Bioactive compounds in Pinang Yaki (Areca vestiaria) fruit as potential source of antifertility agent.

Fruits of Pinang Yaki (Areca vestiaria) are used by the people around Bogani Nani Wartabone as contraseption for men. Extracts from the fruit contain tannin, triterpenoid, flavonoid and saponin which are potential as bioactive compounds. This research aimed at exploring the fractions or bioactive compounds contained in the fruit. The extract was prepared by fractionation using hexane. The fractions were separated and analysed by gas chromatography mass spectrometry (GC-MS) technique. The fractions revealed the presence of five compounds. These compounds were identified by interpretation of mass spectra and comparing their retention time and covate indexes with those from literature. The five compounds are pentadecane, methyl-dodecanate, methyl-tetradecanoate, hexadecanoic acid and methyl-octadecanate.

Identification of light-independent inhibition of human immunodeficiency virus-1 infection through bioguided fractionation of Hypericum perforatum.

BACKGROUND: Light-dependent activities against enveloped viruses in St. John's Wort (Hypericum perforatum) extracts have been extensively studied. In contrast, light-independent antiviral activity from this species has not been investigated. RESULTS: Here, we identify the light-independent inhibition of human immunodeficiency virus-1 (HIV-1) by highly purified fractions of chloroform extracts of H. perforatum. Both cytotoxicity and antiviral activity were evident in initial chloroform extracts, but bioassay-guided fractionation produced fractions that inhibited HIV-1 with little to no cytotoxicity. Separation of these two biological activities has not been reported for constituents responsible for the light-dependent antiviral activities. Antiviral activity was associated with more polar subfractions. GC/MS analysis of the two most active subfractions identified 3-hydroxy lauric acid as predominant in one fraction and 3-hydroxy myristic acid as predominant in the other. Synthetic 3-hydroxy lauric acid inhibited HIV infectivity without cytotoxicity, suggesting that this modified fatty acid is likely responsible for observed antiviral activity present in that fraction. As production of 3-hydroxy fatty acids by plants remains controversial, H. perforatum seedlings were grown sterilely and evaluated for presence of 3-hydroxy fatty acids by GC/MS. Small quantities of some 3-hydroxy fatty acids were detected in sterile plants, whereas different 3-hydroxy fatty acids were detected in our chloroform extracts or field-grown material. CONCLUSION: Through bioguided fractionation, we have identified that 3-hydroxy lauric acid found in field grown Hypericum perforatum has anti-HIV activity. This novel anti-HIV activity can be potentially developed into inexpensive therapies, expanding the current arsenal of anti-retroviral agents.

[Studies on the chemical constituents of Lagotis yunnanensis (II)].

OBJECTIVE: To study the chemical constituents of Lagotis yunnanensis W. W. Smith. METHODS: Compounds were isolated from the ethanolic extract of the title herb by silica gel column chromatography, and their structures were identified by physical and chemical evidences and spectral methods. RESULTS: Seven compounds were isolated and identified as artselaeroside A (1),3-hydroxy-5-methoxy-benzyl alcohol (2), tyrosol (3), glycerin-9'-Z-octadecaenate (4), glycerin-docosanate (5), glycerin-tetracosanate (6), tetracosanoic acid (7), respectively. CONCLUSION: All the compounds were isolated from this plant for the first time.

Reassessment of the phylogenetic position of Caulobacter subvibrioides.

Determination of the 16S rRNA gene sequence of Caulobacter subvibrioides ATCC 15264T (T = type strain) confirmed that this species is a member of the alpha subclass of the Proteobacteria and showed that it is phylogenetically most closely related to the Caulobacter group comprising the species Caulobacter bacteroides, Caulobacter crescentus, and Brevundimonas (Pseudomonas) diminuta, for which 16S rRNA sequences of the type strains are currently available. The closest known relative of strain ATCC 15264T among these species is B. diminuta (level of direct pairwise sequence similarity, 95%). On the basis of its previously determined 16S rRNA sequence (accession number M83797), C. subvibrioides is most closely related to Sphingomonas adhaesiva in the alpha-4 subgroup (level of similarity, 97.7%). Analysis of the hydroxy fatty acids of C. subvibrioides ATCC 15264T showed that the 2-hydroxymyristic acid which is characteristic of the genus Sphingomonas was absent.

Three new cytotoxic metabolites from the marine sponge Plakortis halichondrioides.

Three new cytotoxic compounds, one a cyclic-peroxide-containing acid (5) and the two others alkylated dihydroxy alpha,beta-unsaturated C22 and C21 acids (6 and 7), were isolated from the marine sponge Plakortis halichondrioides, which was collected off the coast of Jamaica. The structures were elucidated through mass and mainly 1D and 2D nmr spectral analysis. All three acids are cytotoxic against P-388 murine leukemia.

Isolation of the non-myristoylated form of a major substrate of protein kinase C (MARCKS) from bovine brain.

A substrate protein of protein kinase C with an apparent molecular mass of 70 kDa has been purified from bovine brain. This protein shares several properties with a major substrate of protein kinase C (myristoylated alanine-rich C kinase substrate; MARCKS). It is heat-stable and copurifies with MARCKS during various steps (ammonium sulfate precipitation and gel filtration). However, its elution from a calmodulin affinity column is different from that of MARCKS. It can be eluted by high ionic strength in the presence of calcium, whereas MARCKS can be eluted only in the absence of calcium. Its earlier elution from a reversed phase column suggests that p70 is less hydrophobic than MARCKS. The electrospray mass spectrum revealed an actual mass of 31,550 +/- 6.5 Da, very far from the apparent molecular mass in SDS-polyacrylamide gel electrophoresis (70,000 Da). This mass is about 200 Da smaller than that of MARCKS determined by mass spectrometry analysis (Manenti, S., Sorokine, O., Van Dorsselaer, A., and Taniguchi, H. (1992) J. Biol. Chem. 267, 22310-22315), close to the value expected for the change due to N-terminal myristoylation (210 Da). N-terminal amino acid sequencing showed that the N terminus is not blocked, and the sequence found for the 10 first amino acids is identical to that deduced from the cDNA sequence of bovine MARCKS. These data clearly establish that this protein is a non-myristoylated form of MARCKS and that the absence of the myristoyl moiety at the N terminus lowers the affinity to calmodulin. The purification performed both from the membrane and the cytoplasmic fractions of bovine brain indicated that this non-myristoylated form represents 20-30% of the MARCKS protein in the cytoplasmic fraction, and less than 5% in the membrane one.

Nonmyristoylated Abl proteins transform a factor-dependent hematopoietic cell line.

N-terminal myristoylation can promote the association of proteins with the plasma membrane, a property that is required for oncogenic variants of Src and Abl to transform fibroblastic cell types. The P210bcr/abl protein of chronic myelogenous leukemia cells is not myristoylated and does not stably transform NIH 3T3 fibroblasts; however, it will transform lymphoid and myeloid cell types in vitro and in vivo, suggesting that myristoylation is not required for Abl variants to transform hematopoietic cells. To test this hypothesis, we introduced point mutations that disrupt myristoylation into two activated Abl proteins, v-Abl and a deletion mutant of c-Abl (delta XB), and examined their ability to transform an interleukin-3-dependent lymphoblastoid cell line, Ba/F3. Neither of the nonmyristoylated Abl proteins transformed NIH 3T3 fibroblasts, but like P210bcr/abl, both were capable of transforming the Ba/F3 cells to factor independence and tumorigenicity. Nonmyristoylated Abl variants did not associate with the plasma membrane in the transformed Ba/F3 cells. These results demonstrate that Abl proteins can transform hematopoietic cells in the absence of membrane association and suggest that distinct functions of Abl are required for transformation of fibroblast and hematopoietic cell types.