Furocaulerpin,a new acetylenic sesquiterpenoid from the green algaCaulerpa prolifera

Summary Furocaulerpin, an acetylenic sesquiterpenoid possessing a furan ring, has been isolated from the marine algaCaulerpa prolifera, and its stereostructure elucidated mainly on the basis of physico-chemical data.This work was carried out in the frame work of the Progetto Finalizzato per l'Oceanografia e i Fondi Marini, CNR, Rome. Thanks are due to the Centro di Metodologie Chimico-Fisiche of the University of Naples (Mr I. Giudicianni) for the determination of PMR-spectra.     

An investigation of the interaction between isoniazid and the contraceptive steroid norethindrone in vivo

Summary Isonicotinic acid hydrazide (isoniazid) was shown to react readily with 17-ethinyl-17-hydroxyestr-4-en-3-one (norethindrone) to form the isonicotinyl hydrazone of the steroid under conditions likely to exist in the stomach. The hydrazone was detected in guinea-pig, but not rat, plasma following its oral administration. Rat liver tissue metabolized the compound more rapidly than guinea-pig liver in vitro which probably accounts for the failure to detect the hydrazone in rat plasma.     

9-α-hydroxyparthenolide,a novel antitumor sesquiterpene lactone fromAnvillea garcini (Burm.) DC1

Summary A novel sesquiterpene lactone, 9--hydroxyparthenolide (1) was isolated from a chloroform extract ofAnvillea garcini that was collected in Iran. The structure of1 was assigned on the basis of high field NMR decoupling experiments and other spectroscopic evidence. This -methylene lactone has shown significant activity in both the 9KB cell culture and P388 mouse leukemia test systems.The authors acknowledge the support of contract No. N01-CM-97296 from the National Cancer Institute and the use of the Purdue University Biochemical Magnetic Resonance Laboratory (NIH grant No. RR01077). This is paper 16 in the series Potential Antitumor Agents.     

Inhibition of rat liver glutamine synthetase by phosphonic analogues of glutamic acid

Summary Analogues of glutamic acid, -methylglutamic acid and glutamine in which the -or -COOH groups are replaced by PO₃H₂ or P(O)(OH₃)OH functions competitively inhibit rat liver glutamine synthetase. The K₁ values are comparable to or lower than K_M for L-glutamate.This study was supported by grant R.1.9.     

Failure of somatostatin to influence experimental tumor cell growth in vivo and in vitro

Summary The influence of somatostatin on tumor cell growth was studied in vivo in mice (sarcoma 180 ascites tumor and Lewis lung tumor) and in vitro on nontransformed and polyoma-transformed cell lines. 4 or 20 g/100 g of cyclic somatostatin and 4 g/100 g of linear protamin Zn-bound somatostatin were injected s.c. twice daily in the in vivo study. Cyclic somatostatin (1, 4 or 10 g/ml) was added twice daily to the cell cultures. Somatostatin administration influenced neither the survival of animals nor the growth rate of cultured cell lines. *** DIRECT SUPPORT *** A2025117 00011     

Inhibitory tripeptide,Lys-Phe-Tyr,as a fragment of physalaemin

Summary Several peptides were separated from-chymotrypsin-treated physalaemin by high voltage paper electrophoresis, and inhibition of the excitability of a molluscan giant neurone (tonically autoactive neurone) by the tripeptide, Lys-Phe-Tyr, was demonstrated.We thank Dr Sadaaki Iwanaga of Osaka University and Dr Atsuo Inoue of Daiichi Pharmaceutical CO for their helpful advice and the donation of the tripeptide (Lys-Phe-Tyr).     

Synthetic identification as a hexapeptide of alpha substance-IB inducing sexual agglutination in Saccharomyces cerevisiae.

For the identification of a peptidyl principle inducing sexual agglutination in the yeast, 2 supposed hexapeptides (1a, b) were synthesized by the conventional method. The 1a (H-Arg-Gly-Pro-Phe-Pro-Ile-OH) revealed complete identity with the natural peptide in TLC, MS and biological property on agglutination. The 1b showed the sexual agglutinability in the same degree as 1a, though distinct differences were observed in the chemical data. Both 1a and 1b had a strong bitter taste.     

In vivo effects of Escherichia coli endotoxin on sulfobromophthalein clearance in the guinea-pig.

In vivo studies indicated that the primary effects of E. coli endotoxin on hepatic clearance of sulfobromophthalein were at the excretory level. Newborns were more sensitive to the LPS than older animals.