Drug glucuronidation and disposition in brain / 药学学报

UDP-glucuronosyltransferase (UGT), a kind of phase II drug-metabolizing enzyme, catalyzes the conjugation of glucuronic acid and drugs. UGTs are widely expressed in brain, but at a relatively low level compared to that in liver. Brain UGTs are inducible or inhibitable, which influences the drug distribution in the central nervous system. UGTs, cytochrome P450 (CYPs) and transporters act together to effect pharmacokinetics of drugs in brain. Several drugs have the capacity to cross the blood brain barrier after glucuronidation and certain drugs may be subject to direct glucuronidate in brain by the function of UGTs. The brain UGTs' isoforms, localization, induction, inhibition, and interaction with CYP and transporters are introduced in this review. The process of drug glucuronidation and distribution in brain is summarized for five drugs. A deep insight into the process of drug metabolism and distribution in brain may provide a valuable reference for drug design for the central nervous system.

The effect of baicalin on human brain microvascular endothelial cell under the glucose deprivation combined with hypoxia condition / 中国应用生理学杂志

<p><b>OBJECTIVE</b>To investigate the mechanisms of baicalin on anti-cerebral ischemic through observing the effect of baicalin on human brain microvascular endothelial cell under the glucose deprivation combined with hypoxia condition.</p><p><b>METHODS</b>Human brain microvascular endothelial cells (HBMVECs) cultured in vitro were divided into the following groups: normal group, model group, baicalin high dose group, baicalin middle dose group, baicalin low dose group, nimodipine group. The kits were used to detect the cell viability, leakage rate of lactate dehydrogenase (LDH), Na(+)-K(+)-ATPase, Ca(2+)-ATPase, the concentration of Ca2+ in each group, and apoptosis rates of each group were analyzed by flow cytometry (FCM).</p><p><b>RESULTS</b>Compared with the normal group, the cell viability, Na(+)-K(+)-ATPase and Ca(2+)-ATPase in model group decreased significantly (P < 0.01, P < 0.05). But the leakage rate of LDH, Ca2+ in cells and apoptosis rates increased remarkably (P < 0.01). Compared with the model group, the cell viability, Na(+)-K(+)-ATPase and Ca(2+)-ATPase increased obviously (P < 0.01, P < 0.05) in baicalin high dose group. But the leakage rate of LDH and Ca2+ in cells in baicalin high dose group decreased significantly comparing with that of model group (P < 0.05, P < 0.01). And the reduction of intracellular Ca2+ was superior to that of nimodipine group. Meanwhile, the apoptosis rates decreased significantly in both baicalin high and middle dose groups (P < 0.01).</p><p><b>CONCLUSION</b>Baicalin could improve the cell viability of HBMVECs under the glucose deprivation combined with hypoxia condition. And the mechanisms were related with improving the energy metabolism, inhibiting intracellular calcium overload and decreasing the apoptosis rate of cells further.</p>

Clinical observation on simple obesity treated by acupuncture / 中国针灸

<p><b>OBJECTIVE</b>To evaluate the effectiveness and safety of simple obesity treated by acupuncture.</p><p><b>METHODS</b>By randomized single-blind clinical trial, one hundred and eighteen cases of simple obesity were divided into an acupuncture group (76 cases) and a placebo-acupuncture control group (42 cases), additionally, health control group (30 cases) was included. In acupuncture group and placebo-acupuncture control group, all the patients received a restricted diet; Zhongwan (CV 12) and Zhongji (CV 3) etc. at abdomen and Liangqiu (ST 34) and Zusanli (ST 36) etc. at limbs were selected; body mass index (BMI), Serum Total Cholesterol, triglyceride (TG), Glucose, Creatinine, urea nitrogen (BUN), Uric Acid and adverse reactions scores were observed.</p><p><b>RESULTS</b>After treatment the BMI in acupuncture grown was lower than that in placebo-acupuncture control group (P < 0.01). In metabolism indices, the serum Total Cholesterol and Glucose after treatment were reduced obviously than those before treatment in acupuncture group (all P < 0.01), and there was no significant differences in other metabolism indices (all P > 0.05) in two groups. After treatment, in adverse reactions scores, the hunger sensation scores in acupuncture group was reduced than that in placebo-acupuncture control group (P < 0.05), and there was no significant differences in other indices (all P > 0.05).</p><p><b>CONCLUSION</b>BMI of simple obesity was reduced by acupuncture, and the Serum Total Cholesterol and Glucose were reduced accordingly. The adverse reac tions such as weakness, nervosa and diarrhea, etc. doesn't appear after acupuncture treatment. Acupuncture therapy is one of the safe and effective methods for simple obesity.</p>