By using active principles of Chinese medicinal materials as lead compounds soquinoline derivatives have been designed and synthesized.Their chemical structures include bisbenzylisoquinoline,benzyl-isoquinoline and pr...By using active principles of Chinese medicinal materials as lead compounds soquinoline derivatives have been designed and synthesized.Their chemical structures include bisbenzylisoquinoline,benzyl-isoquinoline and protoberberine.Their cardiovascular effects were studied involving α-adrenoceptor,adenosine A_1,A_2 and DPH-calcium channel radioreceptor assays.In addition,calmodulin inhibiting,calcium antagonistic potassium channel blocking and antiplatelet aggre- gation activities were also performed.It was found that compound VI_(19) was a new potassium channe blocker with α-adrenoceptor antagonism,compound V_9,and V_(21) lowered blood pressure on various animal models with negative chronotropic action,compound VI_(13)possessed antiarrhythmic and antifi- brillation action,and it may be a candidate tot clinic evaluation.The structure-activity relationships deduced may provide a theoretical basis for further development of new agents.展开更多
Chromatographic behavior of co-eluted compounds from un-extracted drug-free plasma samples was studied by LC-MS and LC-MS/MS with positive APCI.Under soft gradient,total ion chromatogram（TIC） consisted of two major ...Chromatographic behavior of co-eluted compounds from un-extracted drug-free plasma samples was studied by LC-MS and LC-MS/MS with positive APCI.Under soft gradient,total ion chromatogram（TIC） consisted of two major peaks separated by a constant lower intensity region.Early peak（0.15-0.4 min） belongs to polar plasma compounds and consisted of smaller mass ions（m/z〈 250）;late peak（3.6-4.6 min） belongs to thermally unstable phospholipids and consisted of fragments with mlz〈300.Late peak is more sensitive to variations in chromatographic and MS parameters.Screening of most targeted cardiovascular drugs at levels lower than 50 ng/mL has been possible by LC-MS for drugs with retention factors larger than three.Matrix effects and recovery,at 20 and 200 ng/mL,were evaluated for spiked plasma samples with 15 cardiovascular drugs,by MRM-LC-MS/MS.Average recoveries were above 90%and matrix effects expressed as percent matrix factor（%MF） were above 100%,indicating enhancement character for APCI.Large uncertainties were significant for drugs with smaller masses（m/z〈 250） and retention factors lower than two.展开更多
The paper examines the effects of grapefruit consumption in relation to drugs, obesity and cardiovascular risk factors. The review includes the most updated studies found in Pub-Med. The grapefruit effect refers to th...The paper examines the effects of grapefruit consumption in relation to drugs, obesity and cardiovascular risk factors. The review includes the most updated studies found in Pub-Med. The grapefruit effect refers to the ability of grapefruit juice and supplements to interact with a wide variety of pharmaceuticals, either enhancing or limiting their systemic availability. Due to altering the active dosage of the pharmaceutical, Grapefruit juice is commonly not allowed to be used alongside with many drugs. Naringin is the most important one, which can inhibit absorption of some drugs but more commonly 6’7’-dihydroxybergamottin, which inhibits CYP3A4. Lately, grapefruit has been found both in rats and adults to reduce body weight, blood pressure, improve lipid and hepatic profile and decrease platelet aggregation. These promising results must be followed by additional studies in order to add to the importance of the role and effects of grapefruit as part of our diet.展开更多
文摘By using active principles of Chinese medicinal materials as lead compounds soquinoline derivatives have been designed and synthesized.Their chemical structures include bisbenzylisoquinoline,benzyl-isoquinoline and protoberberine.Their cardiovascular effects were studied involving α-adrenoceptor,adenosine A_1,A_2 and DPH-calcium channel radioreceptor assays.In addition,calmodulin inhibiting,calcium antagonistic potassium channel blocking and antiplatelet aggre- gation activities were also performed.It was found that compound VI_(19) was a new potassium channe blocker with α-adrenoceptor antagonism,compound V_9,and V_(21) lowered blood pressure on various animal models with negative chronotropic action,compound VI_(13)possessed antiarrhythmic and antifi- brillation action,and it may be a candidate tot clinic evaluation.The structure-activity relationships deduced may provide a theoretical basis for further development of new agents.
基金supported by Dean of Scientific Research at Jordan University of Science and Technology(JUST)(No.159/ 2012)
文摘Chromatographic behavior of co-eluted compounds from un-extracted drug-free plasma samples was studied by LC-MS and LC-MS/MS with positive APCI.Under soft gradient,total ion chromatogram（TIC） consisted of two major peaks separated by a constant lower intensity region.Early peak（0.15-0.4 min） belongs to polar plasma compounds and consisted of smaller mass ions（m/z〈 250）;late peak（3.6-4.6 min） belongs to thermally unstable phospholipids and consisted of fragments with mlz〈300.Late peak is more sensitive to variations in chromatographic and MS parameters.Screening of most targeted cardiovascular drugs at levels lower than 50 ng/mL has been possible by LC-MS for drugs with retention factors larger than three.Matrix effects and recovery,at 20 and 200 ng/mL,were evaluated for spiked plasma samples with 15 cardiovascular drugs,by MRM-LC-MS/MS.Average recoveries were above 90%and matrix effects expressed as percent matrix factor（%MF） were above 100%,indicating enhancement character for APCI.Large uncertainties were significant for drugs with smaller masses（m/z〈 250） and retention factors lower than two.
文摘The paper examines the effects of grapefruit consumption in relation to drugs, obesity and cardiovascular risk factors. The review includes the most updated studies found in Pub-Med. The grapefruit effect refers to the ability of grapefruit juice and supplements to interact with a wide variety of pharmaceuticals, either enhancing or limiting their systemic availability. Due to altering the active dosage of the pharmaceutical, Grapefruit juice is commonly not allowed to be used alongside with many drugs. Naringin is the most important one, which can inhibit absorption of some drugs but more commonly 6’7’-dihydroxybergamottin, which inhibits CYP3A4. Lately, grapefruit has been found both in rats and adults to reduce body weight, blood pressure, improve lipid and hepatic profile and decrease platelet aggregation. These promising results must be followed by additional studies in order to add to the importance of the role and effects of grapefruit as part of our diet.
