The targeting of pro-inflammatory enzymes becomes a therapeutic intervention when acute inflammation is proliferating in pathological conditions. This research is intended to carry out an evaluation of inhibiting and inducing enzymes with inflammatory associations with 28 cyclohexanone analogs based on the ligustrazine. Tests were undertaken with inhibitor screening assay kits using a range of synthetic compounds to investigate how they could inhibit the activity of cyclooxygenase (COX) enzymes, secretory phospholipase A (sPLA), and lipoxygenase (LOX) enzyme. Significant and similar inhibitory activities against sPLA with were noted with synthetic compounds which included 1f and 1g (IC = 2.2 μM). The optimal inhibitory activity regarding LOX enzyme was shown with compounds 1d (IC = 8.1 μM) and 1e (IC = 7.5 μM). Additionally, the compounds 1b, 1d, 1e, 2n, and 2o were shown to be significant inhibitors of COX-1 activity with IC values 0.09 to 0.7 μM. The outcomes of assays for COX inhibition demonstrated that the same compounds had a further strong inhibitive influence on the COX-2 enzyme, and certain compounds such as 1d, 1e, and 2n demonstrated enhanced potency compared with positive controls.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.ejps.2020.105299 | DOI Listing |
Bioorg Chem
January 2025
State Key Laboratory of Mycology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China; University of Chinese Academy of Sciences, Beijing 100049, China. Electronic address:
Thirteen new meroterpenoids, acremorins A-M (1, 2, 4, 6, 7 and 9-16), together with three known analogues (3, 5 and 8) were isolated from the deep-sea-derived fungus Acremonium sclerotigenum LW14 guided by the genomic and OSMAC strategy. Their structures and absolute configurations were established by extensive spectroscopic analysis, electronic circular dichroism (ECD) calculations, Rh(OCOCF)-induced ECD experiments, and a single-crystal X-ray diffraction experiment. Compounds 2, 4, 6 and 9 represent the rare brominated ascochlorins.
View Article and Find Full Text PDFAnticancer Agents Med Chem
January 2025
Department of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, UPM, Serdang, 43400, Selangor, Malaysia.
Background: Colorectal cancer (CRC) is the second-leading cause of cancer-related deaths. Curcumin has been reported to have suppressive effects in CRC and to address the physiological limitations of curcumin, a chemically synthesized curcuminoid analog, known as (2E,6E)-2,6-Bis (2,3-Dimethoxy benzylidine) cyclohexanone (DMCH), was developed and the anti-metastatic and anti-angiogenic properties of DMCH in colorectal cell line, SW620 were examined.
Methods: The anti-metastatic effects of DMCH were examined in the SW620 cell line by scratch assay, migration, and invasion assay, while for anti-angiogenesis properties of the cells, the mouse aortic ring assay and Human Umbilical Vein Endothelial Cells (HUVEC) assay were conducted.
Sci Total Environ
December 2024
School of Environment and Resource, Southwest University of Science and Technology, Mianyang, China.
Ketamine analogues are rapidly emerging around the world and are considered one of the new psychoactive substances (NPS) of greatest concern. However, little is known about their actual use at the community level and their evolution on the drug market. Wastewater-based epidemiology is a useful tool to explore the profile of NPS use.
View Article and Find Full Text PDFWorld J Microbiol Biotechnol
November 2024
Laboratory of Photobiology and Molecular Microbiology, Department of Botany, Institute of Science, Banaras Hindu University, Varanasi, 221005, India.
Mycosporine-like amino acids (MAAs) are a unique class of UV-screening bioactive molecules with potent antioxidants and photoprotective properties, synthesized by various species of cyanobacteria in different habitats. The cyanobacterial biofilms play a crucial driver in the development of ecological communities. The current study examined the existence of the photoprotective MAAs in a novel epilithic cyanobacterium Lyngbya sp.
View Article and Find Full Text PDFHeliyon
October 2024
Department of Chemistry, Periyar Maniammai Institute of Science and Technology, Thanjavur, 613403, Tamilnadu, India.
The initiation of colorectal cancer is controlled by various factors, including random occurrences and genetic alterations affecting oncogenes and tumor suppressor genes.Curcumin, a significant compound extracted from turmeric, has attracted interest for its robust anticancer properties, particularly regarding its analogs, 2, 6-bisdifurfurylidene cyclohexanone (DFC) and 2, 6-bis (2, 6-dichlorobenzylidene) cyclohexanone (DCC), which were synthesized and assessed for their anticancer efficacy. A combination of spectroscopic techniques and molecular docking methods was utilized to comprehensively evaluate the interaction behaviors of DFC and DCC.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!