Comparing a lowland and an upland ecotype of Cyperus rotundus, the former had greater carbohydrate reserves in tubers, thicker roots and stems with larger air spaces and, under hypoxia, it maintained relatively lower activities of alcohol dehydrogenase and lactate dehydrogenase.

Garcinia dauphinensis is a previously uninvestigated endemic plant species of Madagascar. The new phloroglucinols dauphinols A-F and 3'-methylhyperjovoinol B (1-7) and six known phloroglucinols (8-13) together with tocotrienol 14 and three triterpenoids 15-17 were isolated from an ethanolic extract of G. dauphinensis roots using various chromatographic techniques. The structures of the isolated compounds were elucidated by NMR, MS, optical rotation, and ECD data. Theoretical ECD spectra and specific rotations for 2 were calculated and compared to experimental data in order to assign its absolute configuration. Among the compounds tested, 1 showed the most promising growth inhibitory activity against A2870 ovarian cancer cells, with IC 50 = 4.5 ± 0.9 μM, while 2 had good antiplasmodial activity against the Dd2 drug-resistant strain of Plasmodium falciparum, with IC 50 = 0.8 ± 0.1 μM.

Introduction: Cinnamomum mercadoi is a medicinal tree endemic to the Philippines. Cinnamomum species have been extensively studied for their endophytic fungi with pharma cological importance. This study aims to isolate and evaluate the antibacterial activity of endophytic fungi associated with the bark of C. mercadoi. Materials and Methods: Endophytic fungi were isolated from surface sterilized bark samples aseptically. The pure isolates were identified through their morphological characteristics. Agar plug diffusion assay was employed in the primary screening of their antibacterial activity against Staphylococcus aureus, Bacillus cereus, Escherichia coli and Pseudomonas aeruginosa. Four active endophytes were fermented and extracted with ethyl acetate (EtOAc). The antibacterial activity of the EtOAc extracts was screened using the disk diffusion assay. The minimum inhibitory activity (MIC) was evaluated using the microdilution method. Results: Twelve (12) endophytes were isolated from the bark of C. mercadoi. All endophytes exhibited antibacterial activity on at least one of the test pathogens. However, only two of the four endophytes subjected to the secondary screening showed wide-spectrum activity and inhibited the growth of all test bacteria. Fusarium sp. 2 was identified to have the most promising activity with MIC values ranging from 2.1 -4.2 mg/mL. Conclusion: C. mercadoi harbors endophytes, particularly Fusarium sp. 2, which possess antibacterial activity and thus a potential source of antibacterial compounds. endophytic fungi, particularly those isolated from medicinal plants for their potential as source of new antibiotics. [8][9][10] Several Cinnamomum species has been studied for their associated endophytes because of their promising antibacterial activity.11-13 Moreover, active compounds have been isolated from endophytic fungi associated with this species. Cinnamomum zeylanicum, collected from Honduras, was the host of a novel endophyte Muscador albus which was reported to contain volatile organic compounds with antimicrobial activities.14 Antimycobacterial compounds were isolated from Annulohypoxylon ilanense, an endophyte of a Cinnamomum species from Taiwan. 15 Cinnamomum mercadoi (Lauraceae) is a tree endemic to the Philippines. It is traditionally used as expectorant and for the treatment of digestion problem and tuberculosis. 16,17 Biological studies of C. mercadoi had shown that its crude extract exhibited analgesic, antimicrobial, antioxidant and antidiarrheal properties. [17][18][19] No previous study on its endophytic fungi has been reported to the best of our knowledge. In this study, we have isolated 12 endophytic fungi and screened them for their antibacterial activity. An Ascomycete isolate, Fusarium sp. 2, is being reported to have a broad spectrum and promising antibacterial activity. MATERIALS AND METHODS Sample CollectionBark samples were collected from a healthy Cinnamomum mercadoi tree in Barangay Patag, Baybay, Leyte, Philippines (10.74 °N, 124.79°E,31.5 m elevation) i...

Covering: up to 2015 The Wnt signalling pathway is essential in many biological processes. The Wnt signal is associated with several diseases, particularly cancer and neurodegenerative diseases. Recently, high-throughput screening systems have been developed to rapidly identify compounds, including natural compounds, that target the Wnt signal. Some studies on natural modulators of the Wnt signal have also suggested their possible target. This review highlights some important natural compounds reported to regulate Wnt activity and describes their possible mechanism of action.

Scopadulciol (1), a scopadulan-type diterpenoid, was isolated from Scoparia dulcis along with three other compounds (2−4) by an activity-guided approach using the TCF reporter (TOP) luciferasebased assay system. A fluorometric microculture cytotoxicity assay (FMCA) revealed that compound 1 was cytotoxic to AGS human gastric adenocarcinoma cells. The treatment of AGS cells with 1 decreased β-catenin levels and also inhibited its nuclear localization. The pretreatment of AGS cells with a proteasome inhibitor, either MG132 or epoxomicin, protected against the degradation of β-catenin induced by 1. The 1-induced degradation of β-catenin was also abrogated in the presence of pifithrin-α, an inhibitor of p53 transcriptional activity. Compound 1 inhibited TOP activity in AGS cells and downregulated the protein levels of cyclin D1, c-myc, and survivin. Compound 1 also sensitized AGS cells to tumor necrosis factor-related apoptosis ligand (TRAIL)-induced apoptosis by increasing the levels of the death receptors, DR4 and DR5, and decreasing the level of the antiapoptotic protein Bcl-2. Collectively, our results demonstrated that 1 induced the p53-and proteasome-dependent degradation of β-catenin, which resulted in the inhibition of TCF/β-catenin transcription in AGS cells. Furthermore, 1 enhanced apoptosis in TRAIL-resistant AGS when combined with TRAIL.

The application of 13C-NMR spectroscopy to problems involving the structures and interactions of carbohydrates is described. Both 13C-enriched and natural abundance compounds were used and some advantages of the use of the stable isotope are described. Carbon-carbon and carbon-proton coupling constants obtained from 1-13C enriched carbohydrates were employed in the assignment of their chemical shifts and to establish solution conformation. In all cases studied thus far, C-3 couples to C-1 only in the beta-anomers while C-5 couples to C-1 only in the alpha-anomers. C-6 and C-2 always couple to C-1 in both anomeric species. The alkaline degradation of glucose [1-13C] to saccharinic acids was followed by 13C-NMR. The conversion of glucose [1-13C] to fructose-1, 6-bisphosphate [1, 6-13C] by enzymes of the glycolytic pathway was shown as an example of the use of 13C-enriched carbohydrates to elucidate biochemical pathways. In a large number of glycosyl phosphates the 31P to H-1 and 31P to C-2 coupling constants demonstrate that in the preferred conformation and phosphate group lies between the O-5 and the H-1 of the pyranose ring. The influence of paramagnetic Mn2 + ions on the proton decoupled 13C-NMR spectra of uridine diphosphate N-acetylglucosamine indicates that the Mn2 + interacts strongly with the pyrophosphate moiety and with the carbonyl groups of the uracil and N-acetyl groups.

Rocaglamides are bioactive natural compounds which have a cyclopenta[b]benzofuran core structure. The total synthesis of a reported natural product, 3'-hydroxymethylrocaglate (5), was achieved using [3 + 2] cycloaddition between 3-hydroxyflavone and methyl cinnamate. We also describe the synthesis of rocaglamide heterocycle derivatives and evaluate their Wnt signal inhibitory activities. Compounds 4, 5, 22a, 22b, 22c and 23c showed potent Wnt signal inhibitory activity.

A reporter gene assay that detects neurogenin 2 (Ngn2) promoter activity was utilized to identify compounds that induce neuronal differentiation. Ngn2 is a basic helix-loop-helix transcription factor that activates transcription of pro-neural genes. Using this assay system and an activity-guided approach, seven phenolic compounds were isolated from the methanol extract of Oroxylum indicum: 1 oroxylin A, 2 chrysin, 3 hispidulin, 4 baicalein, 5 apigenin, 6 baicalin, and 7 isoverbascoside. Compounds 1 and 2 induced an estimated 2.7-fold increase in Ngn2 promoter activity, whereas 3 increased the activity by 2.5-fold. Furthermore, 1 and 2 enhanced neuronal differentiation of C17.2 cells, which are multipotent stem cells.