1.Antitussive constituents of Disporum cantoniense.
Xiu-Hai GAN ; Chao ZHAO ; Zhi-Yuan LIANG ; Xiao-Jian GONG ; Hua-Guo CHEN ; Xin ZHOU
China Journal of Chinese Materia Medica 2013;38(23):4099-4103
The antitussive activity assay for the root extraction of Disporum cantoniense was carried out with coughing mice induced by ammonia liquor. The results showed that the ethanol and water extractions of D. cantoniense possess strong antitussive activity, and the high dose of the former was better than positive control, and then the constituents of the ethanol extraction were separated and purified by various modern chromatographic techniques. Their structures were identified by physico-chemical properties and spectroscopic data. As a result, eight compounds were isolated and identified as stigmast-4-en-3-one(1), (22E, 24R)-ergosta-5, 7, 22-trien-3beta-ol(2), obtucarbamate A(3), obtucarbamate B(4), neotigogenin(5), azo-2, 2'-bis[Z-(2,3-dihydroxy-4-methyl-5-methoxy) phenyl ethylene] (6),dimethyl {[carbonylbis (azanediyl)] bis( 2-methyl-5, 1-phenylene) j dicarbamate (7) , and quercetin-3-O-pB-D-glucopyranoside(8). All compounds were isolated from this plant for the first time, and the result of bioactivity-directed isolation showed that compounds 3, 4, and 6 had obvious effect on antitussive activity, and compound 6 had the same level as positive control.
Animals
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Antitussive Agents
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chemistry
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isolation & purification
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pharmacology
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Drugs, Chinese Herbal
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chemistry
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isolation & purification
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pharmacology
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Ethanol
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chemistry
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Female
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Liliaceae
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chemistry
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Male
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Mice
2.Effects of alcohol intake on penile structure and function in rats.
Xiu-guo GAN ; Xue-ming SHI ; Rui LIU ; Rui-hua AN ; Yong-quan WANG
Chinese Medical Sciences Journal 2007;22(3):192-195
OBJECTIVETo investigate the effects of alcohol intake on penile structure and function in rats.
METHODSThirty adult male Wistar rats were randomly divided into two groups: control group and alcohol intake group. They were administered with 2 mL of normal saline and 40% alcohol solution respectively through gastric tubes every day. Three months later, the animal model of alcohol intake was evaluated by modified Nayagida's method, and the effects of alcohol on the rats were studied by sexual behavior, the number of apomorphine-induced penile erection, level of testosterone in the sera, and the content of penile smooth muscle.
RESULTSThe scores of animal model of alcohol intake evaluated by Nayagida's method were 0.66 +/- 2.05 in the control group and 9.26 +/- 5.50 in the alcohol intake group (P < 0.05), which indicated that an animal model of alcohol intake was successfully established. Sexual behavior, the number of apomorphine-induced penile erection, testosterone level in the sera, and the content of penile smooth muscle of the alcohol intake group were all statistically different as compared with the control group (P < 0.05).
CONCLUSIONAlcohol intake induces sexual dysfunction in rats, which may be due to the decline of testosterone level in the sera and decline of penile smooth muscle.
Animals ; Ethanol ; adverse effects ; Female ; Male ; Penis ; anatomy & histology ; drug effects ; physiology ; Rats ; Rats, Wistar ; Sexual Behavior, Animal ; Testosterone ; blood
3.Expressions of voltage-gated K+ channel 2.1 and 2.2 in rat bladder with detrusor hyperreflexia.
Xiu-guo GAN ; Rui-hua AN ; Yu-feng BAI ; De-bin ZONG
Chinese Medical Journal 2008;121(16):1574-1577
BACKGROUNDVoltage-gated K+ channel (Kv) plays a critical role in the modulation of detrusor contraction. This study was conducted to investigate the expressions of Kv2.1 and Kv2.2 in rat bladder with detrusor hyperreflexia (DH).
METHODSThirty adult female Sprague-Dawley rats (200-220 g) were randomly divided into the control group and the experimental group. The experimental group was subjected to spinal cord injury (SCI). In the controls, the surgical procedure was identical with the exception that dura and spinal cord were transected. Four weeks after SCI, in vivo cystometry and mechanical pulling tests of isolated detrusor strips were performed. mRNA was extracted from the detrusors of normal and DH rats for the detection of expression of Kv2.1 and Kv2.2 by RT-PCR. Differences in expression between normal and overactive detrusors were identified by gel imaging.
RESULTSFourteen rats in the experimental group exhibited uninhibited bladder contraction (>8 cmH2O) before voiding after SCI. One rat died from infection. The frequency of DH in the experimental group was significantly different from that in the control group with or without treatment with 4-aminopyridine (4-AP) (P < 0.05), while the amplitude of DH did not change markedly. The rates of variation of the automatic contractile frequency and amplitude were (66.8 +/- 12.4)% and (42.6 +/- 12.6)% respectively in the control group, and (38.4 +/- 9.8)% and (28.0 +/- 4.6)% respectively in the DH group. 4-AP increased the automatic contractile frequency apart from the automatic contractile amplitude in both the control and DH groups (P < 0.05). 4-AP increased the rate of variation of the automatic contractile frequency more markedly in the control group than in the DH group (P < 0.05). Significant expression of Kv2.2 was not detected in bladders in the control group. Compared to the mRNA levels of beta-actin, the mRNA level of Kv2.1 was 1.26 +/- 0.12 in the control group and 0.66 +/- 0.08 in the DH group. SCI significantly reduced the mRNA level of Kv2.1 in rat bladders with DH (P < 0.05).
CONCLUSIONSOur study showed that the mRNA level of Kv2.1 decreased significantly in rat bladder with DH, which was one of the important pathogenetic mechanisms for DH, and suggested that Kv2.1 might be one of the therapeutic targets for bladder overactivity.
Animals ; Female ; In Vitro Techniques ; Muscle Contraction ; RNA, Messenger ; analysis ; Rats ; Rats, Sprague-Dawley ; Reverse Transcriptase Polymerase Chain Reaction ; Shab Potassium Channels ; genetics ; physiology ; Urinary Bladder ; metabolism ; Urinary Bladder, Overactive ; etiology ; metabolism
4.Relationship between ethanol intake and sexual function in rats.
Xiu-guo GAN ; Rui-hua AN ; Yong-quan WANG
National Journal of Andrology 2006;12(12):1099-1101
OBJECTIVETo investigate the relationship between the intake of ethanol and sexual function of rats.
METHODSSixty adult male Wistar rats were randomly divided into five groups: the control, 10% , 20% , 30% and 40 ethanol groups, which received. . 9% sodium chloride, 10% , 20% , 30% and 40% ethanol solutions respectively at a dose of 2 ml through gastric tubes once a day. Three months later, we observed the effects of ethanol on the sexual function of the rats by their sexual behaviors, the number of apomorphine-induced penile erections, and the content of testosterone in the serum and nitric oxide synthase ( NOS) in the penis.
RESULTSCompared with the control group, the number of apomorphine-induced penile erections in the 10% and 20% ethanol groups was not inhibited significantly (P > 0.05), but the latent period of mounting and intromission in the 10% ethanol group was prolonged and the sexual behaviors in the 20% ethanol group were inhibited except the latent period of ejaculation. The sexual behaviors and the number of apomorphine-induced penile erections of the 30% and 40% ethanol groups were inhibited significantly (P < 0.05). Testosterone in the serum and NOS activity in the penis of the experimental groups were reduced (Pat < 0.05).
CONCLUSIONAn adequate volume of ethanol does not induce sexual dysfunction in rats, but long term and excessive intake of ethanol may cause penile erectile dysfunction.
Animals ; Dose-Response Relationship, Drug ; Ethanol ; administration & dosage ; pharmacology ; Male ; Nitric Oxide Synthase ; metabolism ; Penile Erection ; drug effects ; Penis ; metabolism ; Random Allocation ; Rats ; Rats, Wistar ; Sexual Behavior, Animal ; drug effects ; Testosterone ; blood
5.The effect of ethanol on sexual function of males and its mechanism.
Xiu-Guo GAN ; Rui-Hua AN ; De-Bin ZHONG
National Journal of Andrology 2006;12(2):175-177
Though an adequate volume of ethanol relieves nervousness and enhances sexual desire,long term and excessive intake of ethanol can induce sexual dysfunction. The reasons that ethanol results in sexual dysfunction are as follows: ethanol inhibits the hypothalamo-pituitary-testes axis and decreases serum testosterone level. The decline of smooth muscle, choline acetyltransferase and nitric oxide synthase in the penis may be responsible for it.
Acetylcholinesterase
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metabolism
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Animals
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Ethanol
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pharmacology
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Hypothalamo-Hypophyseal System
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drug effects
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Male
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Nitric Oxide Synthase
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metabolism
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Penis
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cytology
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metabolism
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Rats
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Sexual Behavior, Animal
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drug effects
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Testosterone
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blood
6.The dynamic effects of allogenic transplantations with the bladder acellular matrix grafts of rabbits.
Yong-quan WANG ; Xiu-guo GAN ; Rui-hua AN ; Cheng ZHANG ; Yan WANG
Chinese Journal of Surgery 2005;43(18):1219-1222
OBJECTIVETo study the dynamic effects of allogenic transplantations with the bladder acellular matrix grafts (BAMG) of rabbits.
METHODSHemi-cystectomies were performed in 25 rabbits, and the defects were repaired with BAMG about half bladder size. The rabbits underwent postoperative assessment of bladder function at 8 weeks, including cystometry, vesical volume, vesical compliance and cystography. The allografts were observed by light microscope and electron microscope at 1, 2, 4, 8, 12, 16 weeks after surgery.
RESULTSMacroscopic observation revealed that BAMG regenerated gradually. All urodynamic results of 8 weeks after surgery were not different statistically as compared with these of preoperation (P > 0.05). Cystography revealed that the morphous of bladder was recovered. Epithelialization and neovascularity occurred accompanied by infiltration of inflammatory cell at 1 week. Smooth muscle cell and stratified epithelium regenerated 2 weeks after grafting. Neural elements formed around smooth muscle bundles as early as 4 weeks. Each component regenerated on the frame of BAMG sequentially. After 16 weeks, it was difficult to delineate the junction between the host bladder and BAMG by histology.
CONCLUSIONAfter allogenic transplantation with rabbits' BAMG, the constitution and function of the allografts regenerate completely and gradually on the frame of BAMG.
Animals ; Extracellular Matrix ; transplantation ; Rabbits ; Regeneration ; Tissue Engineering ; Transplantation, Homologous ; Urinary Bladder ; cytology ; physiology ; transplantation
7.Studies on the correlation between titer of antibodies against different function regions of hepatitis C virus and HCV RNA of chronic patients.
He-qiu ZHANG ; Guo-hua WANG ; Kun CHEN ; Bing-shui XIU ; Xiao-guo SONG ; He-zhong LIU ; Shi-gan LING
Chinese Journal of Hepatology 2003;11(12):754-755
OBJECTIVETo detect humoral immune response against different function regions of hepatitis C virus (HCV) in chronic patients, and further to investigate the correlativity between anti-HCV antibody titers and HCV RNA concentration.
METHODSUsing recombinant dominate epitope antigens, e.g. HCV Core, NS3, NS4, NS5 and chimeric HVR1, a set of ELISA test reagents was formulated. Then, titers of antibodies against HCV different regions and the RNA concentration of HCV in chronic patient sera were detected by ELISA and quantitative RT-PCR technique, respectively.
RESULTSGreat differences have been noted in antibody titers and positive rate of different HCV function regions in chronic patients. Antibodies against HCV Core and HVR1 have the highest positive rate, then NS3, NS4, and NS5 in sequence.
CONCLUSIONThe titer of antibodies against different regions of HCV in chronic patients has good correlation with HCV RNA concentration.
Hepatitis C Antibodies ; blood ; Hepatitis C, Chronic ; immunology ; virology ; Humans ; RNA, Viral ; blood
8.Preparation of exosome-coated Bcl-2 siRNA and its inhibitory effect on the growth of pancreatic cancer cells
Ling ZUO ; Gan QIAO ; Ming-yue GUO ; Xiu-kun LIN ; Ming-hua LIU
Acta Pharmaceutica Sinica 2020;55(12):2918-2923
High expression of Bcl-2 is associated with the development of pancreatic cancer, and downregulation of Bcl-2 is an effective approach for the treatment of pancreatic malignancy. In the present study exosomes were isolated from the cultured medium of human embryonic kidney cells (HEK293) by ultracentrifugation and exosome-coated Bcl-2 siRNA (exosiBcl-2) was synthesized using electroporation. The results showed that the particle size of exosiBcl-2 was 67.3 ± 9.7 nm and the morphology of exosomes displayed a concave ring structure as determined by transmission electron microscopy (TEM). Western blot analysis indicated that exosomal proteins including CD9, CD81, CD63 and TSG101 were highly expressed. Confocal microscopy revealed that exosiBcl-2 was widely distributed in Miapaca-2 cells, and the transfection efficiency of exosiBcl-2 in Miapaca-2 was 77.2% as determined by flow cytometry. Treatment with exosiBcl-2 at a concentration of 100 nmol·L-1 resulted in an inhibitory effect on the growth of Miapaca-2 cells with an inhibition rate of 63%. ExosiBcl-2 treatment can downregulate Bcl-2 and upregulate Bax protein. This study provides evidence that exosiBcl-2 is able to inhibit the growth of pancreatic cancer cells and the nanoparticles have potential to be developed as a novel anticancer agent.
9.Study on long-acting analgesic lappaconitine hydrobromide lyotropic liquid crystal injection
Wen-xiu YUAN ; Zhi-Chao XIAO ; Yin-yin SUN ; Rong-rong CHEN ; Shi-yan GUO ; Yong GAN
Acta Pharmaceutica Sinica 2023;58(6):1685-1692
Long-acting analgesia is a common clinical treatment method after surgery. The slow-release injection with long-acting analgesia has the advantages of less medication frequency and stable effect. In this study, the analgesic drug lappaconitine hydrobromide lyotropic liquid crystal injection was prepared, and its sustained release mechanism, drug release and pharmacodynamic characteristics were evaluated. The results of polarizing microscope and freeze-transmission electron microscope showed that the lyotropic liquid crystal injection of the liquid crystal precursor preparation of lappaconitine hydrobromide could be obtained by the combination of glycerol monooleate (GMO) and soybean lecithin (SPC) in different proportions. The results of dissolution study