Cytotoxic activity of natural labdanes and their semi-synthetic modified derivatives from Croton oblongifolius

Labda-7,12( E),14-triene-17-oic acid, previously isolated from Croton oblongifolius, and its derivatives were investigated for cytotoxicity against five human tumor cell lines. Six of these compounds, labda-7,12( E),14-triene-17-al, 17-hydroxylabda-7,12( E),14-triene, 17-acetoxylabda-7,12( E),14-triene, 15-hydroxylabda-7,13( E)-diene-17,12-olide, labda-7,13( E)-diene-17,12-olide, and 12,17-dihydroxylabda-7,13( E)-diene showed non-specific, moderate, cytotoxicity against all cell lines, whereas the other compounds were inactive.     

Antiangiogenic effect of chamigrane endoperoxides from a Thai mangrove-derived fungus

As part of our ongoing efforts to investigate natural products with potential for use as cancer treatments, we have recently disclosed the cytotoxicity of unique nor-chamigrane (1) and chamigrane (2, 3) endoperoxides from a Thai mangrove-derived fungus. Reinvestigation of this fungus in a large-scale fermentation led to the isolation of an additional new chamigrane endoperoxide (4) and one known analogue (5). Among these isolated metabolites, compound 3 (merulin C) exhibited potent antiangiogenic activity mainly by suppression of endothelial cell proliferation and migration in a dose-dependent manner, and its effect is mediated by reduction in the phosphorylation of Erk1/2. Merulin C also displayed promising activity in a rat aortic ring sprouting (ex vivo) and a mouse Matrigel (in vivo) assay.     

Diagnostic value of bronchoalveolar lavage and postbronchoscopic sputum cytology in peripheral lung cancer

Abstract The objective of this study was to evaluate the value of bronchoalveolar lavage (BAL) and postbronchoscopic sputum cytology in diagnosing peripheral lung cancer. We performed a prospective study in 55 patients with lesions on chest radiographs who were suspected of having lung cancer and had non-endoscopically visible lesions on fiberoptic bronchoscopy. The sequence of procedures in all cases was BAL and transbronchial forceps biopsy. The final diagnosis of these patients were primary lung cancer in 30 patients, metatastic lung cancer in five and benign diseases in 20. In the primary lung cancer group, BAL was positive for malignant cells in 14 of the 30 patients (46.7%). In seven (50%) of these patients, the cell type diagnosed by BAL agreed with the final diagnosis. The diagnostic yield of BAL was influenced by the size and segmental location of the lesion. Bronchoalveolar lavage provided a higher diagnostic yield (46.7%) than transbronchial biopsy (16.7%). In five patients with metastatic lung cancer and 20 patients with benign disease, BAL gave negative results in all. Postbronchoscopic sputum cytology was positive in only two of the 26 patients (7.7%) from whom samples could be obtained. Bronchoalveolar lavage cytology proved to be a valuable diagnostic tool in detecting peripheral, primary lung cancer. Postbronchoscopic sputum cytology provided no significant additional information.     

11-Hydroxymonocerin from the plant endophytic fungus Exserohilum rostratum

A new analogue of monocerin, 11-hydroxymonocerin (2), along with monocerin (1) and 12-hydroxymonocerin (3) were isolated from cultures of Exserohilum rostratum, a fungal strain endophytic in Stemona sp. The structure of 2 was determined by analysis of NMR and MS data and by comparison of spectroscopic data to those of 1. Monocerin (1) and 11-hydroxymonocerin (2) displayed activity against Plasmodium falciparum (K1, multidrug-resistant strain) with IC50 values of 0.68 and 7.70 microM, respectively. None of the compounds were cytotoxic against any of the tumor cell lines tested.     

Cassane furanoditerpenoids from the seed kernels of Caesalpinia bonduc from Thailand

Three new cassane furanoditerpenoids ( 1- 3), together with 13 known cassane diterpenes ( 4- 16), were isolated from the EtOAc extract of the seed kernels of Caesalpinia bonduc. Their structures were elucidated on the basis of spectroscopic analysis, mainly NMR and MS. Compounds 1- 3 exhibited good antimalarial activity against the multidrug-resistant K1 strain of Plasmodium falciparum, while compound 4 was inactive. None of the compounds were cytotoxic against any of the tumor cell lines tested.     

Furanocembranoids from the stem bark of Croton oblongifolius

Four novel furanocembranoids (1-4) were isolated from the stem bark of Croton oblongifolius. Their structures were elucidated on the basis of spectroscopic analysis, mainly NMR and MS. Compounds 1, 3, and 4 exhibited good cytotoxicity against several human tumor cell lines.