The syntheses, characterizations, and biological activities of three organoplatinum compounds, each containing a triazole ring, are discussed. These organometallic compounds demonstrate superior cytotoxicity against osteosarcoma and human breast cancer cells relative to cisplatin, a well-known chemotherapeutic agent used for chemotherapy.

Asia has intermediate-to-high prevalence and high morbidity of hepatitis B virus (HBV) infection. The use of guideline-recommended nucleos(t)ide analogs with high barrier to resistance, such as entecavir (ETV), tenofovir disoproxil fumarate (TDF), and tenofovir alafenamide (TAF), is one of the key interventions for curbing HBV infection and associated morbidity in Asia. However, there are some challenges to the use of ETV and TDF; while ETV is associated with high resistance in lamivudine (LAM)-exposed (especially LAM-refractory) patients; bone and renal safety issues are a major concern with TDF. Hence, a panel of twenty-eight expert hepatologists from Asia convened, reviewed the literature, and developed the current expert opinion-based review article for the use of TAF in the resource-constrained settings in Asia. This article provides a comprehensive review of two large, phase 3, double-blind, randomized controlled trials of TAF versus TDF in HBeAg-negative (study 0108) and HBeAg-positive (study 0110) chronic HBV patients (> 70% Asians). These studies revealed as follows: (1) non-inferiority for the proportion of patients who had HBV DNA < 29 IU/mL; (2) significantly high rate of normalization of alanine aminotransferase levels; (3) no incidence of resistance; and (4) significantly better bone and renal safety, with TAF vs. TDF up to 144 weeks. Considering the benefits of TAF, the expert panel proposed recommendations for optimizing the use of TAF in Asia, along with guidance on specific patient groups at risk of renal or bone disease suitable for TAF therapy. The guidance provided in this article may help clinicians optimize the use of TAF in Asia.

Two new irregular hexagons (6 and 7) were synthesized from a pyrazine motif containing an organometallic acceptor clip [bearing platinum(II) centers] and different neutral donor ligands (4,4'-bipyridine or pyrazine) using a coordination-driven self-assembly protocol. The two-dimensional supramolecules were characterized by multinuclear NMR, mass spectrometry, and elemental analyses. Additionally, one of the macrocycles (6) was characterized by single-crystal X-ray analyses. Macrocycles are unique examples of [2 + 2] self-assembled ensembles that are hexagonal but irregular in shape. These hexagon frameworks require the assembly of only four tectons/subunits. The cytotoxicity of platinum(II)-based macrocycles was studied using various cell lines such as A549 (human lung carcinoma), KB (human oral cancer), MCF7 (human breast cancer), and HaCaT (human skin keratinocyte) cell lines, and the results were compared with those of cisplatin. The smaller macrocycle (7) exhibited a higher cytotoxic effect against all cell types, and its sensitivity was found to be comparable with that of cisplatin for A549 and MCF7 cells. Cell cycle analysis and live propidium iodide staining suggest that the macrocycles 6 and 7 induced a loss of membrane integrity that ultimately might lead to necrotic cell death.

Background: Acute viral hepatitis (AVH) is usually a self-limiting illness. Diabetics are prone to develop liver diseases and liver regeneration is impaired in them. Natural course of AVH in diabetics has not been assessed and may be severe. Design: Observational prospective study to evaluate natural course of AVH in patients with and without diabetes mellitus. Consecutive patients with AVH were included and categorized in to those with or without diabetes. Etiology, complications, mortality and recovery parameters of AVH were identified and compared between two groups. Results: 131 consecutive AVH between March 2007 and March 2009 were evaluated; 12 diabetics and 83 non-diabetics (n = 95) were included for analysis. Hepatitis E was the commonest cause (n = 55, 57.89%) in the whole cohort. However, Hepatitis B virus (HBV) as the etiology was significantly higher among diabetics than in non-diabetics (58.33% vs. 25.3%, P = 0.02). In contrast, hepatitis E was the etiology in 61.44% of non-diabetics. Frequency of severe hepatitis was significantly higher in diabetics than in nondiabetics (5/12; 41.67% vs. 9/83; 10.64%, P < 0.005). 5 of 14 (36%) with severe hepatitis were diabetics. Liver failure and death occurred in 2 (16%) diabetics, while none among the non-diabetics had liver failure. Multiple variable logistic regression analysis revealed that acute hepatitis B (OR 4.7 (95% CI 1.34-16.47)) and diabetes (OR 4.0 (95% CI 0.96-16.47)) were associated with severe hepatitis. Conclusion: Patients with diabetes are at risk to contact HBV infection and severe hepatitis. ( J CLIN EXP HEPATOL 2013;3:275-280)

No abstract