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AIM To establish an allele specific PCR amplification (ASA-PCR) for determination of the genotype of CYP2D6*10B polymorphism in Chinese subjects. METHODS CYP2D6*10B alleles of 65 healthy Chinese subjects were analyzed by a two-step PCR assay and the correlation of genotype and phenotype was studied. RESULTS There were 20 CYP2D6*10B heterozygous genotypes subjects (wt/m) in 35 very extensive metabolizers (VEMs), which consisted the major part of VEM subjects (57%). Meanwhile, 20 subjects consisting 69% of 29 intermediate metabolizers were CYP2D6*10B homozygous mutant genotypes (m/m). The poor metabolizer was also m/m. The metabolic ratio of CYP2D6*10B m/m subjects were larger than wt/m and wild type, the values were -1.49±0.54, -2.20±0.49 and -2.47±0.61 (P<0.01). CONCLUSION PCR-ASA was shown to be a rapid and specific method. It can be used to study the genetic polymorphism, especially CYP2D6 intermediate metabolism.
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N-acetyltransferase are phase II code proteins with overlapping substrate specifici-DMEs, and two highly similar human NAT gene ty. NAT2 is a polymorphic acetyltransferase gene (designated NAT1 and NAT2) are shown to en- locus and "slow acetylation" in humans is due tonutations in the single coding exon of the NAT2 gene. It was also demonstrated that there exist discrete NAT1 structural variants, and differences in tissue levels of NAT1 among humans are related to specific sequence differences in the NAT1 structural gene. Biochemical studies have shown that NAT1 and NAT2 play an important role in the metabolism of some carcinogens, epidemiological studies have revealed an association between ploy-morphisms of NATs and increased cancer risk.Metabolic phenotypes/genotypes can significantly influence DAN adduct formation and could ultimately lead to alterations in cancer risk. If unequivocal biomarkers of genetic susceptibility to cancer can be developed successfully, then identification of individuals at increased risk would be very helpful in the fields of public health and preventive medicine.
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We observed the effects of 10-hydroxy-decenoic acid ( 10-HDA ) extracted from royal jelly on the immune function of mice. It was showed that after ig or ip administration of 10-HDA, the phagocytosis of mouse peritoneal macrophages to cock red blood cells was inhibited. Although the count of lymphocytes in mouse peripheral blood was not changed after administration of 10-HDA, the in vivo lymphocyte tran- sformation of mice induced by PHA was significantly enhanced. It was also showed in our experiment that after 7d administration of 10-HDA, the content of vitamin C in adrenal glands of mice was significantly increased ( same as after ACTH administration ) . The results of our experiments indicated that 10-HDA has the inhibiting effect on immune function of mice and this effect may be related to enhancing adrenal cortex function.
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0 05).③The level of the expression of AT 1a mRNA of the NO group rats was decreased significantly after hypertension of appeared and that of AT 1b mRNA of the LO group rats increased markedly after Losartan was administered. CONCLUSION Losartan has antihypertensive effects and can reverse myocardial hypertrophy induced by renovascular hypertension. Losartan regulates the mRNAs of the AT 1 receptor subtypes differently, which suggests it possibly has selectivity for AT 1a or AT 1b .
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Hepatic fibrosis in rat induced by intraperitoneal injection of dimethylnitroamine (DMN) was traeted by RNA (4 mg ? kg-1) and CoQ10(2. 5 mg ? kg-1) ,seperately. Normal and pathological groups were compared. In 30, 60 and 90 days treatment, rats were killed for ul-trastructural examination and measurement of serum enzymology, serum amino acids and the quantity of collagenous fibers. The results indicated that, in RNA-treated and CoQ10 treated groups, Aspartate aminotransferase (AST) and Y-glutamyl-transpeptidase(?-GT) were normal, the ratio of albunm to globulin (A/G) had significantly difference compared with controlgroup. In RNA-treated group,L-Alanine:2-Ox-oglutarate Aminotransferase(ALT), monoamine oxidase (MAO) and N-acetyl-?-glucosaminidase (NAG) decreased evidently, serum amino acids increased slightly. Ultrastructural and microscopical examination showed the degree of hepa-tocytic necrosis degeneration and the quantity of collagenous fibers in RNA-treated group were rather mild. It appeared that there were protection effects of RNA on liver enzymology and hepaticfibrosis.
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Triptolide possesses antitumor, anti-inflammatory and immuno-supression activity. 3H-triptolide given intragastrically to rats was rapidly but not totally absorbed. After ig and iv administration of 3H-triptolide to rats, the highest radioactivity level was found in the liver, followed by spleen, lung, kidney, intestine, heart and brain. The radioactivity in organs disappeared slowly. 3H-triptolide in plasma was found to be 64.7% bound to plasma protein. In 21d, the cumulative excretion of radioactivity in urine and feces after ig and iv 3H-triptolide to rats was 67.5% and 61.9% of the total dose, respectively. Among that, the radioactivity was 52.4% and 25.3% of the total dose in feces, respectively. The radioactivity excreted by bile in 24h was 6.73 ? 1.9%. The radioactivity in urine, feces and bile measured by TLC, autoradiography and liquid scintillation count indicated that 3H-triptolide excreted in urine, feces and bile was mainly in unchanged form and a few metabolites was found in urine and feces
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Studies were made on the effect of protoporphyrin in treating the acute liver injury induced by carbon tetrachloride ( CCl4 ) in rabbits and on the liver blood flow, biosynthesis of DNA and protein in liver of mice. The results showed that the protoporphy-rin was able to protect the liver remarkable as evidenced by his-tological studies. And it could inhibit the elevation of serum glut-amic-pyruvic transaminase ( SGPT ) , serum glutamic - oxaloacetic transaminase ( SGOT ) and serum ?-glutamyl- transpeptidase ( S?- GT)also. Protoporphyrin could regulate the metabolism of serum amino -acids in rabbits intoxicated by CCl4 as well. Furthermore,protoporphyrin can improve biosynthesis of DNA and liver protein and it may increase the blood flow in the liver of the mice.
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AIM To establish a high performance liquid chromatographic method (HPLC) to determine the concentration of valsartan in human plasma. METHODS Separation was achieved on the lichrospher C 18 column. The mobile phaseconsisted of pH 3 1 phosphate buffer acetonitrile (53∶47, V/V) was used at a flow rate of 1 0 ml?min -1 . The fluorimetric excitation and emission wavelengths were set at 265 nm and 378 nm, respectively. The plasma samples were acidified with HCl, extracted with ethyl acetate. Separate the organic phase, remove the solvent and then residue was dissolved in mobile phase. RESULTS The retention time of valsartan was 12 5 min. The calibration curves were linear in the range of 5 9～ 2 360 ?g?L -1 . The precision values (RSD) of intra day and inter day were determined to be 2 83%～7 07% and 1 57%～8 41% respectively. The absolute recovery rate were 80 30%?5 13%. The method was applied to determine the peak and valley concentrations in plasma of the hypertensive treated with 80mg valsartan per day. CONCLUSION The assay was sensitive and simple. It is suitable for the study of the pharmacokinetics of valsartan.