piperidines and chloroquine-diphosphate

In previous studies, Cassia spectabilis DC leaf has shown a good antiplasmodial activity. Therefore, this study is a follow-up study of the extract of leaf of C. spectabilis DC on its in vitro and in vivo antiplasmodial activity and mechanism as an antimalarial.. The extract was fractionated, sub-fractionated and isolated to obtain the purified compound. In vitro antiplasmodial activity test against Plasmodium falciparum to find out the active compound. In vivo test against P. berghei ANKA-infected mice was conducted to determine prophylactic activity and antiplasmodial activity either alone or in combination with artesunate. The inhibition of heme detoxification test as one of the antimalarial mechanisms was carried out using the Basilico method.. C. spectabilis DC leaf possessed potent antiplasmodial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.

Topics: Animals; Antimalarials; Artesunate; Cassia; Chloroquine; Heme; Ketones; Malaria; Male; Mice, Inbred BALB C; Phytotherapy; Piperidines; Plant Extracts; Plant Leaves; Plasmodium berghei; Plasmodium falciparum

This paper describes a novel and sensitive method for the estimation of chloroquine phosphate (CQ) using capillary electrophoresis with end-column electrochemiluminescence (ECL) detection. Under the optimized condition, linear calibration curve was obtained for the system over two orders of magnitude with a detection limit of 3x10(-7) M (S/N=3). The relative standard deviations of the ECL intensity and the migration time were 1.4% and 0.05%, respectively (n=6, 5x10(-5) M CQ). Successful separation of chloroquine phosphate, difenidol hydrochloride and clomifene citrate was obtained at pH 7.0. Using the proposed electrochemiluminescence system, a simple method was proposed to study the interaction between chloroquine phosphate and human serum albumin (HSA), and the number of binding sites and binding constant were estimated to be 32.6 and 7.7x10(3) M(-1), respectively.

Topics: Binding Sites; Chloroquine; Clomiphene; Electrochemistry; Electrophoresis, Capillary; Humans; Luminescent Measurements; Organometallic Compounds; Piperidines; Reproducibility of Results; Sensitivity and Specificity; Serum Albumin

Topics: Animals; Antimalarials; Chloroquine; Dimethylpolysiloxanes; Drug Implants; Malaria; Male; Mefloquine; Mice; Mice, Inbred Strains; Naphthoquinones; Piperidines; Plasmodium berghei; Primaquine; Proguanil; Pyrimethamine; Quinolines; Silicone Elastomers; Sulfadiazine; Triazines