Evaluation of the anticancer and antibacterial activities of moscatilin.

Orchids (Dendrobium sp.) have been the subject of extensive research due to their ubiquitous pharmacological, antimicrobial, and anticancer properties. Moscatilin is a bibenzyl secondary metabolite enriched in orchids that exhibits anticancer and antimicrobial properties through mechanisms that have not yet been fully elucidated. The current study aimed to assess the in vitro anticancer and antibacterial potential of moscatilin. The in vitro anti-proliferative effects of moscatilin against breast cancer-MCF-7 and liver-HepG2 cells were assessed using the dimethylthiazol-diphenyltetrazolium bromide assay. Selected six pro-apoptotic (caspase-3, 8, 9, p53, p21 & Bax) and two anti-apoptotic (Bcl-xL & Bcl-2) gene markers were assessed via qPCR and tested antibacterial activity against various bacterial strains using disc diffusion and broth dilution methods. Moscatilin decreased the cellular viabilities of HepG2 and MCF-7 cancer cells, with anti-proliferation rates of 66 % (IC50 51 ± 5.18 µM) and 58 % (IC50 57 ± 4.18 µM), respectively. This effect was selectively observed in cancer cells, and the impact of moscatilin on non-cancerous MCF-12 cells was marginal. Moreover, moscatilin-treated cells exhibited higher mRNA levels of caspase-3,8, 9, Bax, p53, and p21, whereas lower levels of Bcl-2 and Bcl-xL, two anti-apoptotic markers, were observed. Furthermore, moscatilin exhibited varying degrees of antibacterial activity against the bacterial strains investigated. Notably, the highest antibacterial potentials were observed against Staphylococcus epidermidis and Klebsiella pneumonia, while the lowest inhibitory activity was observed in Escherichia coli and Pseudomonas aeruginosa. Overall, these findings demonstrated that moscatilin exerts potent anticancer effects via apoptosis and has antimicrobial properties against Gram-negative and Gram-positive bacteria that are clinically relevant. These findings highlight the potential of moscatilin as a natural therapeutic candidate for the treatment of cancer and clinically important bacterial pathogens.

Moscatilin inhibits vascular calcification by activating IL13RA2-dependent inhibition of STAT3 and attenuating the WNT3/ß-catenin signalling pathway.

INTRODUCTION: Vascular calcification, a devastating vascular complication accompanying atherosclerotic cardiovascular disease and chronic kidney disease, increases the incidence of adverse cardiovascular events and compromises the efficacy of vascular interventions. However, effective therapeutic drugs and treatments to delay or prevent vascular calcification are lacking. OBJECTIVES: This study was designed to test the therapeutic effects and mechanism of Moscatilin (also known as dendrophenol) from Dendrobium huoshanense (an eminent traditional Chinese medicine) in suppressing vascular calcification in vitro, ex vivo and in vivo. METHODS: Male C57BL/6J mice (25-week-old) were subjected to nicotine and vitamin D3 (VD3) treatment to induce vascular calcification. In vitro, we established the cellular model of osteogenesis of human aortic smooth muscle cells (HASMCs) under phosphate conditions. RESULTS: By utilizing an in-house drug screening strategy, we identified Moscatilin as a new naturally-occurring chemical entity to reduce HASMC calcium accumulation. The protective effects of Moscatilin against vascular calcification were verified in cultured HASMCs. Unbiased transcriptional profiling analysis and cellular thermal shift assay suggested that Moscatilin suppresses vascular calcification via binding to interleukin 13 receptor subunit A2 (IL13RA2) and augmenting its expression. Furthermore, IL13RA2 was reduced during HASMC osteogenesis, thus promoting the secretion of inflammatory factors via STAT3. We further validated the participation of Moscatilin-inhibited vascular calcification by the classical WNT/ß-catenin pathway, among which WNT3 played a key role in this process. Moscatilin mitigated the crosstalk between WNT3/ß-catenin and IL13RA2/STAT3 to reduce osteogenic differentiation of HASMCs. CONCLUSION: This study supports the potential of Moscatilin as a new naturally-occurring candidate drug for treating vascular calcification via regulating the IL13RA2/STAT3 and WNT3/ß-catenin signalling pathways.

HPLC fingerprint for different growth period of Dendrobium huoshanense / 中草药

Objective: To establish a HPLC fingerprint method for assessing the quality of Dendrobium huoshanense, in addition to determining concentrations of syringic acid, rutin, dendrophenol and naringenin in this crude drug. Methods: Agilent C18 column (250 mm × 4.6 mm, 5 μm) was utilized with the mobile phase comprising methanol-0.1% phosphoric acid with the flow rate of 1 mL/min in a gradient elution manner. The detection wavelength was set at 240 nm and the column temperature was 30 ℃. The resultant chromatograms were imported to Similarity Evaluation System for Chromatographic Fingerprint of Chinese Materia Medica (2012.1) to obtain retention time and peak area of samples. Similarity for 39 sets of samples were analyzed. The peak area data were processed by SPSS software for cluster analysis and the clustering effect was discussed. Results: The line relationship of this way was good (R > 0.999), with high precision regarding instrument used (RSD < 3.00%), the method showed good reproducibility (RSD < 3.00%), standard recovery was between 99.26% and 100.32% (RSD of 0.35%-1.67%). Different growth period and different planting patterns of D. huoshanense were distinct regarding the concentration of four compounds. Conclusion: The method is useful to evaluate and discriminate D. huoshanense at different growth period for the purpose of providing scientific reference on harvest, development and evaluation of D. huoshanense.