Antitumor activity of the Isodon diterpenoids: structural requirements for the activity.

A significant antitumor activity of oridonin (1) and lasiokaurin (2), the kaurene-type diterpenoids of Isodon species, was shown by their i.p. injection to the test mice inoculated by Ehrlich ascites carcinoma. Enmein (8), compounds 9 and 3 were also active under larger dose. Subsequently, the relationship between their chemical structure and antitumor activity was investigated, and the activity of oridonin (1) and lasiokaurin (2) was rationalized in terms of their structural feature.     

3-Hydroxy-3-Methylglutaric acid and triton-induced hyperlipidemia in rats

Summary 3-Hydroxy-3-methylglutaric acid (HMG) significantly decreased cholesterol, triglyceride and phospholipid levels in whole serum, serum -lipoproteins and liver of Triton-induced hyperlipidemic rats. Therapeutically 50 mg HMG/kg is equivalent to 200 mg nicotinic acid/kg in lowering all these lipid parameters. HMG may exert its hypolipidemic effect through inhibition of lipoprotein synthesis.Acknowledgments. We are grateful to Dr.M. Saleemuddin for encouragement, Dr.P. E. Schurr, Upjohn Co. USA for generous gift of Triton W. R 1339 and Lady Tata Memorial Trust (India) for financial assistance to one of us (SYKY).     

3-Hydroxy-3-methylglutaric acid and experimental atherosclerosis in rats

Summary In rats 3-hydroxy-3-methylglutaric acid effectively counteracts the lipemic and atherosclerotic response of massive doses of vitamin D₂. It regressed the formation of atheromatous arterial lesions. Furthermore the significant decrease in serum -lipoprotein levels on HMG treatment could be due to decrease in VLDL triglyceride and cholesterol levels.Acknowledgments. The authors are indebted to Dr.W. Drell, President, Calbiochem, San Diego, California, USA, for generous gift of HMG and Lady Tata Memorial Trust, India, for providing financial assistance to one of us (S.Y.K.Y.).     

Hymenin,a novel α-adrenoceptor blocking agent from the Okinawan marine spongeHymeniacidon sp.

Summary A novel bromine-containing alkaloid, hymenin, has been isolated from the Okinawan marine spongeHymeniacidon sp. as a potent -adrenoceptor blocking agent and its structure determined to be1 on the basis of the spectral data.     

Enzyme-linked immunosorbent assay for measuring serum IgE

Summary Serum IgE was measured by a sandwich method using polystyrene beads coated with anti-IgE -globulin and peroxidase labelled anti-IgE -globulin. The method was simple, and as sensitive as the radioimmunoassay.We are grateful for the skillful assistance of Mrs K. Kobayashi.     

Effects of thyrotrophic-releasing hormone (TRH) on thermoregulation in the rat

Summary At ambient temperatures (T_a) of both 8 and 22°C, intraventricular administration of TRH (10–80 g) produced a dose-dependent hypothermia in rats. The hypothermia was due to both decreased metabolic heat production and cutaneous vasodilatation. In contrast, at 30°C T_a, TRH increased metabolic heat production (due to behavioral excitation) and led to hyperthermia.This work was supported by the grants from the National Science Council of Republic of China and the Pjing-Ling Neurological Foundation (VGH, Taipei, Taiwan).     

Anti-oxidative effect of coenzyme Q10

Summary Coenzyme Q₁₀ is effective as an anti-oxidant like -tocopherol, especially in the heart.     

On the genesis of the soil mantle of the region of Manaus,Central Amazonia,Brazil

Summary The dynamics of the forest to the north of Manaus is tightly linked to that of the soil. The latosol that covers the plateau, which supports a dense forest, consists from top to bottom of: (a) a brown, clayey organic horizon (0.3 m), (b) a yellow horizon, very rich in clay but permeable (from 0.3 to 4 m), (c) a nodular horizon rich in Al and Fe oxides (from 4 to 9 m), and (d) a horizon which still preserves the sedimentary structures of the parent sandstone, where quartz is intensely dissolved and kaolinite crystallizes in pores. In perfectly flat areas, the clay of the organic horizon is destroyed by acidocomplexolysis, and the dissolved Al is transported vertically by the drainage water. A part of this Al is used to make the gibbsite nodules of horizon (c), and the rest is used to make kaolinite in horizon (d). Because aluminum is thus conserved within any vertical prism, the rate of destruction of horizon (a) is equivalent to the rate of advance of the kaolinization zone into the sediment: the latosol is said to be in equilibrium, the surface remains perfectly flat as it slowly sinks, the quantity of kaolinite increases with time, and the silica released by quartz dissolution in the whole profile is exported by drainage water to the water table. In contrast, near drainage axes, however small initially, the drainage becomes inclined toward the axis. Part of the Al released by acidocomplexolysis of horizon (a) is now exported to rivers, and Al is no longer conserved within any given prism. The rate of advance of the kaolinization zone (d) into the sediment now becomes less than the rate of destruction of horizon (a) and the surface sinks faster than that of the surrounding plateau. After this differential podzolization has gone on long enough, it creates a network of geochemical valleys characterized by convex slopes and bounded by sandy soils (campinas). The vegetation becomes sparser and sparser. At the end, only some bushes and lichens survive on the white sand.Acknowledgments. The authors are indebted to Dr E. Merino (Dept. of Geology, Indiana University) for helpful criticisms and suggestions. This research was carried out in I.N.P.A. (Instituto Nacional de Pesquisas da Amazonia) and was financially supported by the CNPq-CNRS/ORSTOM conv.