The devastating appearance of numerous drug-unresponsive strains of Leishmania donovani and severe toxic side effects of conventional antileishmanial therapy necessitates the search for novel leads, to treat visceral leishmaniasis efficiently. The current study deals with the synthesis and biological evaluation of a unique C-5 functionalized oxindole based polyphenol to ascertain its activities against L. donovani infection, in vitro. The polyhydroxylated oxindole derivative (1) was generated by coupling styrene derivatives with 5-bromo bis-arylidene oxindole using Heck coupling reaction. The synthesized molecule 1 was tested for its antileishmanial activity using both promastigote and amastigote stages of L. donovani. Molecule 1 showed promising anti-promastigote and anti-amastigote activities with IC values 15 µM and 1 µM, respectively, with no cytotoxicity towards host splenocytes. The results revealed that this compound induced parasite death by promoting oxidative stress, thereby triggering apoptosis.
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http://dx.doi.org/10.1016/j.bmcl.2018.02.023 | DOI Listing |
Cancer Cell Int
December 2024
Department of General Surgery, Affiliated Zhongda Hospital of Southeast University, Nanjing, 210009, China.
Insulin-like growth factor II mRNA-binding proteins (IGF2BPs), a family of RNA-binding proteins, are pivotal in regulating RNA dynamics, encompassing processes such as localization, metabolism, stability, and translation through the formation of ribonucleoprotein complexes. First identified in 1999 for their affinity to insulin-like growth factor II mRNA, IGF2BPs have been implicated in promoting tumor malignancy behaviors, including proliferation, metastasis, and the maintenance of stemness, which are associated with unfavorable outcomes in various cancers. Additionally, non-coding RNAs (ncRNAs), particularly long non-coding RNAs, circular RNAs, and microRNAs, play critical roles in cancer progression through intricate protein-RNA interactions.
View Article and Find Full Text PDFCardiovasc Diabetol
December 2024
Cardiovascular Research Institute, Icahn School of Medicine at Mount Sinai, 1470 Madison Ave, s7-119, New York, NY, USA.
Background: Long-term consumption of Western Diet (WD) is a well-established risk factor for the development of cardiovascular disease (CVD); however, there is a paucity of studies on the long-term effects of WD on the pathophysiology of CVD and sex-specific responses.
Methods: Our study aimed to investigate the sex-specific pathophysiological changes in left ventricular (LV) function using transthoracic echocardiography (ECHO) and LV tissue transcriptomics in WD-fed C57BL/6 J mice for 125 days, starting at the age of 300 through 425 days.
Results: In female mice, consumption of the WD diet showed long-term effects on LV structure and possible development of HFpEF-like phenotype with compensatory cardiac structural changes later in life.
Spectrochim Acta A Mol Biomol Spectrosc
December 2024
Department of Chemistry, COMSATS University, Abbottabad 22060, KPK, Pakistan.
The ruthenium compounds have been known to have the wide range of potential applications as anticancer, antibacterial and anti-diabetic etc. The ligand substitutions play a vital role in enhancing the pharmacological and biological activities. In the present study, three ruthenium-metal based complexes, designated as (I-III), were synthesized and characterized employing element analysis, FTIR and HNMR.
View Article and Find Full Text PDFBiomed Chromatogr
January 2025
State Key Laboratory of Radiation Medicine and Protection, School of Radiation Medicine and Protection, Medical College of Soochow University, Collaborative Innovation Center of Radiological Medicine of Jiangsu Higher Education Institutions, Soochow University, Suzhou, China.
An animal model of radiation-induced lung injury (RILI) was established using female rats given sublethal whole-thorax X-ray irradiation (15 Gy) at a dose rate of 2.7 Gy/min. The rats were studied for up to day 45 and compared with sham-irradiated controls.
View Article and Find Full Text PDFExp Cell Res
December 2024
School of Life Science and Key Laboratory of the Ministry of Education for Experimental Teratology, Shandong University, Qingdao, 266237, China; Department of Pharmacology, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, 250100, China. Electronic address:
Spermatogenesis and sperm maturation are complex biological processes that involve intricate cellular and molecular interactions. The Aldh2 gene is involved in the metabolism of specific aldehydes generated by oxidative stress. Aldh2 is abundantly expressed in the testis and epididymis; however, the specific role of Aldh2 in regulating spermatogenesis and sperm maturation remains unclear.
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