Chromatographic conditions in the expression of corticosteroid receptor specificity

Summary It is shown that cytosol preparations bound with various concentrations of a steroid are necessary to reveal physicochemically distinct, heterogeneous and polymorphic receptors present in the hormone specific target organ, that these cannot be fully appreciated in one-shot experiments at suboptimal steroids levels, and that they escape detection by equilibrium binding and Scatchard analysis alone.     

Effect of various factors on the activity of trehalase from the larvae ofSesamia inferens walker (Insecta)

Summary Trehalase from the salivary glands and the midgut ofSesamia inferens showed optimum activity at pH 5.8, and at temperatures of 50 and 60°C respectively. The increase in the incubation period, enzyme concentration, and substrate concentration respectively increased the end-product, the hydrolysis, and the rate of hydrolysis of the substrate. Dialysis did not affect, tryptophan accelerated, and other amino acids and end-product inhibited the enzyme activity.The author wishes to express his thanks to ProfessorR. Rakshpal for his constructive criticism, and to University Grants Commission, India, for awarding a Junior Research Fellowship.     

AGPAT2 is mutated in congenital generalized lipodystrophy linked to chromosome 9q34

Congenital generalized lipodystrophy is an autosomal recessive disorder characterized by marked paucity of adipose tissue, extreme insulin resistance, hypertriglyceridemia, hepatic steatosis and early onset of diabetes. We report several different mutations of the gene (AGPAT2) encoding 1-acylglycerol-3-phosphate O-acyltransferase 2 in 20 affected individuals from 11 pedigrees of diverse ethnicities showing linkage to chromosome 9q34. The AGPAT2 enzyme catalyzes the acylation of lysophosphatidic acid to form phosphatidic acid, a key intermediate in the biosynthesis of triacylglycerol and glycerophospholipids. AGPAT2 mRNA is highly expressed in adipose tissue. We conclude that mutations in AGPAT2 may cause congenital generalized lipodystrophy by inhibiting triacylglycerol synthesis and storage in adipocytes.     

The selective esterification of the 5′-hydroxyl of thymidine

Zusammenfassung Ein einfacher Weg zur selektiven Esterbildung mit der 5-Hydroxylgruppe von Thymidin wird beschrieben. Beispiele: Thymidin-5-phosphat, Thymidin-5-sulfat und Thymidin-5-trichloracetat.     

Lack of conversion of C29-phytosterols to cholesterol in the khapra beetle,Trogoderma granarium Everts

Summary Metabolic studies in which³H-sitosterol,³H-stigmasterol, and¹⁴C-desmosterol were administered by feeding and injection to the khapra beetle,Trogoderma granarium Everts, provided strong evidence that this insect is unable to dealkylate phytosterols and convert them to cholesterol.     

Synthesis of Heterocyclic Ring Systems Using Organometallic Reagents

We developed novel synthetic routes to heterocyclic ring systems by using transition metal-mediated or -catalyzed reactions. A Lewis acid-promoted addition of the propargyl Grignard reagent 2 to the Schiff base 1 followed by a silvermediated oxidative cyclization of the homopropargylamine 3 provided the aryl-substituted pyrrole 4. Combined with a cherroseleetive hydrogenation of the pyrrole ring, this rnethod has been applied to the total synthesis of the biologically active fused indolizidine alkaloids （ ± ）-harmicine and （ ± ）-crispine A. See Fig. 1.     

Effect of chronic alloxan diabetes and insulin administration on intestinal brush border enzymes.

Brush border sucrase and lactase activities are significantly elevated in alloxan-induced chronic diabetes and are restored to control levels after insulin treatment. Alkaline phosphatase and Mg-ATPase levels remain unchanged in diabetes, compared to a control group. Insulin treatment alone to control animals also led to enhanced activities of these enzymes.