RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Alantolactone (AL), one of the main active ingredients in Inula helenium L., has been included in various prescriptions of traditional Chinese medicine. The effects of AL on cytochrome P450 (CYP450) were still unclear. This study evaluated the inhibitory effect of AL on cytochrome P450s in vitro and in vivo. MATERIALS AND METHODS: The inhibitory effects of AL on the CYPs activity were evaluated in human liver microsomes (HLMs) and recombinant cDNA-expressed enzymes incubation system, and then determined by LC-MS/MS based CYPs probe substrate assay. C57BL/6 mice were treated AL orally (0, 25, 50, 100 mg/kg) for 15 days. The inhibitory effects of AL on major Cyps in mice were examined at both the mRNA and enzyme activity levels. RESULTS: AL showed a potent inhibitory effect on CYP3A4 activity with IC50 values of 3.599 (HLMs) and 3.90 (recombinant CYP3A4) µM, respectively. AL strongly decreased CYP3A4 activity in a dose-dependent but not time-dependent way in HLMs. Results from typical Lineweaver-Burk plots showed that AL could inhibit CYP3A4 activity noncompetitively, with a Ki value of 1.09 µM in HLMs. Moreover, activity of CYP2C19 could also be inhibited by AL with IC50 of 36.82 µM. Other CYP450 isoforms were not markedly affected by AL. The inhibition was also validated by in vivo study of mice. AL significantly decreased mRNA expression of Cyp2c and 3a family. CONCLUSION: The study indicates that herb-drug interaction should be paid more attention between AL and drugs metabolized by CYP3A4.
Assuntos
Inibidores das Enzimas do Citocromo P-450/farmacologia , Sistema Enzimático do Citocromo P-450/metabolismo , Lactonas/farmacologia , Sesquiterpenos de Eudesmano/farmacologia , Animais , Sistema Enzimático do Citocromo P-450/genética , Humanos , Fígado/efeitos dos fármacos , Fígado/enzimologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Microssomos Hepáticos/efeitos dos fármacos , Microssomos Hepáticos/enzimologiaRESUMO
By reading ancient acupuncture-moxibustion literature, the authors expound the origin and development of fire needle therapy from its sprout, development and mature stage, reveal the origin of fire needle, development of needling instrument and manipulation methods, indications of fire needle therapy and so on, in order to have a better learning on fire needle therapy and make it applicative in clinic.
Assuntos
Humanos , Terapia por Acupuntura , História , Métodos , China , História Antiga , Medicina na Literatura , AgulhasRESUMO
<p><b>OBJECTIVE</b>To compare therapeutic effects of acupuncture and mosapride in relieving diabetic gastroparesis.</p><p><b>METHODS</b>Forty cases were randomly divided into a treatment group and a control group, 20 cases in each group. The treatment group were treated by acupuncture at Zhongwan (CV 12) and Zusanli (ST 36), and the control group by oral administration of mosapride 5 mg, t. i. d. Their therapeutic effects were evaluated by indexes of therapeutic effect.</p><p><b>RESULTS</b>The total effective rate was 95.0% in the treatment group and 83.3% in the control group with a significant difference between the two groups (P<0.05), and the adverse effect in the treatment group was less than that in the control group (P<0.05).</p><p><b>CONCLUSION</b>Acupuncture can significantly relieve diabetic gastroparesis, the therapeutic effect being better than mosapride, with a less adverse effects.</p>