Oroxylin A inhibits glycolysis-dependent proliferation of human breast cancer via promoting SIRT3-mediated SOD2 transcription and HIF1α destabilization.

Alterations of cellular metabolism play a central role in the development and progression of cancer. Oroxylin A, an active flavonoid of a Chinese traditional medicinal plant, was previously shown to modulate glycolysis in cancer cells. However, the mechanism by which oroxylin A regulates glycolysis is still not well defined. Here, we show that oroxylin A inhibits glycolysis in breast cancer cells via the Sirtuin 3 (SIRT3)-mediated destabilization of hypoxia-inducible factor 1α (HIF1α), which controls glycolytic gene expression. Oroxylin A promotes superoxide dismutase (SOD2) gene expression through SIRT3-regulated DNA-binding activity of FOXO3a and increases the activity of SOD2 by promoting SIRT3-mediated deacetylation. In vivo, oroxylin A inhibits the growth of transplanted human breast tumors associated with glycolytic suppression. These data indicate that oroxylin A inhibits glycolysis-dependent proliferation of breast cancer cells, through the suppression of HIF1α stabilization via SIRT3 activation, providing preclinical information for the cancer therapies of SIRT3 stimulation.

Preparation of inulin-type fructooligosaccharides using fast protein liquid chromatography coupled with refractive index detection.

A fast protein liquid chromatography coupled with refractive index detection (FPLC-RID) method was firstly developed for preparation and purification of fructooligosaccharides with different degree of polymerization from burdock, Arctium lappa. After extraction with 60% ethanol and decolorization with MCI gel CHP20P, total fructooligosaccharides were purified on Bio-Gel P-2 column eluted with water at the flow rate of 0.3 ml/min, which was the optimized conditions. The obtained fructooligosaccharides with degree of polymerization of 3-9 were identified based on their methylation analysis, MS and NMR data. This method has the advantages of high automation, good recovery and easy performance, which could be used for preparation of FOS from other sources, as well as other targeted compounds without UV absorbance.

A novel strategy with standardized reference extract qualification and single compound quantitative evaluation for quality control of Panax notoginseng used as a functional food.

Root of Panax notoginseng (Burk.) F.H. Chen (Sanqi in Chinese) is one of traditional Chinese medicines (TCMs) based functional food. Saponins are the major bioactive components. The shortage of reference compounds or chemical standards is one of the main bottlenecks for quality control of TCMs. A novel strategy, i.e. standardized reference extract based qualification and single calibrated components directly quantitative estimation of multiple analytes, was proposed to easily and effectively control the quality of natural functional foods such as Sanqi. The feasibility and credibility of this methodology were also assessed with a developed fast HPLC method. Five saponins, including ginsenoside Rg1, Re, Rb1, Rd and notoginsenoside R1 were rapidly separated using a conventional HPLC in 20 min. The quantification method was also compared with individual calibration curve method. The strategy is feasible and credible, which is easily and effectively adapted for improving the quality control of natural functional foods such as Sanqi.

Oroxylin A induces dissociation of hexokinase II from the mitochondria and inhibits glycolysis by SIRT3-mediated deacetylation of cyclophilin D in breast carcinoma.

Oroxylin A is a major active component of the Chinese traditional medicinal plant Scutellaria baicalensis Georgi, which has been reported as a potential anticancer drug. We demonstrated that, Oroxylin A inhibited the glycolysis and the binding of hexokinase II (HK II) with mitochondria in human breast carcinoma cell lines, which was dependent on sirtuin-3 (SIRT3). The level of SIRT3 in mitochondria was increased by Oroxylin A. Then SIRT3 deacetylated cyclophilin D, diminished its peptidyl-prolyl cis-trans isomerase activity and induced its dissociation from the adenine nucleotide translocator. Finally, SIRT3-induced inactivation of cyclophilin D resulted in the detachment of mitochondrial HK II and the inhibition of glycolysis. These results have important implications for the metabolism reprogramming effect and the susceptibility to Oroxylin A-induced mitochondrial cytotoxicity through the regulation of SIRT3 in breast carcinoma.

[Pharmacognostical studies on the rhizome and root of Alpinia nigra].

Morphological and histological characters of the rhizome and root of Alpinia nigra (Gaertn.) Burtt, used as the origin of a traditional Chinese medicine, were described and illustrated with line drawing. These studies provide referential information for the identification and quality control.

[Studies on the chemical constituents of Zanthoxylum dimorphophyllum Hemsl. var spinifolium Rhed. et Wils].

AIM: To study the chemical components from the dried roots of Zanthoxylum dimorphophyllum Hemsl. var spinifolium Rhed. et Wils. METHODS: Modern chromatography was used to isolate chemical components and the compounds isolated from Zanthoxylum dimorphophyllum Hems1. var spinifolium Rhed. et Wils were identified by various spectral methods. RESULTS: Five compounds were isolated and identified as 6-(2',3'-dihydroxy-3'-methybutyl)-7-acetoxy-2H-1-benzopyran-2-one (I), 6-(2',3'-dihydroxy-3'-methybutyl)-7-(beta-D-glucopyranosyloxy)- 2H-1-benzopyran-2-one (II), hexacosanoci acid (III), aurepten (IV), 6-[6'-O-(-deoxy-alpha-L-mannopyranosyl)-beta-D-benzopyran-4-one (V). CONCLUSION: All of the above compounds were isolated from the plant for the first time, among them, I is a new compound.

[Pharmacognostical studies on the root and rhizome of Globba racemosa].

Morphological and histological characters of the root and rhizome of Globba racemosa Smith were described and illustrated with line drawing. These studies provided referential information for the identification and quality control.

[Pharmacognostical studies on the rhizome, root and leaf of Alpinia jianganfeng T.L. Wu].

Morphological and histological characters of the rhizome, root and leaf of Alpinia jianganfeng T.L. Wu used as the origin of a traditional Chinese medicine, were described and illustrated with line drawing. These studies provide referential information for the identification and quality control.

Alterations of prostate biomarker expression and testosterone utilization in human LNCaP prostatic carcinoma cells by garlic-derived S-allylmercaptocysteine.

BACKGROUND: This study determined the effects of S-allylmercaptocysteine (SAMC), a phytoconstituent from garlic, on the expression of androgen-responsive biomarkers, prostate specific antigen (PSA), and prostate specific membrane antigen (PSMA), in human prostatic carcinoma cells (LNCaP). METHODS: Secretion of PSA was determined as well as the activity of PSMA measured as a function of its ability to hydrolyze poly-gamma-glutamated folate and N-acetylaspartylglutamate (NAAG). Folate hydrolase capacity was also determined in SAMC-treated cells grown in charcoal stripped fetal calf serum (CS-FCS). In addition, testosterone disappearance was measured from culture media of SAMC-treated LNCaP and PC-3 cells as well as from cell free lysates. RESULTS: PSA secretions were significantly decreased compared to control values at 1 day (8.4 +/- 2.6 vs. 18.9 +/- 1.7, P < 0.01), 4 days (18.9 +/- 5.3 vs. 73.8 +/- 4. 4, P < 0.001), and 6 days (35.6 +/- 2.1 vs. 96.5 +/- 17.9 ng/10(5) cells, P < 0.01; mean +/- SD). By contrast, PSMA activity measured as either folate hydrolase or NAAG dipeptidase (NAALADase) activity increased in cells treated with SAMC. PSMA-folate hydrolase activity in SAMC-treated cells grown in CS-FCS increased beyond that observed in cells grown in CS-FCS alone. Pre-exposure of LNCaP cells to SAMC resulted in enhanced rate of testosterone disappearance from culture media at 6 hr (P < 0.01) and at 48 hr (P < 0.001) compared to media from cells not previously exposed to SAMC. Results similar to these were also observed in androgen-independent PC-3 cells treated with SAMC. In lysates of SAMC-treated LNCaP cells, the rate of testosterone catabolism was twice that from phosphate buffered saline (PBS)-treated cells. SAMC-treated LNCaP cells grown in media supplemented with testosterone temporarily exhibited enhanced growth over a 2 day period but cell numbers declined later to levels similar to those of SAMC treatment. CONCLUSIONS: These results show that SAMC exhibits differential effects on recognized biomarkers for LNCaP cells similar to those produced by androgen deprivation and strongly suggests that this effect may be mediated, in part, by diminishing the trophic effects of testosterone, likely by converting it to metabolites less reactive toward androgen receptors.

[Evaluation on antiendotoxic action and antiviral action in vitro of tetraploid Isatis indigotica].

OBJECTIVE: To evaluate the pharmacological effect of tetraploid Isatis indigotica Fort. METHODS: Comparing these actions of tetraploid I. indigotica with those of the diploid parent. RESULTS: These actions of tetraploid I. indigotica were obviously stronger than those of the diploid parent. The pharmacological effect of leaves was greater than that of roots with identical ploidy. CONCLUSION: Tetraploid I. indigotica is a new line of better quality, deserving to be exploited and utilized on a large scale.

[A new fatty ketone of Radix Polygoni Multiflori Preparata].

OBJECTIVE: Investigating the chemical constituents of Radix Polygoni Multiflori Preparata. METHODS: Compounds were isolated from the CHCl3 extract with column chromatography on silica gel, and identified on the basis of spectral analysis(IR, EI-MS, 1H-NMR, 13C-NMR) and phytochemical properties. RESULTS: Two compounds were isolated and identified as 1,2-dihydroxynonadecone-3(I) and gallic acid(II). CONCLUSION: Compound I is a new compound.

[Structural elucidation of a new tetrahydroxystilbene of Radix Polygoni Multiflori Preparata and study on its cardiovascular activity].

AIM: To investigate the cardiovascular active constituents of Radix Polygoni multiflori Preparata. METHODS: Compounds were isolated from the water soluble extract with column chromatography of Sephadex, ODS and HPLC. The compounds were identified on the basis of spectral analysis (IR, EI-MS, FAB-MS, 1HNMR, 13CNMR, 2D-NMR) and phytochemical properties. Its inhibitory effect on the proliferation of bovine vascular smooth muscle cells were bioassayed in vitro. RESULTS: One compound was isolated and identified as: 2,3,5,4'-tetrahydroxystilbene-2-O-(6"-O-alpha-D- glucopyranosyl)-beta-D-glucopyranoside. CONCLUSION: Compound I is a new compound with cardiovascular activity.

[The morphological variation in species of Anemarrhena asphodeloides].

In this paper, morphological studies modified the description in some literatures. The features of Anemarrhena asphodeloides Bunge growing in different districts vary. Carefully observation under Scanning Electron Microscope (SEM) showed that surface characters of leaves at the same developing stage, which were collected from cultivated plants formerly growing in different districts, vary greatly but regularly. It was found that the morphology of pollen grains were similar.

[Determination of organic acids of tetraploid Isatis indigotica with high performance capillary electrophoresis].

The content of organic acids, being antiendotoxic activities in vitro, of tetraploid Isatis indigotica Fort. were determined with high performance capillary electrophoresis. The results showed that the contents of organic acids of tetraploid Isatis indigotica Fort. were obviously higher than that of diploid parent. Tetraploid Isatis indigotica Fort. was a new lines with better quality, which had notably value of exploiting and utilizing.

[Analysis of the constituents of essential oil from radix Polygoni multiflori preparata].

The chemical constituents of oil from Radix Polygoni Multiflori Preparata were analyzed by GC-MS-DS.27 constituents were identified.

[Research on cause of distinction in antiendotoxic activation of radix isatidis from different cultivated populations].

OBJECTIVE: To research into the cause of distinction in antiendotoxic activation of Radix Isatidis from different cultivated populations. METHOD: 19 samples of Radix Isatidis were gathered. 12 portions of seeds were cultivated in the same field in Shanghai, and the selected and artificially bred autotetraploid seeds were planted in 5 different locations. All the samples were compared through antiendotoxic experiment. RESULTS: There are some marked distinction among the 19 samples from different populations. The distinction of the 12 samples cultivated in the same field didn't disappear. The activation of autotetraploid from 5 different locations didn't vary on the whole. CONCLUSION: Germplasm is the main factor to cause activation distinctions of Radix Isatidis, while environment is less important.

[Determination on chemical constituents of Curcuma L. produced in China].

OBJECTIVE: To provide some valuable information for the research on species systematization and quality standardization of Curcuma drugs. METHODS: Colorimetry, TLC-colorimetry and water vapour distillation were used to determine the contents of curcuminoids, curcumin and essential oils of 34 samples of Curcuma produced in China. RESULTS AND CONCLUSION: The contents of curcuminoids and curcumin are different upto an extent of over 100 times among the varieties of Curcuma, and those of essential oils to an extent of 6 times. But there is little difference in the samples of the same species from different producing areas. There is also an obvious correlativity between the contents of curcuminoids and essential oils in the varieties of curcuma.

[Determination of sarsasapogenin in Anemarrhena asphodeloides Bunge by GC].

OBJECTIVE: To determine sarsasapogenin in Anemarrhena asphodeloides. METHOD: Chloromethane extract (1 microliter) with cholesterol as internal standard was analyzed on HP-1 column, operated at 270 degrees C with N2 as carrier gas and FID. RESULT: The method was linear within the range of 0.245-2.94 micrograms.microliter-1, with a correlation coefficient of 0.9996. The average recovery was 95.52% +/- 1.77%, CONCLUSION: The method is reproducible, rapid and sensitive.

Effects of garlic thioallyl derivatives on growth, glutathione concentration, and polyamine formation of human prostate carcinoma cells in culture.

This study investigated whether naturally occurring garlic derivatives and synthetic S-cysteinyl compounds that resemble garlic constituents have antiproliferative effects on human prostate carcinoma (LNCaP) cells. Studies also examined whether S-allylmercaptocysteine and S-allylcysteine affect two important molecular targets, namely reduced glutathione and polyamines. Results showed that S-allylmercaptocysteine (50 mg/L) diminished LNCaP cell growth whereas the antiproliferative effect of S-allylcysteine was not as pronounced. Studies using synthetic S-cysteinyl analogues revealed that growth inhibition was most effective with compounds containing a disulfide or an active diallyl moiety. Marginal to no inhibitory effect was observed with monosulfinic analogues. Both S-allylmercaptocysteine and S-allylcysteine caused an increase in LNCaP cell reduced glutathione concentrations. Putrescine and spermine concentrations decreased and spermidine increased 3 d after S-allylmercaptocysteine treatment. At 5 d after S-allylmercaptocysteine treatment, polyamine concentrations were similar to those of saline-treated controls. Diminished cell growth and altered polyamine concentrations suggest that S-allylmercaptocysteine may impede the polyamine synthesizing enzyme, ornithine decarboxylase, either by enhancing the formation of reduced glutathione, a known inhibitor of ornithine decarboxylase, or by reacting directly with ornithine decarboxylase at its nucleophilic thiol moiety. Because S-allylcysteine also increases reduced glutathione formation but does not significantly inhibit growth, the latter mechanism may be more likely for this compound. These data provide further evidence that nonessential nutrients derived from garlic may modulate tumor growth. Further research is required on effects of garlic derivatives in vivo before information from the present studies can be used to assist in the development of effective nutritional strategies for preventing progression of prostate cancer.

[Effect of processing on chemical composition and medical activity of rhizoma Anemarrhenae].

A comparative study was conducted on the chemical composition and medical activity of different kinds of processed drug of Rhizoma Anemarrhenae. It was found that the content of effective components of zhimu was affected obviously by processing: the rhizome should not be barked when used as drug. It was also observed that different kind of processed drug should be used in line with different particular circumstance.