloids, were isolated from S. flavescens. The structures were established on the basis of spectroscopic techniques.

Limonoids from the root of Dictamnus radicis cortex.

Chemical investigation of the roots of Dictamnus radicis Cortex led to the isolation of a new limonoid isodictamdiol (1) and a known dictamdiol (2), the first 5S/9S-type degraded limonoids, together with other six known limonoids (3-8). The chemical structures were identified on the basis of modern spectroscopic methods, including IR, MS, NMR ((1)H-NMR, (13)C-NMR, (1)H-(1)H COSY, HMQC, HMBC, NOESY). Additionally, the absolute configurations of limonoid isodictamdiol (1) and dictamdiol (2) were separately elucidated by single crystal X-ray diffraction, as well as their circular dichroism spectra. Furthermore, all compounds were evaluated for antibacterial activity against three bacterial cultures.

Antibacterial constituents from Pedicularis armata.

A new neolignan glycoside named armaoside (1), together with six known compounds (2-7), have been isolated from the whole plant of Pedicularis armata Maxim. The structure of 1 was elucidated as erythro-(7S,8R)-1-(4-O-beta-D-glucopyranosyl-3-methoxyphenyl)-2-[3,5-dimethoxyl-4-oxo-cinnamic aldehyde]propane-1, 3-diol by spectroscopic and chemical methods. All compounds were assayed against Bacillus subtilis, Escherichia coli, and Staphylococcus aureus.