Terpenoids from leaves of Chinese hawthorn / 中国中药杂志

Fifteen compounds were isolated from the 70% EtOH extract of leaves of Chinese hawthorn(Crataegus pinnatifida var. major) by various purification steps, and their structures were determined as 2α,3α,12β,19α,-tetrahydroxyursan-13β,28-olide(1),euscaphic acid(2), tormentic acid(3), ursolic acid(4), pomolic acid(5), corosolic acid(6), maslinic acid(7), linalyl rutinoside(8),(Z)-3-hexenyl β-D-glucoside(9),(3S, 6S)-cis-linalool-3,7-oxide-β-D-glucopyranoside(10), pisumionoside(11), icariside B6(12), byzantionoside B(13),(6R,7E,9R)-9-Hydroxy-4,7-megastigmadien-3-one 9-O-β-D-glucopyranoside(14) and(6S,7E,9R)-6,9-dihydroxy-4,7-megastigmadien-3-one 9-O-β-D-glucopyranoside(15) mainly based on the mass spectrum(MS) and nuclear magnetic resonance(NMR) spectroscopic techniques, of which compound 1 was a new pentacyclic triterpene, and compounds 2, 5, 6, 8, 10, 13 and 15 were isolated form this plant for the first time.

A new triterpenoid saponin from leaves of Panax japonicas var. major / 中草药

Objective: To study the chemical composition from the leaves of Panax japonicus var. major. Methods: Column chromatographies (including macroporous resin, silica gel, Sephadex LH-20 and ODS) and semi-preparative HPLC were used to separate the constituents. The structures were elucidated by the analysis of spectral data and chemical properties. Results: Three compounds were isolated and elucidated as dammar-20(21),24-diene-3β,6α,12β-triol (1), dammar-20(22) Z,24-diene-3β,6α,12β-triol (2), and 3-O-[-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl]-20-O-[-β-D-xylopyranosyl-(1→6)-β-D-glucopyranosyl]-23E,25-diene- 20(S)-protopanoxadiol (3). Conclusion: Compound 1 and 2 was obtained from the plant for the first time. And compound 3 named as majoroside Z is a new triterpenoid saponin.

Study on antitumor activity of triterpenoid saponins from Tujia ethnomedicine Kouziqi / 中草药

Objective: To study the active triterpenoid saponins of Tujia ethnomedicine Kouziqi (Panax japonicus var. major). The antitumor activity was screened and the relationship between the structure and activity of the compounds was discussed. Methods: The ethanol extract of Kouziqi was isolated by Silica gel, ODS and MCI column chromatograph and purified by preparative HPLC. The structures were elucidated on the basis of spectroscopic analysis and compared with literatures. Using MTT assay to detect the cytotoxicity of 14 compounds in BGC-823, HCT-116, Hela, HepG-2 cells. Results: A total of 14 known compounds were isolated from Tujia ethnomedicine Kouziqi and determined as chikusetsusaponin IVa methyl ester (1), chikusetsusaponin IVa butyl ester (2), chikusetsusaponin IV (3), chikusetsusaponin IVa (4), 28-desglucosylchikusetsusaponin IVa (5), oleanolic acid-3-O-β-D-(6'- methylester)-glucuronopyranoside (6), (24R)-majonoside R1 (7), (24R)-pseudoginsinoside F11 (8), (20S)-notoginsinoside-R2 (9), (20S)-ginsenoside Rg2 (10), ginsenoside Rg1 (11), ginsenoside Re (12), ginsenoside Rd (13) and chikusetsusaponin-V methyl ester (14). Among the 14 compounds, compounds 5 and 6 showed dose-dependent cytotoxicity to BGC-823, HCT-116, Hela and HepG-2 cells. Compound 5 had cytotoxicity in BGC-823 and HCT-116 cells with IC50 values of 9.94 and 14.17 μmol/L, respectively. Compound 6 had the best cytotoxicity in HepG-2 cells with IC50 value of 12.70 μmol/L. Conclusion: Compound 6 is isolated from Kouziqi for the first time and its spectral data were reported. The antineoplastic activity of Tujia ethnomedicine Kouziqi is based on the oleanolic acid-type triterpenoid saponins and related to the substituents of C-28, but the mechanism still needs to be deeply studied.

Effects of shading on key enzyme genesexpression and accumulation of saponins in Panax japonicus var. major / 中国中药杂志

To explore the effects of shading and the expression of key enzyme genes on the synthesis and accumulation of Panax japonicus var. major saponins, different shading treatments (0%, 30%,50%) of potted P. japonicus var. major were used as test materials, the expression of three key enzyme genes(CAS,DS,-AS) of leaves and rhizomes in different growth periods of P. japonicus var. major was determined by real-time quantitative PCR, the content of total saponins was determined by ultraviolet spectrophotometry. The results indicated that, in flowering stage, CAS,DS,-AS were highly expressed in the aerial parts of P. japonicus var. major, 30% shading treatment significantly inhibited the expression of CAS in leaves and promoted the expression of DS and -AS in stems, leaves and flowers, it was speculated that the main part of saponin synthesis was leaf in this stage. Both the expression levels of DS and -AS and changes in the content of total saponins in leaves showed a tendency of low-high-low throughout the growth cycle, correlation coefficient analysis showed that there was a positive correlation between them. Compared with control, the expression levels of DS and -AS and the content of total saponins were greatly enhanced under shading treatment, 30% shading treatment significantly promoted the accumulation of total saponins. Therefore, it is suggested that 30% shading treatment should be applied to the artificial cultivation of P. japonicus var. major, which is beneficial to the accumulation and quality improvement of saponins.

Apoptotic effect of arundoin on human prostatic cancer cells by activating Poly ADP ribose polymerase / 中草药

Objective: To study the potential apoptotic effect of arundoin on human prostatic cancer cells. Methods: Arundoin was isolated and purified from the crude ethanol extract of Imperatae Rhizoma. Human prostatic cancer cell line PC3 was treated with arundoin. The relative cell viabilities were determined by MTT assay; Apoptosis was analyzed by Annexin V/PI dual staining with flow cytometry; The protein expression levels of Poly ADP ribose polymerase (PARP) and other apoptotic related proteins were detected by Western blotting. Results: Arundoin (20, 40, and 80 μmol/L) reduced the viability of PC3 cells dose- and time-dependently. Moreover, arundoin induced apoptosis in PC3 cells. Western blotting analysis showed that arundoin up-regulated the expression level of PARP in a dose-dependent manner. In addition, apoptosis related proteins such as Bax, Bcl-2, and casapases were all affected by arundoin. Conclusion: Arundoin could induce apoptosis in human prostatic cancer cells, which provides novel information for clinical application of arundoin and its preparations for the prostatic cancer patients.

Effects of Ethanol Extract of Crataegus Pinnatifida Bge. Var. major N. E. Br. from Heilongjiang Province on Hemodynamics of Acute Myocardial Ischemia and Platelet Aggregation in Rats / 中国药师

Objective: To observe the effect of ethanol extract of Crataegus Pinnatifida Bge. Var. major N. E. Br. from Hei-longjiang province on hemodynamics of acute myocardial ischemia caused by ligation and platelet aggregation induced by isoproterenol. Methods:After the model establishment of acute myocardial ischemia by ligation in rats, the systolic blood pressure ( SBP) ,diastolic blood pressure ( DBP ) , heart rate ( HR ) , left ventricular systolic pressure ( LVSP ) , left ventricular end-diastolic pressure ( LV-EDP) , left ventricular peak systolic ( +) and diastolic ( -) rate ( ± dp ·dt max-1 ) were recorded. Meanwhile, the acute myocar-dial ischemia model induced by isoproterenol was established. The platelet aggregation was measured by a platelet aggregation instru-ment. Results:The ethanol extract of Crataegus Pinnatifida Bge. Var. major N. E. Br. from Heilongjiang province could significantly increase the SBP, DBP, LVSP, +dp · dtmax-1 and HR, and reduce LVEDP,-dp·dtmax-1 in high dose group with statistical sig-nificance (P<0. 05). The medium dose group had small impact on the DBP, while showed statistically significant effect on the other hemodynamic indices. The low dose group had statistically significant effect on the SBP, LVSP and ± dp·dtmax-1 (P<0. 05), while showed no notable effects on the other indices. The results of aggregation rate in 1 min and 5 min after the determination and the maxi-mum one in the high and medium dose groups showed that the ethanol extract could significantly inhibit the platelet aggregation with sta-tistical significance (P<0. 05). Conclusion:The ethanol extract of Crataegus Pinnatifida Bge. Var. major N. E. Br. can improve the blood flow of acute myocardial ischemia in rats and reduce platelet aggregation after ischemia.

Phenolic compounds from roots of Imperata cylindrica var. major / 中草药·英文版

Objective: To study the chemical constituents from the roots of Imperata cylindrica var. major. Methods: The chemical constituents were isolated and purified by combination of silica gel, Sephadex LH-20, polyamide, and ODS column chromatography. The structures of the isolated compounds were identified by means of spectral data and physicochemical property. Results: Twelve phenolic compounds were isolated from I. cylindrica var. major and identified as 4,7-dimethoxy-5-methylcoumarin (1), 7-hydroxy-4-methoxy-5-methylcoumarin (2), 7- O-β- D-glucopyranosyl-4-methoxy-5-methylcoumarin (3), 6-hydroxy-5-methoxyflavone (4), 5-methoxyflavone (5), 5,7-dihydroxy-8-methoxyflavone (6), 4-hydroxybenzaldehyde (7), 4-hydroxy-cinnamic acid (8), 4-hydroxy-3-methoxybenzoic acid (9), 3,4-dimethoxyphenyl- O-β- L-rhamnopyranosyl-(1β6)-β- D-glucopyranoside (10), impecyloside (11), and graminone A (12). Conclusion Compounds 2β4, 6, and 10 are obtained from this plant for the first time. © 2013 Tianjin Press of Chinese Herbal Medicines.

ISSR Genetic diversity analysis of Panax japonicus var. major by molecular makers / 中草药

Objective: To analyze the genetic diversity of Panax japonicus var. major by inter simple sequence repeat (ISSR) molecular makers. Methods: Genetic diversity of 19 samples from main production areas was investigated by ISSR and analyzed by principal coordinate analysis and UPGMA cluster analysis. Results: A total of 181 bands were generated by 13 ISSR primers, among which 166 bands (91.71%) were polymorphic bands (PPB). The coefficient of genetic similarity ranged from 0.60 to 0.83. The results of UPGMA cluster analysis and principal coordinate analysis showed that the genetic diversity of P. japonicus var. major from the same region presented a geographical distribution regularity. Conclusion: The results of ISSR analysis reveals that P. japonicus var. major has a high genetic diversity level and the genetic relationship closely contacts with the geographical location.

Pharmacokinetic study of isoquercitrin in rat plasma after intravenous administration at three different doses

The aim of this study is to develop a simple and specific HPLC method using vitexin as the internal standard to investigate the pharmacokinetics of isoquercitrin (ISOQ) after three different doses administrated intravenously to rats. The pharmacokinetic parameters were calculated by both compartmental and non-compartmental approaches. The results showed that ISOQ fitted a three-compartment open model. The values of AUC increased proportionally within the range of 5-10 mg·kg-1. Moreover, a half-life, b half-life, ªCL, MRT0-t and MRT0→∞ of ISOQ in rats showed significant differences between 20 mg·kg-1 and other doses, indicating that ISOQ presented dose-dependent pharmacokinetics in the range of 5-10 mg·kg-1 and non-linear pharmacokinetics at higher doses.

O objetivo deste estudo é desenvolver um método simples e específico de HPLC usando vitexina como padrão interno para investigar a farmacocinética do isoquercitrina (ISOQ) após três doses diferentes administradas por via intravenosa a ratos. Os parâmetros farmacocinéticos foram calculados pelas abordagens compartimental e não compartimental. Os resultados mostraram que ISOQ se encaixa no modelo de três compartimentos. Os valores de AUC aumentaram proporcionalmente na faixa de 5-10 mg·kg-1. Além disso, a meia-vida, b meia-vida, ªCL, MRT0-t and MRT0→∞ de ISOQ em ratos mostraram diferenças significativas entre 20 mg·kg-1 e outras doses, o que significa que ISOQ apresenta farmacocinética dose-dependente no intervalo de 5-10 mg·kg-1 e farmacocinética não linear em doses mais elevadas.

Studies on chemical constituents from fruit of Crataegus pinnatifida / 中草药

Object To look for the proprietary constituent and the constituents with blood lipid regulating effect from the dried fruit of Crataegus pinnatifida Bge var major N E Br Methods Various column chromatographic techniques were employed for isolation and purification of the constituents UV, IR, EI MS, FAB MS, 1HNMR, 13 CNMR, HMBC, HMQC and 13 CGATE were used to identify the structure of the isolated constituents Results Six compounds were isolated from the fruit of C pinnatifida They were identified as 5, 7, 4′ trihydroxy flavone 8 C ? L rhamnopyranosyl (1→2) ? D glucopyranoside, i e vitexin rhamnoside (Ⅰ), hyperoside (Ⅱ), citric acid (Ⅲ), vitexin (Ⅳ), quercetin (Ⅴ), ursolic acid (Ⅵ) Conclusion Compound Ⅰ is a proprietary constituent in the fruit of C pinnalifida, which was obtained from this plant for the first time Compound Ⅱ is a main constituent with blood lipid reducing effect in flavonoids

A Study on Chemical Constituents of Volatile Oils from Panax Japonicus C. A. Meyer Var Major (Burk) Wh et Feng / 昆明医科大学学报

The volatile oils from Panax Japonicus C. A. Meyer var major (Burk) Wu et Feng grown in Teng-chong County were analyzed by GC/MS/DS. 27 kinds of components were identified and their relative contents were determined. Among them 10 molecules of sesquiterpene and 1 of sesquiterpenol appeared.