Oxobedfordia acid reduces colon cancer cell viability through apoptosis induction and inhibits colon cancer growth in mice model

Purpose: Colon cancer is amongst the most commonly diagnosed carcinoma globally and ranks 3rd highest of all the kinds of tumors. In the present study effect of oxobedfordia acid on colon cancer cell viability and colorectal tumor growth in vivo was investigated.Methods: Cytotoxicity of oxobedfordia acid in SW480, HCT116, and FHC cells was evaluated by MTT assay. Colon cancer in the mice was induced by implanting subcutaneously 2 x 106 HT-29 cells/mouse in the right flank. Various parameters, including cell viability, tumor growth and expression levels of cancer factors, were also assessed.Results: Treatment with oxobedfordia acid significantly reduced viability in SW480 and HCT116 cells (p < 0.05). Furthermore, oxobedfordia acid caused increased miR-331-3p levels in cells. Moreover, oxobedfordia acid caused a significant reduction in NRP2 expression and increased apoptosis induction in SW480 and HCT116 cells. Oxobedfordia acid treatment for 48 h significantly increased p53 and p-c- Jun levels, but reduced Bcl-2 expression in cells (p < 0.05). In the mouse model of colon cancer, oxobedfordia acid significantly retarded tumor growth. Furthermore, in oxobedfordia acid-treated mice, expression of miR-331-3p was elevated while NRP2 level was lowered when compared with control group (p < 0.05).Conclusion: Oxobedfordia acid treatment suppresses colon cancer cell viability and inhibits tumor growth in mice through enhancement of miR-331-3p and reduction in NRP2 expression. Hence, oxobedfordia acid can potentially be developed as an agent for the management of colorectal cancer.&nbsp

Strong Association Between Two Polymorphisms on 15q25.1 and Lung Cancer Risk: A Meta-Analysis

Background: The association between polymorphisms on 15q25.1 and lung cancer has been widely evaluated; however, the studies have yielded contradictory results. We sought to investigate this inconsistency by performing a comprehensive meta-analysis on two polymorphisms (CHRNA3 gene: rs1051730 and AGPHD1 gene: rs8034191) on 15q25.1. Methods: Data were extracted from 15 and 14 studies on polymorphisms rs1051730 and rs8034191 involving 12301/14000 and 14075/12873 lung cancer cases/controls, respectively. The random-effects model was applied, addressing heterogeneity and publication bias. Results: The two polymorphisms followed Hardy-Weinberg equilibrium for all studies (P\u3e0.05). For rs1051730-G/A, carriers of A allele had a 36% increased risk for lung cancer (95% confidence interval [CI]: 1.27–1.46; P\u3c0.0005), without heterogeneity (P = 0.258) or publication bias (PEgger = 0.462). For rs8034191-T/C, the allelic contrast indicated that C allele conferred a 23% increased risk for lung cancer (95% CI: 1.08–1.4; P = 0.002), with significant heterogeneity (P\u3c0.0005), without publication bias (PEgger = 0.682). Subgroup analyses suggested that the between-study heterogeneity was derived from ethnicity, study design, matched information, and lung cancer subtypes. For example, the association of polymorphisms rs1051730 and rs8034191 with lung cancer was heterogeneous between Caucasians (OR = 1.32 and 1.22; 95% CI: 1.25–1.44 and 1.05–1.42; PP = 0.237 and 0.934, respectively) under the allelic model, and this association was relatively strengthened under the dominant model. There was no observable publication bias for both polymorphisms. Conclusions: Our findings demonstrated that CHRNA3 gene rs1051730-A allele and AGPHD1 gene rs8034191-T allele might be risk-conferring factors for the development of lung cancer in Caucasians, but not in East-Asians

API : an index for quantifying a scholar's academic potential

In the context of big scholarly data, various metrics and indicators have been widely applied to evaluate the impact of scholars from different perspectives, such as publication counts, citations, ${h}$-index, and their variants. However, these indicators have limited capacity in characterizing prospective impacts or achievements of scholars. To solve this problem, we propose the Academic Potential Index (API) to quantify scholar's academic potential. Furthermore, an algorithm is devised to calculate the value of API. It should be noted that API is a dynamic index throughout scholar's academic career. By applying API to rank scholars, we can identify scholars who show their academic potentials during the early academic careers. With extensive experiments conducted based on the Microsoft Academic Graph dataset, it can be found that the proposed index evaluates scholars' academic potentials effectively and captures the variation tendency of their academic impacts. Besides, we also apply this index to identify rising stars in academia. Experimental results show that the proposed API can achieve superior performance in identifying potential scholars compared with three baseline methods. © 2019 IEEE

Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety

We herein report the design and synthesis of benzothiazinones containing a piperidine moiety as new antitubercular agents based on the structure feature of IMB-ZR-1 discovered in our lab. Some of them were found to have good in vitro activity (MIC < 1 μg/mL) against drug-susceptible Mycobacterium tuberculosis H37RV strain. After two set of modifications, compound 2i were found to display comparable in vitro anti-TB activity (MIC < 0.016 μg/mL) to PBTZ169 against drug-sensitive and resistant mycobacterium tuberculosis strains. Compound 2i also showed acceptable PK profiles. Studies to determine PK profiles in lung and in vivo efficacy of 2i are currently under way