AI Article Synopsis
- Researchers designed and synthesized quillaic acid derivatives with various substituents on the 28-carboxyl group to test their effectiveness against human cancer cells.
- Five cancer cell lines were examined, and some derivatives exhibited better antiproliferative activity compared to the original quillaic acid.
- One specific compound showed significant efficacy, being about four times more effective than quillaic acid against HCT116 cells, and it works by inducing cell cycle arrest and apoptosis through specific cellular pathways.
Article Abstract
A series of quillaic acid derivatives with different substituents on the 28-carboxyl group were designed and synthesized. Five human cancer cell lines (HCT116, BEL7402, HepG2, SW620, and MCF-7) were evaluated for their antitumor activity Some of the tested derivatives showed improved antiproliferative activity compared to the lead compound, quillaic acid. Among them, compound (IC = 2.46 ± 0.44 μM) showed the strongest antiproliferative activity against HCT116 cells; compared with quillaic acid (IC > 10 μM), its efficacy against HCT116 cancer cells was approximately 4-fold higher than that of quillaic acid. Compound also induces cell cycle arrest and apoptosis by modulating NF-κB and MAPK pathways. Therefore, the development of compound is certainly valuable for anti-tumor applications.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9490060 | PMC |
| http://dx.doi.org/10.3389/fchem.2022.951713 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Synthesis of Quillaic Acid through Sustainable C-H Bond Activations.
J Org Chem
April 2024
School of Pharmacy, College of Medicine, National Taiwan University, Taipei 100, Taiwan.
To meet the demand for quillaic acid, a multigram synthesis of quillaic acid was accomplished in 14 steps, starting from oleanolic acid, leading to an overall yield of 3.4%. Key features include C-H activation at C-16 and C-23.
View Article and Find Full Text PDFCombinatorial optimization and spatial remodeling of CYPs to control product profile.
Metab Eng
November 2023
Shenzhen Key Laboratory for the Intelligent Microbial Manufacturing of Medicines, Shenzhen Institute of Advanced Technology, Chinese Academy of Sciences, Shenzhen, 518055, China; CAS Key Laboratory of Quantitative Engineering Biology, Shenzhen Institute of Synthetic Biology, Shenzhen Institute of Advanced Technology, Chinese Academy of Sciences, Shenzhen, 518055, China; Center for Synthetic Biochemistry, Shenzhen Institute of Synthetic Biology, Shenzhen Institute of Advanced Technology, Chinese Academy of Sciences, 518055, China. Electronic address:
Activating inert substrates is a challenge in nature and synthetic chemistry, but essential for creating functionally active molecules. In this work, we used a combinatorial optimization approach to assemble cytochrome P450 monooxygenases (CYPs) and reductases (CPRs) to achieve a target product profile. By creating 110 CYP-CPR pairs and iteratively screening different pairing libraries, we demonstrated a framework for establishing a CYP network that catalyzes six oxidation reactions at three different positions of a chemical scaffold.
View Article and Find Full Text PDFTriterpenoid saponins from Psammosilene tunicoides and their antinociceptive activities.
Phytochemistry
October 2023
Key Laboratory of Chemistry in Ethnic Medicinal Resources, State Ethnic Affairs Commission and Ministry of Education, School of Ethnic Medicine, Yunnan Minzu University, Kunming, 650504, Yunnan, China. Electronic address:
Herein, five undescribed oleanane-type triterpenoid saponins, namely, psammosaponins A-E, along with nine known compounds, were isolated from the roots of Psammosilene tunicoides. Moreover, part of the ethanolic extract of P. tunicoides was acid-hydrolyzed and three aglycones were isolated from the resulting hydrolysate.
View Article and Find Full Text PDFModulators of diabetic neuropathy and inflammation from : Isolation of active phytochemicals and potential mechanisms of action.
J Tradit Complement Med
May 2023
Department of Pharmacology, Faculty of Pharmacy, Arab International University, Damascus, Syria.
Background And Aim: Natural metabolites are rich in neuroactive and anti-inflammatory phytochemicals. Soapwort or (Sap) has been utilized for its immunomodulatory and ant-rheumatic properties. Thus, the aim is to exploit Sap phytochemically and to investigate Sap isolated active phytochemicals effect to modulate diabetic neuropathy and inflammation, and their possible mechanisms of action.
View Article and Find Full Text PDFPhytotoxicity of Leaf Saponins and Their Bioherbicide Potential.
Plants (Basel)
February 2023
Plant Physiology Laboratory, Center for Biotechnology and Department of Botany, Federal University of Rio Grande do Sul, Porto Alegre 91501-970, RS, Brazil.
Weeds are major threats to the integrity of agricultural and natural environments due to their invasive and competing potential. Bioherbicides are substances based on natural compounds that are biodegradable and often have low residual effects. Plant species able to produce and release phytotoxic compounds may represent effective bioherbicide sources.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!