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Cholangiocarcinoma (CCA) is a very aggressive tumor. The development of a new therapeutic drug for CCA is required. This study aims to evaluate the antitumor effect of ∆9-tetrahydrocannabinol (THC), the major psychoactive component of marijuana (Cannabis sativa), and cannabinol (CBN), a minor, low-psychoactive cannabinoid, on CCA cells and xenograft mice. THC and CBN were isolated, and their identities were confirmed by comparing 1H- and 13C-NMR spectra and mass spectra with a database. Cell proliferation, cell migration, and cell apoptosis assays were performed in HuCCT1 human CCA cells treated with THC or CBN. The phosphorylation of signaling molecules in HuCCT1 cells was detected. To determine the effects of THC and CBN in an animal model, HuCCT1 cells were inoculated subcutaneously into nude mice. After the tumors reached an appropriate size, the mice were treated with THC or CBN for 21 days. Tumor volumes were monitored and calculated. The 1H- and 13C-NMR data of THC and CBN were almost identical to those reported in the literature. THC and CBN significantly inhibited cell proliferation and migration and induced apoptosis in HuCCT1 cells. The phosphorylation of AKT, GSK-3α/β, and ERK1/2 decreased in HuCCT1 cells treated with THC or CBN. CCA xenograft mice treated with THC showed significantly slower tumor progression and smaller tumor volumes than control mice. THC and CBN induced apoptosis in CCA by inhibiting the AKT and MAPK pathways. These findings provide a strong rationale for THC and CBN as therapeutic options for CCA.

A previous bioassay-guided fractionation of the active CH2Cl2-soluble layer from the liquid fermentation of Herbidospora daliensis yielded one actinomycete strain, 0385M-1T, which was isolated from sediment samples collected from a city in Taiwan. This resulted in the isolation of a new compound, daliensilin (1), The structure of the isolate was established by spectroscopic methods, including UV, IR, HR-ESI-MS, and extensive 1D and 2D NMR techniques, as well as by comparison with literature reports.

Investigation of the soil-derived fungus

A new phenolic glucoside, acremonoside (1), along with two known compounds, F-11334 A2 and 2,2-dimethyl-2H-chromen-6-ol, were isolated from the sea fan-derived fungus Acremonium polychromum PSU-F125. The structure of 1 was elucidated by spectroscopic techniques, acid hydrolysis and X-ray crystallographic analysis. The isolated compounds were tested for antibacterial, antimalarial, antimycobacterial and cytotoxic activities.

A new pentacyclic cytochalasin (diaporthalasin, 1) and a new ethyl trihydroxytridecatrienoate (diaporthacol, 2) together with five known compounds, R-mevalonolactone (4), dothiorelone C (5), (4S,7S,13S)-4,7-dihydroxy-1,3-tetradeca-1,5-dienolide (6), 4β-acetoxy-9β,10β,15α-trihydroxyprobotrydial (7) and O-methyldihydrobotrydial (8) were isolated from the marine-derived fungus Diaporthaceae sp. PSU-SP2/4. The structures were established by spectroscopic techniques. Compound 1 displayed significant antibacterial activity against both Staphylococcus aureus and methicillin-resistant S. aureus with equal MIC values of 2 μg/mL.

Five new polyketides including two benzopyranones (1 and 2), one isochroman (3) and two anthraquinone-citrinin derivatives (4 and 5) were isolated from the sea fan-derived fungus Penicillium citrinum PSU-F51 together with thirteen known compounds. The structures were determined by spectroscopic methods. The anthraquinone-citrinin derivatives are rare natural products. Compound 4 displayed moderate antibacterial activity against both Staphylococcus aureus and methicillin-resistant S. aureus with equal MIC values of 16 μg/mL, while the known coniochaetone A displayed moderate antifungal activity against Candida albicans with MIC value of 16 μg/mL.

Five new metabolites, fusaranthraquinone (1), fusarnaphthoquinones A-C (2-4), and fusarone (5), were isolated from the sea fan-derived fungi Fusarium spp. PSU-F14 and PSU-F135 along with 18 known compounds. The structures were elucidated on the basis of spectroscopic evidence. Their antibacterial, antifungal, antimycobacterial, antimalarial, and cytotoxic activities were examined.

Nigrosporanenes A (1) and B (2), two new cylohexene derivatives, and tyrosol (3) were isolated from the sea fan-derived fungus Nigrospora sp. PSU-F11, whereas five known compounds: 4-hydroxybenzoic acid (4), aplysiopsene D (5), 3-isochromanone (6), (-)-drimenin (7) and diketopiperazine derivative (8), were obtained from the fungus Nigrospora sp. PSU-F12. Their structures were established by spectroscopic evidence. We also tested their cytotoxic (on African green monkey kidney fibroblast and breast cancer cells), antioxidant (in the DPPH assay), and antibacterial (against the standard Staphylococcus aureus ATCC 25923 and methicillinresistant S. aureus) activities.

Garcinia dulcis (Roxb.) Kurz is a tropical fruit tree native to Southeast Asia where it has a long history of use as a traditional medicine for the treatment of ailments such as lymphatitis, parotitis, struma, scurvy, cough, and sore throat. Despite its medicinal values, this plant is not well known and rarely found nowadays. Research on the phytochemical constituents and biological activities of G. dulcis have demonstrated that various parts of the plant contain an abundance of bioactive compounds mainly xanthones and flavonoids, with significant pharmacological properties such as anti-atherosclerosis, anti-bacterial, anti-cancer, anti-hypertension, and anti-malarial. In the present review, current knowledge of the phytochemistry of G. dulcis and biological activities of its active constituents based on the available literature are summarized in order to explore application potentials and prospective research works on this plant.

A new [11]cytochalasin derivative, xylarisin (1), was isolated from the marine-derived fungus Xylaria sp. PSU-F100 along with six known metabolites: three mellein derivatives (2-4), one pyrone derivative (5) and two carboxylic acids (6,7). The structure and stereochemistry of 1 were determined by NMR and X-ray diffraction analyses. All isolated compounds showed mild antibacterial activity against standard Staphylococcus aureus ATCC 25923 and methicillin-resistant strain.

A new [11]cytochalasin derivative, xylarisin (1), was isolated from the marine-derived fungus Xylaria sp. PSU-F100 along with six known metabolites: three mellein derivatives (2-4), one pyrone derivative (5) and two carboxylic acids (6,7). The structure and stereochemistry of 1 were determined by NMR and X-ray diffraction analyses. All isolated compounds showed mild antibacterial activity against standard Staphylococcus aureus ATCC 25923 and methicillin-resistant strain.