SOLID-PHASE PEPTIDE SYNTHESIS OF ISOTOCIN WITH AMIDE OF ASPARAGINE PROTECTED WITH 1-TETRALINYL. TRIFLUOROMETHANESULPHONIC ACID (TFMSA) DEPROTECTION, CLEAVAGE AND AIR OXIDATION OF MERCAPTO GROUPS TO DISULPHIDE

Isotocin, a nonapeptide amide, was synthesised on a benzhydryl-resin using the Boc-strategy. Benzyl group was used in the protection of the side-chains of tyrosine, serine and cysteine. Tetralinyl group was used to protect asparagine side-chain. TFMSA-TFA-thioanisole-1,2-ethanedithiol (2:20:2:1 v/v) was used on the peptide-resin under different cleavage conditions to obtain isotocin in a one-pot reaction. The cleavage at 40 ° C for two hours gave isotocin quantitatively. Isotocin could be isolated in 61% yield. (Received February 13, 2001; revised August 31, 2001) Bull.Chem.Soc.Ethiop. 2001, 15(2), 143-15

8-Methoxyneorautenol and radical scavenging flavonoids from Erythrina abyssinica

A new pterocarpan (named 8-methoxyneorautenol) was isolated from the acetone extract of the root bark of Erythrina abyssinica. In addition, the known isoflavonoid derivatives eryvarin L, erycristagallin and shinpterocarpin were identified for the first time from the roots of this plant. The structures were determined on the basis of spectroscopic evidence. The new compound showed selective antimicrobial activity against Trichophyton mentagrophytes. The acetone extract of the root bark of E. abyssinica showed radical scavenging activity towards 2,2-diphenyl-1-picrylhydrazyl radical (DPPH). The pterocarpenes, 3-hydroxy-9-methoxy-10-(3,3- dimethylallyl)pterocarpene and erycristagallin, were the most active constituents of the roots of this plant and showing dose-dependent activities similar to that of the standard quercetin

<b>8-Methoxyneorautenol and radical scavenging flavonoids from <i>Erythrina abyssinica</i></b>

A new pterocarpan (named 8-methoxyneorautenol) was isolated from the acetone extract of the root bark of <i>Erythrina abyssinica</i>. In addition, the known isoflavonoid derivatives eryvarin L, erycristagallin and shinpterocarpin were identified for the first time from the roots of this plant. The structures were determined on the basis of spectroscopic evidence. The new compound showed selective antimicrobial activity against <i>Trichophyton mentagrophytes</i>. The acetone extract of the root bark of <i>E. abyssinica</i> showed radical scavenging activity towards 2,2-diphenyl-1-picrylhydrazyl radical (DPPH). The pterocarpenes, 3-hydroxy-9-methoxy-10-(3,3-dimethylallyl)pterocarpene and erycristagallin, were the most active constituents of the roots of this plant and showing dose-dependent activities similar to that of the standard quercetin

Isolation and in vitro antiplasmodial activities of alkaloids from Teclea trichocarpa: in vivo antimalarial activity and X-ray crystal structure of normelicopicine.

Seven alkaloids have been isolated from Teclea trichocarpa including four, normelicopicine (1), arborinine (2), skimmianine (6), and dictamnine (7), that are reported for the first time in addition to the previously reported alkaloids melicopicine (3), tecleanthine (4), and 6-methoxytecleanthine (5). The structure of 1 was confirmed by single-crystal X-ray crystallography. Two alkaloids, 1 and 2, displayed limited in vitro activities against Plasmodium falciparum strains HB3 and K1, but there appeared to be little cross-resistance with chloroquine. Alkaloid 1 was found to have some activity against P. berghei in mice (32% suppression of parasitaemia at a dose of 25 mg x kg(-1) x day(-1)), but unlike chloroquine it did not inhibit beta-haematin formation in a cell-free system; 1 was found to have low in vitro cytotoxicity to KB cells (IC50 > 328 microM)