Author: Kim, Sang Wha ; Han, Se Jin ; Kim, Sang Guen ; Yun, Saekil ; Jun, Jin Woo ; Kim, Hyoun Joong ; Sukumaran, V ; Park, Se Chang ; Giri, Sib Sankar ; Kang, Jeong Woo

The present study was conducted to isolate and characterise Pb-resistant lactic acid bacteria (LAB), and thus determine their potential for use as probiotics against Pb toxicity. A total of 107 Pb-resistant LAB strains were isolated from the gut content of Cyprinus carpio, of which 41 were established to be gram-positive and catalase-negative. Investigation of the Pb-binding ability of these isolated LAB identified seven strains (P2, P6, P7, P9, P16, P19 and P22) with comparatively high Pb-binding activities. These were selected for further screening to establish their Pb tolerance, anti-oxidative capacity and in vitro probiotic characteristics. Strain P16 exhibited both the highest Pb-binding and a relatively good antioxidant capacity. Furthermore, P16 displayed a high survival rate during 4 h of exposure to both low-pH (2.5-3.5) conditions and 10.0% fish bile, and a strong capacity to adhere to fish intestinal mucus (62.4%). Furthermore, P16 showed strong antibacterial activities against all tested fish pathogens. Strains P6, P9, P16, P19 and P22 were susceptible to a range of tested antibiotics, but not to vancomycin. Thus, of the isolated lactobacilli, strain P16 exhibited the best Pb-binding ability, a high level of antioxidant activity and satisfactory in vitro probiotic properties. Biochemical and 16S-rRNA gene analyses identified P16 as Lactobacillus reuteri. Thus, the results of the conducted in vitro tests suggest that the fish-associated P16 Lact. reuteri strain is a promising candidate probiotic, which should undergo further investigation to assess its suitability for use in protecting against lead-exposure-induced toxicities in aquaculture.

01 Dec 2018·The FASEB JournalQ2 · BIOLOGY

Delivery of a TNF‐α–derived peptide by nanoparticles enhances its antitumor activity by inducing cell‐cycle arrest and caspase‐dependent apoptosis

Q2 · BIOLOGY

Article

Author: Gong, Huizhen ; Xiao, Xing ; Chen, Xueming ; Dang, Shiying ; Yan, Qiuxia ; Ma, Yi ; Qiu, Pei ; Hong, An

ABSTRACTProstate cancer is the second‐most common malignancy of the male genitourinary system. TNF‐α has attracted intense attention as a potential therapeutic agent against various cancers. However, its therapeutic application is restricted by short half life and severe toxic side‐effects. In this study, we constructed a stable nanodrug called TNF‐α–derived polypeptide (P16)‐conjugated, chitosan (CTS)‐modified selenium nanoparticle (SC; SCP), which is composed of SC as a slow‐release carrier conjugated to P16. SCP had significant inhibitory effects on multiple types of tumor cells, especially DU145 prostate cancer cells, but not on RWPE‐1 normal human prostate epithelial cells. SCP could induce G0/G1 cell‐cycle arrest and apoptosis in DU145 cells more effectively than could P16 and TNF‐α. In DU145 xenograft tumor models, SCP exerted much stronger antitumor effects than P16 or estramustine (the clinical drug for prostate cancer) but caused fewer toxic side‐effects. In addition, SCP significantly inhibited proliferation and accelerated apoptosis in DU145 xenograft tumors. Further mechanistic studies revealed that SCP exerted antitumor effects via activation of the p38 MAPK/JNK pathway, thus inducing G0/G1 cell‐cycle arrest and caspase‐dependent apoptosis. These findings suggest that SCP may represent a potential long‐lasting therapeutic agent for human prostate cancer with fewer side effects.—Yan, Q., Chen, X., Gong H., Qiu, P., Xiao, X., Dang S., Hong A., Ma, Y. Delivery of a TNF‐α–derived peptide by nanoparticles enhances its antitumor activity by inducing cell‐cycle arrest and caspase‐dependent apoptosis. FASEB J. 32, 6948–6964 (2018). www.fasebj.org

14 Apr 2016·Anti-Cancer Agents in Medicinal ChemistryQ4 · MEDICINE

Multiple Pharmacological Properties of a Novel Parthenin Analog P16 as Evident by its Cytostatic and Antiangiogenic Potential Against Pancreatic Adenocarcinoma PANC -1 Cells

Q4 · MEDICINE

Article

Author: Bhushan, Shashi ; Joshi, Amit ; Shah, Bhahwal Ali ; Batra, Navneet ; Guru, Santosh Kumar ; Malik, Fayaz Ahmad ; Kumar, Ajay ; Singh, Jagtar ; Goswami, Akshra

Pancreatic ductal adenocarcinoma (PDA) remains one of the deadliest types of cancers. Median survival rate is very poor with the currently available chemotherapeutical regimens. Therefore, discovery of new antineoplastic agents against PDA is one of the focused areas of contemporary research. The present study was undertaken to explore the antitumour activity of a potent parthenin analog P16. Among PANC-1, Mia PaCa-2 and AsPC-1 pancreatic cancer cells, PANC-1 showed highest sensitivity to P16 with an IC50 value of 3.4 μM. Time dependent cell cycle studies revealed that P16 suppressed the growth of PANC-1 cells by arresting the progression through the cell cycle in G2/M phase via downregulation of cyclin B1 and cyclin A. However, P16 did not alter the expressions of CDK-1 and CDC25C in PANC-1 cells. The P16 induced cell cycle arrest, which consequently, led to induction of apoptosis, which was accompanied by activation of caspase-9 and -3. Interestingly, PANC-1 cells displayed increasing loss of mitochondrial potential, which seemed to be correlated to the activation of caspase-3. Additionally, P16 was also able to down-regulate the cell migration in PANC-1 cells. Furthermore, P16 treatment of hypoxic PANC-1 cells strongly suppressed the expression of proangiogenic factors VEGFR-2, HIF1α and HIF1β. Antiangiogenic ability of P16 was also reflected in the human umbilical vascular endothelial cells (HUVECs), where it effectively suppressed the migration and inhibited the formation of the tube in a matrigel based assay. Therefore, cytostatic and antiangiogenic properties of P16 against pancreatic adenocarcinoma cells make it a suitable candidate for further investigation.

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Indication	Highest Phase	Country/Location	Organization	Date
Arteriosclerosis	Discovery	US	13therapeutics	-
Inflammatory Bowel Diseases	Discovery	US	13therapeutics	-

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