For making use of Ginseng resources that exhibit an antitumor activity and for finding new anticancer drugs, three new fatty acid ester compounds： 3/β-acetoxy panaxadiol （ Ⅰ ）, 3β-palmitic acid aceloxy panaxadi...For making use of Ginseng resources that exhibit an antitumor activity and for finding new anticancer drugs, three new fatty acid ester compounds： 3/β-acetoxy panaxadiol （ Ⅰ ）, 3β-palmitic acid aceloxy panaxadiol （ Ⅱ ） , and 3β-octadecanoic acid aceloxy panaxadiol（ Ⅰ , Ⅱ, and m） were synthesized with panaxadiol, diacetyl oxide, palmityl chloride and stearyl chloride, and their structures were determined via MS, ^13C NMR, IR, TLC, and so on. The molar yields of the three compounds are 75.14%, 79. 08%, and 72. 57%, respectively. Meanwhile, the antitumor activity of the three new panaxadiol fatty acid ester derivatives and panaxadiol was compared by using the method of MTT. Tumor cell used was Vero cell line. Positive control was 5-FU, blank was an RPMI1640 culture medium, negative control was an RPMI1640 culture medium and the solvent for drugs to be tested. Compound Ⅰ has the strongest antitumor activity followed by panaxadiol; compounds Ⅱ and Ⅲ have similar and weakest antitumor activities. Furthermore, the antitumor activities of the panaxadiol fatty acid ester derivatives show positive correlation with the concentration of the test group, but show no relationship with the molecular weight of fatty acid. The methods that are used to synthesize the three compounds with high yields and strong antitumor activities are simple and show a great potential for meeting the needs of industrial manufacture of these drugs.展开更多
Objective To study the intestinal absorption and transepithelial transport of three limoninoids: evodol (EVO), limonin (LIM), and shihulimonin A (SHIA), isolated from Fructus Evodiae [the unripe fruit of Evodia rutaec...Objective To study the intestinal absorption and transepithelial transport of three limoninoids: evodol (EVO), limonin (LIM), and shihulimonin A (SHIA), isolated from Fructus Evodiae [the unripe fruit of Evodia rutaecarpa and Evodia rutaecarpa var. bodinieri] in the human intestine. Methods The in vitro cultured human colon carcinoma cell line, Caco-2 cell monolayer model, was applied to studying the absorption and transepithelial transport of the three limoninoids from apical (AP) to basolateral (BL) side and from BL to AP side. The three limoninoids were measured by reversed-phase high performance liquid chromatography coupled with ultraviolet absorption detector. Transport parameters and apparent permeability coefficients (Papp) were then calculated and compared with those of Propranolol as a control substance of high permeability and Atenolol as a control substance of poor permeability. Results The Papp value of EVO and LIM from AP to BL side for absorption and transport were 1.78 × 10-5 cm/s and 1.16 × 10-5 cm/s, respectively, which was comparable to that of Propranolol with Papp 2.18 × 10-5 cm/s. Conclusion The absorption and transport of both EVO and LIM are main passive diffusion as the dominating process in Caco-2 cell monolayer model, and they were estimated to be high absorbed compounds. SHIA in Caco-2 cell monolayer model may be involved in metabolism in the transport processes.展开更多
Saposhnikovia divaricata is a valuable Chinese medicinal herb; the transformation from vegetative growth to reproductive growth may lead to the decrease of its pharmacological activities. Therefore, the study of bolti...Saposhnikovia divaricata is a valuable Chinese medicinal herb; the transformation from vegetative growth to reproductive growth may lead to the decrease of its pharmacological activities. Therefore, the study of bolting and flowering for Saposhnikovia divaricata is warranted. The present study aimed to reveal differentially expressed genes(DEGs) and regularity of expression during the bolting and flowering process, and the results of this study might provide a theoretical foundation for the suppression of early bolting for future research and practical application. Three sample groups, early flowering, flower bud differentiation, and late flowering(groups A, B, and C, respectively) were selected. Transcriptomic analysis identified 67, 010 annotated unigenes, among which 50, 165 were differentially expressed including 16, 108 in A vs B, and 17, 459 in B vs C, respectively. Gene ontology(GO) and Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway functional classification analysis were performed on these differentially expressed genes, and five important pathways were significantly impacted(P ≤ 0.01): plant circadian rhythm, other glycan degradation, oxidative phosphorylation, plant hormone signal transduction, and starch and sucrose metabolism. Plant hormone signal transduction might play an important role in the bolting and flowering process. The differentially expressed indole-3-acetic acid(IAA) gene showed significant down-regulation during bolting and flowering, while the transport inhibitor response 1(TIR1) gene showed no significant change during the bolting process. The expression of flowering related genes FLC, LYF, and AP1 also showed a greater difference at different development stages. In conclusion, we speculate that the decrease in auxin concentration is not caused by the degrading effect of TIR1 but by an alternative mechanism.展开更多
基金the National Natural Science Foundation of China(No 30370159)
文摘For making use of Ginseng resources that exhibit an antitumor activity and for finding new anticancer drugs, three new fatty acid ester compounds： 3/β-acetoxy panaxadiol （ Ⅰ ）, 3β-palmitic acid aceloxy panaxadiol （ Ⅱ ） , and 3β-octadecanoic acid aceloxy panaxadiol（ Ⅰ , Ⅱ, and m） were synthesized with panaxadiol, diacetyl oxide, palmityl chloride and stearyl chloride, and their structures were determined via MS, ^13C NMR, IR, TLC, and so on. The molar yields of the three compounds are 75.14%, 79. 08%, and 72. 57%, respectively. Meanwhile, the antitumor activity of the three new panaxadiol fatty acid ester derivatives and panaxadiol was compared by using the method of MTT. Tumor cell used was Vero cell line. Positive control was 5-FU, blank was an RPMI1640 culture medium, negative control was an RPMI1640 culture medium and the solvent for drugs to be tested. Compound Ⅰ has the strongest antitumor activity followed by panaxadiol; compounds Ⅱ and Ⅲ have similar and weakest antitumor activities. Furthermore, the antitumor activities of the panaxadiol fatty acid ester derivatives show positive correlation with the concentration of the test group, but show no relationship with the molecular weight of fatty acid. The methods that are used to synthesize the three compounds with high yields and strong antitumor activities are simple and show a great potential for meeting the needs of industrial manufacture of these drugs.
基金supported partly by the Beijing Science Foundation (No. Z0004105040311)National High Technology Program (No. 2002AA2Z343C+2 种基金 No. 2004AA2Z3783)National Sciences and Technology Program (No. 2006BAI 06A01-02 No. 2006BAI08B03-09) of China
文摘Objective To study the intestinal absorption and transepithelial transport of three limoninoids: evodol (EVO), limonin (LIM), and shihulimonin A (SHIA), isolated from Fructus Evodiae [the unripe fruit of Evodia rutaecarpa and Evodia rutaecarpa var. bodinieri] in the human intestine. Methods The in vitro cultured human colon carcinoma cell line, Caco-2 cell monolayer model, was applied to studying the absorption and transepithelial transport of the three limoninoids from apical (AP) to basolateral (BL) side and from BL to AP side. The three limoninoids were measured by reversed-phase high performance liquid chromatography coupled with ultraviolet absorption detector. Transport parameters and apparent permeability coefficients (Papp) were then calculated and compared with those of Propranolol as a control substance of high permeability and Atenolol as a control substance of poor permeability. Results The Papp value of EVO and LIM from AP to BL side for absorption and transport were 1.78 × 10-5 cm/s and 1.16 × 10-5 cm/s, respectively, which was comparable to that of Propranolol with Papp 2.18 × 10-5 cm/s. Conclusion The absorption and transport of both EVO and LIM are main passive diffusion as the dominating process in Caco-2 cell monolayer model, and they were estimated to be high absorbed compounds. SHIA in Caco-2 cell monolayer model may be involved in metabolism in the transport processes.
基金supported by Chinese National Agro-scientific Research in the Public Interest(No.201303111)Traditional Chinese Medicine Standardization Construction of China(No.ZYBZH-Y-ZY-45) and (No.ZYBZH-C-GD-08)
文摘Saposhnikovia divaricata is a valuable Chinese medicinal herb; the transformation from vegetative growth to reproductive growth may lead to the decrease of its pharmacological activities. Therefore, the study of bolting and flowering for Saposhnikovia divaricata is warranted. The present study aimed to reveal differentially expressed genes(DEGs) and regularity of expression during the bolting and flowering process, and the results of this study might provide a theoretical foundation for the suppression of early bolting for future research and practical application. Three sample groups, early flowering, flower bud differentiation, and late flowering(groups A, B, and C, respectively) were selected. Transcriptomic analysis identified 67, 010 annotated unigenes, among which 50, 165 were differentially expressed including 16, 108 in A vs B, and 17, 459 in B vs C, respectively. Gene ontology(GO) and Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway functional classification analysis were performed on these differentially expressed genes, and five important pathways were significantly impacted(P ≤ 0.01): plant circadian rhythm, other glycan degradation, oxidative phosphorylation, plant hormone signal transduction, and starch and sucrose metabolism. Plant hormone signal transduction might play an important role in the bolting and flowering process. The differentially expressed indole-3-acetic acid(IAA) gene showed significant down-regulation during bolting and flowering, while the transport inhibitor response 1(TIR1) gene showed no significant change during the bolting process. The expression of flowering related genes FLC, LYF, and AP1 also showed a greater difference at different development stages. In conclusion, we speculate that the decrease in auxin concentration is not caused by the degrading effect of TIR1 but by an alternative mechanism.
