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Identification of Telmisartan as a Unique Angiotensin II: Receptor Antagonist With Selective PPARγ–Modulating Activity
Abstract—The metabolic syndrome is a common precursor of cardiovascular disease and type 2 diabetes that is characterized by the clustering of insulin resistance, dyslipidemia, and increased bloodExpand
Antimalarial Artemisinin Drugs Induce Cytochrome P450 and MDR1 Expression by Activation of Xenosensors Pregnane X Receptor and Constitutive Androstane Receptor
Activation of PXR and CAR and especially the resulting induction of CYP3A4 and MDR1 demonstrate that artemisinin has a higher risk of potential drug interactions than anticipated previously. Expand
Physicochemical Characterization of Berberine Chloride: A Perspective in the Development of a Solution Dosage Form for Oral Delivery
The physicochemical characteristics of berberine chloride and the complexation of drug with 2-hydroxypropyl-β-cyclodextrin (HPβCD) were evaluated and the feasibility of developing an oral solution dosage form of the drug was demonstrated. Expand
Mollamides B and C, Cyclic Hexapeptides from the Indonesian Tunicate Didemnum molle
Two new cyclic hexapeptides, mollamides B and C, were isolated from the Indonesian tunicate Didemnum molle along with the known peptide keenamide A and mollamide B and show cytotoxicity against several cancer cell lines. Expand
Cycloartane glycosides from Sutherlandia frutescens.
Four new cycloartane glycosides, sutherlandiosides A-D (1-4), were isolated from the South African folk medicine Sutherlandia frutescens and their structures established by spectroscopic methods andExpand
Current progress in the chemistry, medicinal chemistry and drug design of artemisinin based antimalarials.
This review covers developments in relation to artemisinin-based antimalarial agents and the contribution of these efforts towards rational drug design in order to access potent, non-toxic antimalaria drugs based on art Artemisinin. Expand
Type 2 diabetes and oral antihyperglycemic drugs.
The pros and cons of the six classes of oral hypoglycemic drugs available to treat Type IIabetes are presented and some of the latest advances towards the development of new drugs for the treatment of Type II diabetes are discussed. Expand
Resistance to artemisinin of malaria parasites (Plasmodium falciparum) infecting alpha-thalassemic erythrocytes in vitro. Competition in drug accumulation with uninfected erythrocytes.
The increase in IC50 values for the parasites infecting variant erythrocytes was also related to the decrease in parasite accumulation, indicating that drug accumulation capacity of the parasite also has a role in determining drug sensitivity. Expand
Rapid determination of artemisinin and related analogues using high-performance liquid chromatography and an evaporative light scattering detector.
This paper describes a high-performance liquid chromatographic method developed and validated for artemisinin and several analogues of art Artemisinin using a readily available evaporative light scattering detector and was found to be straight forward, rapid, inexpensive and reproducible. Expand
Structure-activity relationships of the antimalarial agent artemisinin. 6. The development of predictive in vitro potency models using CoMFA and HQSAR methodologies.
CoMFA and HQSAR models were developed having statistically excellent properties, which also possessed good predictive ability for test set compounds and did an outstanding job in statistical analysis and also handled predictions well. Expand