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Objective To observe the effects of different doses of Sappan Lignum and Chuanxiong Rhizoma on tumor stem cells marker ABCG2 in vivo. Methods Sphere cells obtained from serum culture were inoculated in nude mouse armpit, which were randomly divided into 5 groups: control group, Sappan Lignum high- and low-dose groups, and Chuanxiong Rhizoma high- and low-dose groups. Each medication group was given relevant medicine for gavage. 21 days later, inhibition tumor rate and ABCG2 protein and mRNA expression were detected with confocal microscope, Western blot, and RT-PCR. Results The sphere cells obtained from serum free culture had the abilities of cancer stem cells, such as proliferation, anti-aptosis and high expression of cancer stem cells markers. Chuanxiong Rhizoma high- and low-dose groups could inhibit tumor growth (P0.05). Compared with the control group, Chuanxiong Rhizoma low-dose group could significantly inhibit the expression of resistant protein of ABCG2. Sappan Lignum high- and low-dose groups could not inhibit the protein expression of ABCG2. Each medication group up-regulated the mRNA expression of ABCG2 except for Chuanxiong Rhizoma low-dose group. Conclusion Low dose of Chuanxiong Rhizoma can inhibit the expression of ABCG2 protein levels, which can be the targeting killer for cancer stem cells.
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Objective: To study the chemical constituents in Sappan Lignum (the core material of Caesalpinia sappan). Methods: The chemical constituents of Sappan Lignum were isolated by different column chromatographic techniques, including silica gel and Sephadex LH-20 columns. The structures of these compounds were identified by a comprehensive analysis on the spectroscopic data. Results: Fifteen compounds were isolated from the EtOAc extract of Sappan Lignum. The compounds were identified as protosappanin A (1), 3,7-dihydroxychroman-4-one (2), 7,3',4'-trihydroxy-3-benzyl-2H-chromene (3), bonducellin (4), 3'-deoxysappanol (5), 3'-deoxy-4-O-methylepisappanol (6), 3-deoxysappanchalcone (7), 3,8,9-thihydroxy-6H-benzo[c] chromen- 6-one (8), 3,9-dihydroxy-8-methoxydibenzo [b, d] pyran-6-one (9), (-)-syringaresinol (10), dibutyl phthalate (11), β-sitosterol (12), β-daucosterol (13), stigmasterol (14), and 1-heneicosanol (15). Conclusion: Compounds 9, 11, and 12 are first isolated from the plants of Caesalpinia Linn. and compound 4 is first isolated from this plant.
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Objective: To investigate, purify, and characterize the active ingredients in the aqueous extract from Sappan Lignum (the dry heartwood of Caesalpinia sappan). Methods: HPLC-MS/MS was used in the analysis of the chemical constituents in the aqueous extract from Sappan Lignum. Then the inhibitory effect of the aqueous extract from Sappan Lignum on human bladder tumor cell line T24 in vitro was studied. The main chemical constituents were purified by column chromatography and their structures were characterized by NMR. Results: In the aqueous extract from Sappan Lignum, 16 compounds were separated and detected well by HPLC-MS/MS and 14 were identified. The main compounds were quercetin, brazilin, isoliquiritigeni, protosappanin B, brazil A, 3'-deoxysappanol, 4-O-hydroxybrazilin, sappanchalcone, and (αS)-α, 2', 4, 4'-tetrahydroxy dihydrochalcone. The killing rate of cancer cells was positively correlated to the concentration of the main component which was brazilin. At last, according to the purification by column chromatography and the structural characterization by NMR, we obtained the pure brazilin in the aqueous extract from Sappan Lignum. Conclusion: The research offers a new method for the identification of the components in the aqueous extract from Sappan Lignum and provides a basis for the medicinal functions of Sappan Lignum for future study.
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Objective To develop a reversed phase high performance liquid Chromatographie (RP-HPLC) analysis system for hydroxysafflor yellow A (HSYA) in rat model of cold coagulation and blood stasis (CCBS), and to investigate the influence of Sappan lignum on the pharmacokinetics of HSYA in CCBS rats. Methods Rat CCBS models were randomly divided into two groups with each containing 6 animals. Rats were orally given Carthami flos extract or Carthami flos extract combined with Sappan lignum (The dosage: 20. 0 g/kg crud drug of Carthami flos). Plasma samples were collected in heparinized tubes from the oculi chorioideae vein at 5, 10, 20, 30, 45, 60, 90, 120, 150, 210, and 270 min after drug administration; and the plasma proteins were precipitated with 20% trichloroacetic acid aqueous solution. Plasma concentrations of HSYA were detected by RP-HPLC at different time points after drug administration. The data were processed by DAS 2. 0 software to calculate the pharmacokinetic parameters. Results Compared with the Carthami flos group, the pharmacokinetic parameters V1/F and CL/ Fof HSYA in the Carthami flos combined with Sappan lignum group were significantly decreased (P<0. 01), and the AUCo-t, Cmax, and t1/2α of HSYA were significantly increased (P<0. 01). Conclusion Sappan lignum can promote the absorption of HSYA in rat model of CCBS and reduce the distribution of HSYA, thus exercise an efficacy-enhancing effect.
ABSTRACT
Caesalpinia sappan (C. sappan) is a medicinal plant used for promoting blood circulation and removing stasis. During a screening procedure on medicinal plants, the ethylacetate extract of the lignum of C. sappan (CLE) showed inhibitory activity on arginase which has recently been reported as a novel therapeutic target for the treatment of cardiovascular diseases such as atherosclerosis. CLE inhibited arginase II activity prepared from kidney lysate in a dose-dependent manner. In HUVECs, inhibition of arginase activity by CLE reciprocally increased NOx production through enhancement of eNOS dimer stability without any significant changes in the protein levels of eNOS and arginase II expression. Furthermore, CLE-dependent arginase inhibition resulted in increase of NO generation and decrease of superoxide production on endothelium of isolated mice aorta. These results indicate that CLE augments NO production on endothelium through inhibition of arginase activity, and may imply their usefulness for the treatment of cardiovascular diseases associated with endothelial dysfunction.