The structures of three new cucurbitane-type triterpenoids isolated from the methanol extract of the fruit of Japanese Momordica charantia were established as (19R,23E)-5beta,19-epoxy-19-methoxycucurbita-6,23,25-trien-3beta-ol (1), (23E)-3beta-hydroxy-7beta-methoxycucurbita-5,23,25-trien-19-al (2), and (23E)-3beta-hydroxy-7beta,25-dimethoxycucurbita-5,23-dien-19-al (3) on the basis of spectroscopic methods. These compounds were accompanied by the known (19R,23E)-5beta,19-epoxy-19,25-dimethoxycucurbita-6,23-dien-3beta-ol (4) and (19R,23E)-5beta,19-epoxy-19-methoxycucurbita-6,23-diene-3beta,25-diol (5). This is the first report of the isolation of tetracyclic triterpenoids possessing a delta23,25-conjugated diene system, viz., 1 and 2, from a natural source.

Amplification of chirality has been reported in polymeric systems. It has also been shown that related effects can occur in polymer-like dynamic supramolecular aggregates, if a subtle balance between noncovalent interactions allows the coupling between a chiral information and a cooperative aggregation process. In this context, we report a strong majority-rules effect in the formation of chiral dynamic nanotubes from chiral bisurea monomers. Furthermore, similar helical nanotubes (with the same circular dichroism signature) can be obtained from racemic monomers in a chiral solvent. Competition experiments reveal the relative strength of the helical bias induced by the chiral monomer or by the chiral solvent. The nanotube handedness is imposed by the monomer chirality, whatever the solvent chirality. However, the chirality of the solvent has a significant effect on the degree of chiral induction.

AO-0002 was suggested to have a different anti-influenza virus action to that of oseltamivir and was verified to show anti-influenza activity in vitro and in vivo.

The methanol extract of galangal (the rhizomes of Alpinia officinarum L.) exhibited remarkable antitumor-promoting activity on an in vivo two-stage carcinogenesis test of mice using 7,12-dimethylbenz[a]anthracene as an initiator and 12-O-tetradecanoylphorbol-13-acetate (TPA) as a promoter. Seven diarylheptanoids (1-7) were isolated and identified from the active fraction of the methanol extracts of the galangal. These compounds, 1-7, were evaluated for their inhibitory effects on TPA-induced inflammation (1 microg/ear) in mice. These compounds (1-7) tested showed marked anti-inflammatory effects, with a 50% inhibitory dose of 0.8-2.7 micromol/ear.

Seventeen cucurbitane-type triterpenoids, 1-17, including six new compounds, (23E)-3β,25-dihydroxy-7β-methoxycucurbita-5,23-dien-19-al (1), (23S*)-3β-hydroxy-7β,23-dimethoxycucurbita-5,24-dien-19-al (6), (23R*)-23-O-methylmomordicine IV (7), (25ξ)-26-hydroxymomordicoside L (8), 25-oxo-27-normomordicoside L (9), and 25-O-methylkaravilagenin D (12), were isolated from a MeOH extract of the leaves of Japanese Momordica charantia. The structures of new compounds were elucidated on the basis of extensive spectroscopic analyses and comparison with literature. Compounds 1-17 were examined for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced with 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells, a known primary screening test for inhibitors of tumor promotion. Four compounds, 1, (23E)-3β,7β-dihydroxy-25-methoxycucurbita-5,23-dien-19-al (2), karavilagenin D (11), and 12, showed potent inhibitory effects on EBV-EA induction with IC(50) values in the range of 242-264 mol ratio/32 pmol TPA. In addition, compounds 1 and 11 exhibited inhibitory effects on skin-tumor promotion in an in vivo two-stage mouse skin carcinogenesis test based on 7,12-dimethylbenz[a]anthracene (DMBA) as initiator, and with TPA as a promoter. Furthermore, upon evaluation of the cytotoxic activities of compounds 1-17 against human cancer cell lines, compounds 2, 5-7, 9, and 14 showed potent activities against HL60 cell line, and compound 2 against SK-BR-3 cell line.

Neuroblastoma (NB) is a very common malignant solid tumor in childhood. Prognosis in NB patients tends to vary greatly, and many studies have demonstrated that both clinical and molecular biological factors are correlated with outcome. 1) For example, patients under the age of 1 year at diagnosis usually have good prognoses, but those diagnosed over the age of 1 year have poor prognoses.2) Increased expression of the molecular biological factors MYCN, H-ras and trkA is well known in NB. [3][4][5][6][7][8][9][10][11] Recently, there has been great interest in apoptosis, or programmed cell death, the mechanism by which cells essentially suicide.12) Many inhibitors of apoptosis are known to contribute to tumorigenicity and increased spread of tumor cells.13) Survivin is a recently described member of the inhibitor of apoptosis protein (IAP) family.14) This gene exists on chromosome 17q and inhibits apoptosis by blocking the effects of caspase-9, which is activated in extrinsic and intrinsic pathways.14-17) Survivin is expressed in many malignant tumors, including breast, lung, stomach, colon and pancreatic cancers, bladder tumors, malignant lymphoma, and NB.18) It is not usually present in normal tissues and is rarely found in mature tissues.17) Thus, survivin expression is likely to be an important prognostic factor in tumor malignancy, and we considered that survivin mRNA expression would be useful in determining tumor malignancy and prognosis in NB.We therefore used reverse transcription-polymerase chain reaction (RT-PCR) to investigate the expression of survivin mRNA in NB cell lines, normal blood cell samples, and clinical NB tumor samples.Here, we describe how the degree of expression of survivin mRNA is a very useful prognostic indicator. MATERIALS AND METHODSCell Lines, Clinical NB Tumor Samples, and Normal Blood Cell Samples Three NB cell lines 19,20) SK-N-SH, 20,21) and NB- 39 20) ) were examined. They were cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum, 100 U/ml penicillin, 0.1 mg/ml streptomycin, and 2 g/l sodium bicarbonate under 5% CO 2 at 37°C. Two normal adult blood cell samples and 13 clinical NB tumor samples were also examined. Two of the tumor samples were from recurrent tumors. These tumor tissues had been stored at Ϫ80°C since collection. The clinical diagnoses for these patients had been made by histopathology. Informed consent was obtained from all patients before the study began.RNA Extraction Total RNA from the three cell lines and 13 NB tumor samples was extracted with TRI ZOL reagent (Gibco BAL) by the acid-guanidium-phenol chloroform extraction method.22) Total RNA from the two normal blood cell samples was extracted with TRI ZOL LS Reagent (Gibco BAL) by acid-guanidium-phenol chloroform extraction method. 16)Reverse Transcription-Polymerase Chain Reaction For determination of survivin mRNA expression, total RNA (1 mg) was reverse-transcribed in a 10 ml reaction mixture with a first strand cDNA synthesis kit (Rever Tra-a-TM , Toyobo). RT was performed with Oligo...

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