Chryroxosides A-E: five new triterpene saponins from the leaves of Chrysophyllum roxburghii G.Don. and their cytotoxic activity.

Five undescribed oleanane triterpene glycosides named chryroxosides A-D (1-5), together with five known compounds (6-10) were isolated from the leaves of Chrysophyllum roxburghii G.Don. Their chemical structures were elucidated by extensive spectroscopic data analyses including IR, HR-ESI-MS, 1D and 2D NMR). Compounds 1, 3, and 5 showed cytotoxic effects against KB, HepG2, HL60, P388, HT29, and MCF7 cell lines with the IC50 values ranging from 14.40 to 52.63 µM compared to the positive control compound (ellipticine) with the IC50 values ranging from 1.34 to 1.99 µM.

Discovery of Four New Compounds from Macropanax membranifolius and Their Cytotoxic Activity.

A phytochemical investigation of the methanolic extract of the Macropanax membranifolius C.B. Shang leaves led to the isolation of three new flavans, (2R,3R)-4'-O-methylcatechin 5-O-ß-D-glucopyranoside (1), (2S,3S)-4'-O-methylcatechin 5-O-ß-D-glucopyranoside (2), (2S,3R)-4'-O-methylcatechin 5-O-ß-D-glucopyranoside (3), one new triterpene glycoside 3-O-ß-D-xylopyranosyl-(1→6)-[ß-D-xylopyranosyl-(1→2)]-ß-D-glucopyranosyl-oleanolic acid 28-O-ß-D-glucopyranoside (4), together with nine known compounds (5-13). Their chemical structures were elucidated based on HR-ESI-MS, NMR spectroscopic data. The absolute configurations of compounds 1-3 were established by electronic circular dichroism (ECD) spectra. At concentration of 20 µM, compounds 1-13 showed the percentages of dead cell in the range of 2.14 % to 33.61 % against KB, HepG2, HL60, P388, HT29, and MCF7 cancerous cell lines by SRB assay.

Design, synthesis and evaluation the bioactivities of novel 1,3-dimethyl-6-amino-1H-indazole derivatives as anticancer agents.

Indoleamine 2,3-dioxygenase (IDO1) is a heme-containing enzyme mainly responsible for the metabolism of tryptophan to kynurenine. To date, the IDO1 inhibitors have been developed intensively for the re-activation of the anticancer immune response. In this report, we designed, and synthesized novel 1,3-dimethyl-6-amino indazole derivatives as IDO1 inhibitors based on the structure of IDO1 active site. We further examined their anticancer activity on hypopharyngeal carcinoma cells (FaDu), squamous cell carcinoma of the oral tongue (YD-15), breast cancer cells (MCF7), and human dental pulp stem cells (HDPSC). Of them, compound N-(4-bromobenzyl)-1,3-dimethyl-1H-indazol-6-amine (7) remarkably suppressed IDO1 expression in a concentration - dependent manner. In addition, 7 was the most potential anticancer compound with inducing apoptosis activity as well as selectively activated extracellular signal-regulated kinases (ERK) in mitogen-activated protein kinase (MAPK) pathways on FaDu cells. Finally, compound 7 suppressed cell mobility in wound healing assay with the reduced expression of matrix metalloproteinase MMP9. Taken together, we believe that 7 is the most promising compound, which may be applied to treatment of hypopharyngeal carcinoma.

Ultra-low detection limit chemoresistive NO2 gas sensor using single transferred MoS2 flake: an advanced nanofabrication.

In this work, a method of fabricating a NO2 nano-sensor working at room temperature with a low detectable concentration limit is proposed. A 2D-MoS2 flake is isolated by transferring a single MoS2 flake to SiO2/Si substrate, followed by applying an advanced e-beam lithography (EBL) to form a metal contact with Au/Cr electrodes. The resulting chemoresistive nano-sensor using a single MoS2 flake was applied to detect a very low concentration of NO2 at the part-per-billion (ppb) level. This result is obtained due to the ability to create microscopic nano-sized MoS2 gaps using e-beam lithography (300 nm-400 nm). Experimental results also show that the sensor can capture changes in concentration and send the information out extremely quickly. The response and recovery time of the sensor also reached the lowest point of 50 and 75 ms, outperforming other sensors with a similar concentration working range.

The insecticidal capacity of ethanol extract from Cascabela peruviana (L.) Lippold against fruit fly.

Cascabela peruviana (L.) Lippold (C. peruviana) has been extensively used for its antifungal and antibacterial properties. However, its role in anti-insect is still under investigation. To investigate the ability of the ethanol extract of C. peruviana against insects, we used the fruit fly (Drosophila melanogaster) as a model to gain more insight into the toxic effects of this extract. We found that the ethanol extract from the stem and leaves of C. peruviana was effective against insects and contained polyphenol and flavonoid compounds. C. peruviana could induce mortality of 2nd-instar larvae and reduce growth and reproduction of fruit flies. Interestingly, the toxicity of C. peruviana extract has been remained to affect the development of the next generation of fruit flies. The locomotor activity and feeding ability of the F1 generation of this insect were significantly reduced by C. peruviana. In addition, flavonoids and polyphenols, as well as saponins and tannins were detected in the ethanol extract of C. peruviana. We assume that the ability of the extract of C. peruviana to control insects may be related to the presence of high levels of these compounds. The findings highlighted that the extract from the leaves of Cascabela peruviana has the potential to be used as an insecticide.

Optimizing outcomes for patients with metastatic prostate cancer: insights from South East Asia Expert Panel.

AIMS: Clinical decision making is challenging in men with metastatic prostate cancer (mPC), as heterogeneity in treatment options and patient characteristics have resulted in multiple scenarios with little or no evidence. The South East Asia Expert Panel 2019 addressed some of these challenges. METHODS: Based on evidence in the literature and expert interviews, 19 statements were formulated for key challenges in the treatment of men with castration-sensitive and -resistant prostate cancer in clinical practice. A modified Delphi process was used to reach consensus among experts in the panel and develop clinical practice recommendations. RESULTS: The majority of the panel preferred a risk-based stratification and recommended abiraterone or enzalutamide as first-line therapy for symptomatic chemotherapy naïve patients. Abiraterone is preferred over enzalutamide as a first-line treatment in these patients. However, the panel did not support the use of abiraterone in high risk lymph-node positive only (N+M0) or in non-metastatic (N0M0) patients. In select patients, low dose abiraterone with food may be used to optimize clinical outcomes. Androgen receptor gene splice variant status may be a useful guide to therapy. In addition, generic versions of approved therapies may improve access to treatment to a broader patient population. The choice of treatment, as well as sequencing are guided by both patient and disease characteristics, preferences, drug access, cost, and compliance. CONCLUSION: Expert recommendations are key to guidance for the optimal management of mPC. Appropriate choice, timing, and sequence of treatment options can help to tailor therapy to maximize outcomes in men with mPC.

Traphanoside GO1, a new triterpenoid saponin from the aerial parts of Glinus oppositifolius with the inhibitory effect on PGE2 production in LPS-induced HepG2 cells.

A new saponin, 3-O-[α-ʟ-rhamnosyl-(1→3)-ß-D-glucopyranosyl]-28-O-ß-D-glucopyranosyl serjanic acid (Traphanoside GO1, 11) along with eleven compounds (1-10 and 12) were isolated from the aerial parts of Glinus oppositifolius. The structures of all isolates were elucidated by analyzing extensive 1 D- and 2 D-NMR and HR-ESI-MS, comparing with reported literature data. Compounds 7-8, 10-11, and 90% ethanol extract (GOE90) were evaluated for the inhibitory effect on PGE2 production from activated HepG2 cells. Among these, new compound 11 showed the most potent inhibitory activity by suppressing LPS-induced PGE2 production on the HepG2 cells.

Two polymorphisms, rs2046210 and rs3803662, are associated with breast cancer risk in a Vietnamese case-control cohort.

Breast cancer is the most common cancer in women worldwide. Breast tumorigenesis encompasses both extrinsic and intrinsic factors. Among intrinsic aspects, the appearance of DNA variation can cause genetic instability, which may lead to carcinogenesis. Genome-wide association studies have found several potential breast cancer-associated single nucleotide polymorphisms (SNPs) in many different populations. Among these, seven (rs2046210, rs1219648, rs3817198, rs3803662, rs889312, rs10941679 and rs13281615) have been shown to be significantly associated with breast cancer risk in various populations including those very similar to the Vietnamese. Here, therefore, we have investigated the relationship between these SNPs and breast cancer risk in a Vietnamese population case-control cohort. Real-time PCR high-resolution melt analysis was performed to genotype 300 breast cancer cases and 325 healthy controls, and the association between the seven SNPs and breast cancer risk was determined by analyzing the differences in allelic and genotypic frequencies between case and control groups using R software. While five of the seven showed no association with breast cancer, there was a relationship between the other two SNPs, rs2046210 and rs3803662, and the risk of developing this disease in Vietnamese women. The A allele is the risk allele for both rs2046210 (OR [95% CI] = 1.43 [1.14 - 1.78], P = 0.0015) and rs3803662 (OR [95% CI] = 1.45 [1.16 - 1.83], P = 0.001). We conclude that two polymorphisms, rs2046210 in ESR1 and rs3803662 in TNRC9, are associated with breast cancer risk in the Vietnamese population.