ABSTRACT
AIM@#To investigate the quinoline alkaloids from the roots of Dictamnus angustifolius G.Don ex Sweet (Rutaceae).@*METHOD@#The quinoline alkaloids were isolated by various column chromatographic methods and their structures were elucidated on the basis of spectral analysis.@*RESULTS@#A new quinoline alkaloid, 5-methoxylrobustine (1), along with five known quinoline alkaloids were obtained, and their structures were identified as dictamnine (2), robustine (3), isopteleine (4), γ-fagarine (5), and skimmianine (6). Cytotoxicity testing of these alkaloids showed that all of them had weak cytotoxic activities against human breast cancer cells (MCF7).@*CONCLUSION@#Compound 1 is a new quinoline alkaloid. Alkaloid 3 showed stronger anti-proliferation effect than the other alkaloids.
Subject(s)
Humans , Antineoplastic Agents, Phytogenic , Pharmacology , Therapeutic Uses , Breast Neoplasms , Drug Therapy , Cell Line, Tumor , Dictamnus , Chemistry , Hydroxyquinolines , Chemistry , Pharmacology , Therapeutic Uses , Molecular Structure , Phytotherapy , Plant Extracts , Chemistry , Pharmacology , Therapeutic Uses , Plant Roots , Chemistry , Quinolines , Chemistry , Pharmacology , Therapeutic UsesABSTRACT
This study was performed to evaluate the efficacy of 1-Butyl-3-[2E-3-[dimethylamino] prop-2 enoyl] 4-hydroxyquinoline-2 [IH]-one [BDHQ] when given to hamsters after infection with Schistosoma haematobium [350 +/- 50 cercariae/hamster]. The drug was prepared as an aqueous suspension by suspending 100, 150, 200 mg in 10 mI of vehicle for each hamster [mg/kg body weight]. Praziquantel was prepared as an aqueous suspension by dissolving 150 mg of the vehicle to estimate the schistosomal worms and ova/tissues were counted in the hepatic and intestinal tissues. The data of the present work revealed that the percentage reduction in number of worms recovered after oral administration of [BDHQ] ranged between 40% and 98% when compared with the control. As regards the worm burden and distribution, the percent of worms recovered from the liver was ranged between 21% and 50%. While those recovered from portomesentric veins reached 70% to 98%. Beside during in vivo study, the effect of oral administrate of hydroxy quinoline [BDHQ] on ova tissue count of Schistosoina hac'matobiu, n. The number of ova per gram tissue is also an important criterion for the evolution of both magnitude of infection and efficacy of antischistosomal agents. In this study when the infected hamster treated with [BDHQ] at a dose of 100mg/kg body weight. Tissue egg count significantly decline by 40.2% in intestine, six weeks after treatment, moreover the tissue egg count significantly declined by 43.9% in liver and 40.2% intestine, when the infected hamster were treated with BDHQ at a dose 150mg/kg b.w. beside at dose 200mg/kg b.w, the percentage reduction in ova count unchanged significantly when compared with PZQ treated hamsters which represented by 60% in number of ova count
Subject(s)
Male , Animals, Laboratory , Hydroxyquinolines , Cricetinae , MaleABSTRACT
To study the chemical constituents of the mycelia of the Endophytes YD-01, 2, 3-dihydroxy-quinoline-4-O-beta-D-glucopyranoside (1), 3-methyl-pyrrol opiperazine-2, 5-dione (2) and naringenin (3) were isolated from its acetone extracts by using silica gel column chromatography and Sephadex LH-20. Their structures were elucidated on the basis of spectroscopic analysis. Compound 1 is a new compound.
Subject(s)
Alternaria , Chemistry , Diketopiperazines , Chemistry , Flavanones , Chemistry , Glucosides , Chemistry , Hydroxyquinolines , Chemistry , Molecular Structure , Mycelium , Chemistry , Pyrroles , ChemistryABSTRACT
En 1958 el autor describe junto con el Dr. Régulo Pachano el primer caso de acro-dermatitis enteropática en Venezuela en un niño de seis años de edad, quien respondió favorablemente a la diiodohidroxiquinolona. Posteriormente, el autor reúne 13 nuevos casos de la enfermedad, todos procedentes del barrio San Francisco, situado al Sur de la ciudad de Maracaibo, todos los cuales eran hijos de padres consanguíneos. El tratamiento con diiodohidroxiquinolona en estos casos, produjo el mismo efecto favorable constatado en el primer caso. Dos de los pacientes que habían evolucionado favorablemente con el tratamiento, presentaron una recidiva de la enfermedad que no fue posible controlar, aun con altas dosis de la droga y que curaron con la aplicación de una nueva terapéutica de la enfermedad a base de sulfato de zinc. Después de hacer una revisión de los casos observados desde 1958, el autor analiza la etiopatogenia de la enfermedad, su terapéutica y, en particular, el papel del zinc en patología humana, así como la toxicidad de los derivados halogenados de la hidroxiquinolona
Subject(s)
Humans , Male , Female , Acrodermatitis/complications , Dermatitis/complications , Hydroxyquinolines/adverse effectsABSTRACT
Inhibition of photosystem II (PS II) activity by 8-hydroxyquinoline (8-HQ) has been investigated in case of spinach chloroplasts and isolated photosystem II particles using the thermoluminescence technique. In presence of 8-HQ, water to methylviologen (MV) photoreduction in isolated chloroplasts is inhibited while the reduction of dichlorophenol indophenol is inhibited in both chloroplasts as well as in photosystem II particles. The activity can be restored fully by addition of diphenylcarbazide (DPC), suggesting that the donor side of water oxidation complex is affected. The changes in the thermoluminescence peaks indicate that the charge recombination processes involving S2 or S3 states of the Kok's cycle are probably affected by 8-HQ treatment.