Xinjiang Huashidan Pharmaceutical Research Co.

Urunchi, China

Xinjiang Huashidan Pharmaceutical Research Co.

Urunchi, China
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Li Z.-J.,China Pharmaceutical University | Abulizi A.,Xinjiang Medical University | Zhao G.-L.,China Pharmaceutical University | Wang T.,China Pharmaceutical University | And 3 more authors.
Phytotherapy Research | Year: 2017

Psoralea corylifolia L. (Fructus Psoraleae) is widely used in Asia, but there are concerns about hepatotoxicity caused by constituents such as psoralens and bakukiol. Bakuchiol (BAK) has antiinflammatory, antipyretic, antibacterial antiviral, anticancer, and estrogenic activity but appears to be hepatotoxic in in vitro tests. This study investigated the hepatotoxicity in vivo in rats. Using intragastrically administered bakuchiol at doses of 52.5 and 262.5 mg/kg for 6 weeks. Bodyweight, relative liver weight, biochemical indicators, histopathology, mRNA expression of CYP7A1, HMG-CoA reductase, BSEP, PPARα, SREBP-2, and MRP3 were measured. Many abnormalities were observed in the bakuchiol-treated groups including suppression of weight gain and food intake, change of some parameters in serum biochemistry, and increased weight of liver. The mRNA expression of CYP7A1, HMG-CoA reductase, PPARα, and SREBP-2 decreased in bakuchiol-treated group, the expression of BSEP increased in bakuchiol-treated low dosage, and the expression of BSEP decreased in bakuchiol-treated high dosage. In conclusion, we provide evidence for the first time that bakuchiol can induce cholestatic hepatotoxicity, suggesting potential hepatotoxicity. The mechanism may be related to effects on liver lipid metabolism, but further investigation is necessary. © 2017 John Wiley & Sons, Ltd.


Guo L.,Xinjiang Huashidan Pharmaceutical Research Co. | Fan W.,Xinjiang Huashidan Pharmaceutical Research Co. | Gan Z.,Xinjiang Huashidan Pharmaceutical Research Co. | Chen W.,Xinjiang Huashidan Pharmaceutical Research Co. | And 2 more authors.
Journal of Chinese Pharmaceutical Sciences | Year: 2015

In the present study, we designed and synthesized a series of 1-substituted-β-carboline derivatives through modification of position-1, 2 and 9 of β-carboline nucleus in order to discover novel leading compounds with better antitumor activities and less toxicity. Their structures were confirmed by 1H NMR, 13C NMR, MS, IR and elemental analyses. All the target compounds were tested for cytotoxic activity against six cancer cell lines, including Bel-7402, HepG2, A549, A375, 786-0 and HT-29 by methyl thiazolyl tetrazolium (MTT) method. Studies of structure-activity relationships indicated that the effects of substituents in position-1 on cytotoxic activities were in an order as follows: 2-thienyl >2-chlorophenyl >4-chlorophenyl >benzyl group. © Journal of Chinese Pharmaceutical Sciences, School of Pharmaceutical Sciences, Peking University.


Chen X.-M.,China Pharmaceutical University | Chen X.-M.,Xinjiang University | Chen X.-M.,Xinjiang Huashidan Pharmaceutical Research Co. | Liu J.,China Pharmaceutical University | And 2 more authors.
Toxicology in Vitro | Year: 2012

Colchicine is an alkaloid that has been widely used to treat gout. It also has a curative effect on cancer. Although many studies have shown that its effect on cell apoptosis was mediated by the activation of caspase-3, the pathways involved in the process remained obscure. Here we show some evidence regarding the missing information using human normal liver cells L-02 in our study. The effect of colchicine on apoptosis in L-02 cells and the apoptosis-associated signaling pathways were determined using different tests including cell viability assay, Annexin V and propidium idodide binding, PI staining, Hoechst 33342 staining, mitochondrial membrane potential assay, caspase activity assay and Western blot analysis. We found that colchicine-induced a dose-dependent drop of cell viability in L-02 cells; early apoptosis happened when cells were treated with 0.1 μM of colchicine. The colchicine-induced loss of mitochondrial membrane potential, activation of caspase-3 and 9, up-regulation of Bax and down-regulation of Bcl-2 showed an evidence for the colchicine activity on apoptosis, at least, by acting via the intrinsic apoptotic pathway. © 2012.


Lu X.-H.,Xinjiang Medical University | Zhou F.,Xinjiang Huashidan Pharmaceutical Research Co. | Ma Q.,Xinjiang Huashidan Pharmaceutical Research Co.
Chinese Pharmaceutical Journal | Year: 2015

OBJECTIVE: To determine the contents of antler peptides in Cervus elaphus yarkandensis from different locations and harvest periods to evaluate their qualities. METHODS: The concentration of antler peptides of Cervus elaphus yarkandensis was measured by BCA protein assay kit. The protein contents between differen regions and harvest time were compared. RESULTS: A good linear relationship was achieved for the calibration curve of antler peptides in the range of 20-2 000 μg · mL-1 (r=0.997 9). The average recovery was 99.06% with RSD of 2.08% (n=6). The contents of antler peptides in Cervus elaphus Linnaeus from different locations were significantly different. There were also differences in the antler peptides content of the same origin samples collected in different periods. CONCLUSION: The established method is simple, accurate and reproducible, which can be adopted for determination of antler peptides in Cervus elaphus Linnaeus. Copyright 2015 by the Chinese Pharmaceutical Association.


Guo L.,Shihezi University | Guo L.,Xinjiang Huashidan Pharmaceutical Research Co. | Cao R.,Sun Yat Sen University | Fan W.,Xinjiang Huashidan Pharmaceutical Research Co. | And 2 more authors.
Gaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities | Year: 2016

A series of novel bivalent β-carbolines with a spacer of three to ten methylene units between the 7-oxygen was synthesized and characterized by nuclear magnetic resonance(NMR) and mass spectrometry(MS). The antitumor activities against Bel-7402, 786-0, BGC-823, A375, 769-P and MCF7 cell lines in vitro were investigated by MTT method. The results demonstrated that compounds 4c, 4k and 4r were almost inactive against all tumor cell lines, compounds 4g and 4o displayed significant cytotoxic activities with IC50 value of lower than 10 μmol/L against all tumor cell lines. Most compounds displayed good and selective cytotoxic activities against HT-29 and Blu-87 cell lines. Primary structure-activity relationships(SARs) analysis indicated that the length of the spacer affected cytotoxic activities in vitro, and 8-10 methylene units were more favorable. Moreover, n-butyl or i-butyl substituents in position-9 of β-carboline facilitated the antitumor potencies. © 2016, Higher Education Press. All right reserved.


Guo L.,Xinjiang Huashidan Pharmaceutical Research Co. | Cao R.,Xinjiang Huashidan Pharmaceutical Research Co. | Cao R.,Sun Yat Sen University | Fan W.,Xinjiang Huashidan Pharmaceutical Research Co. | Ma Q.,Xinjiang Huashidan Pharmaceutical Research Co.
Gaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities | Year: 2014

In order to search for novel candidate compounds endowed with better antitumor activities and less neurotoxicities, a series of harmine derivatives were synthesized by modiflcation of position 2, 7 and 9 of β-carboline nucleus through N9-alkylated, C7-demethylated and C7-phenolic hydroxyl alkylated. C7-demethylation compounds could be easily obtained from the N9-alkylated derivatives using acetic acid and hydrobromic acid as reaction solvent, but N9-arylted derivatives couldn't get the demethylation compounds in the same way. The N2-quaternarized compounds(4a, 4b, 8a and 8b) were prepared from demethylation compounds (3a, 3b, 7a and 7b) by the addition of benzyl bromide in refluxing ethyl acetate. Eleven target compounds were synthesized and characterized by 1H NMR, 13C NMR, IR, MS and elemental analysis. All the target compounds were tested for cytotoxic activity against six cancer cell lines including Bel-7402, 786-0, BGC-823, A375, 769-P and MCF7 by methyl thiazolyl tetrazolium (MTT) method in vitro. Structure-activity relationships studies confirmed that N2-quaternarized compounds (4a, 4b, 8a and 8b) had more remarkable cytotoxic activities in vitro than harmine.


Guo L.,Xinjiang Huashidan Pharmaceutical Research Co. | Fan W.,Xinjiang Huashidan Pharmaceutical Research Co. | Chen X.,Xinjiang Huashidan Pharmaceutical Research Co. | Ma Q.,Xinjiang Huashidan Pharmaceutical Research Co. | And 2 more authors.
Chinese Journal of Organic Chemistry | Year: 2013

In search of more effective antitumor agents, based on the previous results of computer aided drug design. The starting material L-tryptophan reacted with formaldehyde via Pictet-Spengler condensation and followed by oxidation and decarboxylation to afford the intermediate β-carboline. The intermediate was further reacted with halogenated hydrocarbon by N9-alkylation and N2-quaternarization to obtain new β-carboline derivatives. Fourteen novel β-carboline derivatives were synthesized and characterized by 1H NMR, IR, MS and elemental analysis. Compound 5h was further studied by X-ray single crystal diffraction analysis. The antitumor activity of the target compounds was studied by MTT method. The results demonstrated that N2-quaternarized compounds (5a~5n) had more remarkable cytotoxic activities in vitro than 9-phenylpropyl-β-carboline (4). The tumor inhibition rates of the selected compounds 5e and 5h in mice bearing Lewis lung cancer. The compound 9 showed inhibition activity on transplanting-tumor growth of Lewis lung cancer. © 2013 Chinese Chemical Society & SIOC, CAS.


Ma Q.,Xinjiang Medical University | Ma Q.,Xinjiang Huashidan Pharmaceutical Research Co. | Guo L.,Xinjiang Huashidan Pharmaceutical Research Co. | Sun J.,Xinjiang Huashidan Pharmaceutical Research Co. | Fan W.-X.,Xinjiang Huashidan Pharmaceutical Research Co.
Yaoxue Xuebao | Year: 2013

The starting material L-tryptophan reacted with 4-chlorobenzaldehyde via Pictet-Spengler condensation and followed by oxidation and decarboxylation to afford the 1-(4-chlorophenyl)-β-carboline. The intermediate was further reacted with alkyl halogenide by N9-alkylation and N 2-quaternarization to obtain 12 novel 1-(4-chlorophenyl)-β- carboline derivatives. The chemical structures of all target compounds were characterized by elemental analyses, MS and 1H NMR spectra. The antitumor activities of the target compounds were evaluated by MTT method. The results demonstrated that N2-quaternarized compounds enhanced the antitumor activity significantly. In particular, compound 15 was found to be the most potent compound with IC50 values lower than 5 μmol·L-1 against 6 human tumor cells. These results confirmed that the N2-alkyl or aralkyl substituent on the β-carboline ring played an important role in the modulation of the antitumor activities.


Patent
Xinjiang Huashidan Phar Maceutical Research Co. | Date: 2012-11-26

Disclosed in the present invention are a bis--carboline compound and a preparation method, a pharmaceutical composition and the use thereof. In particular, the bis--carboline compound and a pharmaceutical salt thereof are described as general formula I, and the bis--carboline compound is prepared through the condensation of -carboline intermediate and dihaloalkane. Also disclosed in the present invention are a pharmaceutical composition comprising an effective dose of the bis--carboline compound as shown in formula I and a pharmaceutically acceptable carrier, and the use of the bis--carboline compound in preparing drugs resistant to tumours such as melanoma, stomach cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermoid carcinoma, cervical cancer, ovarian cancer, pancreatic cancer, prostate cancer, and colon cancer.


Patent
Xinjiang Huashidan Pharmaceutical Research Co. | Date: 2015-09-30

Disclosed in the present invention are a bis--carboline compound and a preparation method, a pharmaceutical composition and the use thereof. In particular, the bis--carboline compound and a pharmaceutical salt thereof are described as general formula I, and the bis--carboline compound is prepared through the condensation of -carboline intermediate and dihaloalkane. Also disclosed in the present invention are a pharmaceutical composition comprising an effective dose of the bis--carboline compound as shown in formula I and a pharmaceutically acceptable carrier, and the use of the bis--carboline compound in preparing drugs resistant to tumours such as melanoma, stomach cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermoid carcinoma, cervical cancer, ovarian cancer, pancreatic cancer, prostate cancer, and colon cancer.

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