Synthesis of some novel imidazolinones as potent anticonvulsant agents.

Imidazolinone derivatives of IIa-IIc, IIIa-IIIf and IVa-IVf have been synthesised by the condensation of some known sulpha drugs with 5-oxazolone derivatives, which were prepared by Erlenmeyer condensation of benzoyl glycine with different aldehydes in the presence of sodium acetate and acetic anhydride. The constitution of the products has been supported by elemental analysis and IR, 1H-NMR spectral data. The products have been screened for their (a) in vitro growth inhibitory activity against several microorganisms and (b) in vivo anticonvulsant activity.

Picrorhiza kurroa (Kutaki) Royle ex Benth as a hepatoprotective agent--experimental & clinical studies.

Picrorhiza kurroa (Pk), a known hepatoprotective plant, was studied in experimental and clinical situtations. The standardization of active principles--Picroside 1 and 2 was done with High Performance Liquid Chromatography. Picroside 1 ranged from 2.72 to 2.88 mg/capsule and picroside 2 from 5.50 to 6.00 mg/capsule. In the galactosamine-induced liver injury in rats, Pk at a dose of 200 mg/kg p.o. showed a significant reduction (p < 0.05) in liver lipid content, GOT and GPT. In a randomised, double-blind placebo controlled trial in patients diagnosed to have acute viral hepatitis (HBsAg negative), Pk root powder 375 mg three times a day was given for 2 weeks (n = 15) or a matching placebo (n = 18) was given. Difference in values of bilirubin, SGOT and SGPT was significant between placebo and Pk groups. The time in days required for total serum bilirubin to drop to average value of 2.5 mg% was 75.9 days in placebo as against 27.44 days in Pk group. The present study has shown a biological plausability of efficacy of Pk as supported by clinical trial in viral hepatitis, hepatoprotection in animal model and an approach for standardizing extracts based on picroside content.

Erythrocyte glucose-6-phosphate dehydrogenase status of newborns and adults in eastern Libya.

One hundred and twenty cord and 320 venous blood samples were collected from Libyan newborns and adults respectively for the estimation of glucose-6-phosphate dehydrogenase (G-6-PD) activity by a screening technique and by quantitative estimation. The mean (S.D.) enzyme activity in the non-deficient neonates and adults was 1.13 (0.23) and 0.87 (0.21) IU/ml RBC/min respectively. The incidence of G-6-PD deficiency in the male population was 2.8%. The enzyme activity in the deficient male population ranged from 0-19.5%; none of them was symptomatic or had haematological abnormality. Of the female subjects 1.8% had enzyme activity of 50-65%. The frequency of enzyme deficiency appears to be low compared with that found in other Arab populations and is comparable with the incidence in other mediterranean countries.

Incidence of hepatitis B (Australia) antigen among three communities in malarial Western Maharashtra, India.

The incidence of hepatitis B surface antigen (HBs Ag, Australia antigen) has been determined in three communities residing in an endemic malarial region in Western Maharashtra. A high incidence (5.92%) is found in the Marathas, a socially well-placed community, as compared to Nava-Buddhas (2.62%) and scheduled castes (1.63%) which are socially low-placed communities. A higher incidence (8.91%) among the Maratha females is a surprising observation as the males have been shown to be predominant among HBs Ag carriers in most world populations. A positive association of HBs Ag and the anthropometric traits, skinfold thickness of biceps and triceps, has been observed in the present study. The results demonstrate that other factor(s) (e.g. immunological) besides malarial infection may be involved in the maintenance of a high HBs Ag frequency in Western Maharashtra.

Further evidence for oxidative damage to hemoglobin and red cell membrane in leukemia.

The presence of significant methemoglobinemia in a large number (79%) of cases of leukemia prompted us to look into the evidence for oxidative injury to the other red cell constituents, e.g. the cell membrane. Forty-five per cent of cases showed increased malonyldialdehyde (MDA) levels indicating in vivo peroxidation of membrane lipids in leukemia patients. Red cell superoxide dismutase (SOD) activity was reduced in 25% of cases while plasma alpha-tocopherol levels were markedly low in 68% of patients. The presence of an inverse correlation between MDA levels and SOD and tocopherol levels in a large number of cases suggested that the red cells in leukemia lack the ability to counter increased oxidative stress. Low hemoglobin content of the red cells in these patients seemed to contribute to the oxidative injury to the membrane by rendering the latter more accessible to the oxidants. While methemoglobinemia may enhance tissue hypoxia, membrane lipid peroxidation could explain the shortened erythrocyte life-span and anemia in leukemia.

Hereditary high-adenosine triphosphate syndrome: study of a new variant.

A new variant of hereditary hemolytic anemia in a family due to high adenosine triphosphate (ATP) is reported. The increase in ATP levels varied from 83 to 105% in the family members. Low 2,3-diphosphoglycerate levels and low 2,3-diphosphoglyceromutase activity were observed in three family members, with normal glucose-6-phosphate dehydrogenase and pyruvate kinase activity.

Tolerability of ibuprofen and flurbiprofen in G-6-PD deficient subjects: in vitro study.

1 A 'GSH (reduced glutathione) stability test' which consists of incubating blood samples with acetylphenylhydrazine and other test drugs and measuring GSH level before and after incubation, was carried out. 2 Application of this test to the blood of eight normal volunteers and twelve known G-6-PD deficient persons demonstrated that acetylphenylhydrazine and primaquine produced a significant decrease in GSH levels in G-6-PD deficient red cells compared to the reduction seen in normal red cells incubated with these drugs. No such change was observed with aspirin, ibuprofen and flurbiprofen. 3 The results of this in vitro study seem to indicate that ibuprofen and flurbiprofen are relatively innocuous in G-6-PD deficient individuals.