Biological Evaluation of Endophytic Fungus, Chaetomium globosum JN711454, as Potential Candidate for Improving Drug Discovery

2013 ◽  
Vol 68 (1) ◽  
pp. 67-82 ◽  
Author(s):  
Khaled A. Selim ◽  
Ahmed A. El-Beih ◽  
Tahany M. Abdel-Rahman ◽  
Ahmed I. El-Diwany
Keyword(s):  
Drug Discovery ◽  
Endophytic Fungus ◽  
Biological Evaluation ◽  
Chaetomium Globosum ◽  
Potential Candidate

scholarly journals Biological Evaluation of Endophytic Fungus Chaetomium sp. NF15 of Justicia adhatoda L.: A Potential Candidate for Drug Discovery

2016 ◽  
Vol Inpress (Inpress) ◽  
Author(s):  
Nighat Fatima ◽  
Usman Mukhtar ◽  
Ihsan-Ul-Haq ◽  
Muneer Ahmed Qazi ◽  
Muniba Jadoon ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Endophytic Fungus ◽  
Biological Evaluation ◽  
Potential Candidate ◽  
Justicia Adhatoda

Novel Conjugated Quinazolinone-Based Hydroxamic Acids: Design, Synthesis and Biological Evaluation

2020 ◽  
Vol 16 ◽  
Author(s):  
Tran Khac Vu ◽  
Nguyen Thi Thanh ◽  
Nguyen Van Minh ◽  
Nguyen Huong Linh ◽  
Nguyen Thi Phương Thao ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Cell Lines ◽  
Cancer Cell ◽  
Hdac Inhibitors ◽  
Cancer Cell Lines ◽  
Hydroxamic Acids ◽  
Biological Evaluation ◽  
Hdac Inhibition ◽  
Ic50 Value ◽  
Mcf 7

Background: Target-based approach to drug discovery currently attracts a great deal of interest from medicinal chemists in anticancer drug discovery and development. Histone deacetylase (HDAC) inhibitors represent an extensive class of targeted anti-cancer agents. Among the most explored structure moieties, hydroxybenzamides and hydroxypropenamides have been demonstrated to have potential HDAC inhibitory effects. Several compounds of these structural classes have been approved for clinical uses to treat different types of cancer, such as vorinostat and belinostat. Aims: This study aims at developing novel HDAC inhibitors bearing conjugated quinazolinone scaffolds with potential cytotoxicity against different cancer cell lines. Method: A series of novel N-hydroxyheptanamides incorporating conjugated 6-hydroxy-2 methylquinazolin-4(3H)- ones (15a-l) was designed, synthesized and evaluated for HDAC inhibitory potency as well as cytotoxicity against three human cancer cell lines, including HepG-2, MCF-7 and SKLu-1. Molecular simulations were finally performed to gain more insight into the structure-activity. relationships. Results: It was found that among novel conjugated quinazolinone-based hydroxamic acids synthesized, compounds 15a, 15c and 15f were the most potent, both in terms of HDAC inhibition and cytotoxicity. Especially, compound 15f displayed up to nearly 4-fold more potent than SAHA (vorinostat) in terms of cytotoxicity against MCF-7 cell line with IC50 value of 1.86 µM, and HDAC inhibition with IC50 value of 6.36 µM. Docking experiments on HDAC2 isozyme showed that these compounds bound to HDAC2 with binding affinities ranging from -10.08 to -14.93 kcal/mol compared to SAHA (-15.84 kcal/mol). It was also found in this research that most of the target compounds seemed to be more cytotoxic toward SKLu-1than MCF-7 and HepG-2. Conclusion: The resesrch results suggest that some hydroxamic acids could emerge for further evaluation and the results are well served as basics for further design of more potent HDAC inhibitors and antitumor agents.

scholarly journals Synthesis and Biological Evaluation of a Novel Glycidyl Metharcylate/Phaytic Acid-Based on Bagasse Xylan Composite Derivative

Polymers ◽  
2021 ◽  
Vol 13 (13) ◽  
pp. 2084
Author(s):  
Mingkun Li ◽  
Heping Li ◽  
Hongli Liu ◽  
Zhiming Zou ◽  
Chaoyu Xie
Keyword(s):  
Lung Cancer ◽  
Thermal Stability ◽  
Ionic Liquid ◽  
Molecular Docking ◽  
Phytic Acid ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Potential Candidate ◽  
Reaction Conditions ◽  
Cell Proliferation Inhibition

The development of natural biomass materials with excellent properties is an attractive way to improve the application range of natural polysaccharides. Bagasse Xylan (BX) is a natural polysaccharide with various biological activities, such as antitumor, antioxidant, etc. Its physic-chemical and biological properties can be improved by functionalization. For this purpose, a novel glycidyl metharcylate/phytic acid based on a BX composite derivative was synthesized by a free radical polymerization technique with glycidyl metharcylate (GMA; GMABX) and further esterification with phytic acid (PA; GMABX-PA) in ionic liquid. The effects of the reaction conditions (i.e., temperature, time, initiator concentration, catalyst concentration, GMA concentration, PA concentration, mass of ionic liquid) on grafting rate(G), conversion rate(C) and degree of substitution(DS) are discussed. The structure of the composite material structure was confirmed by FTIR, 1H NMR and XRD. SEM confirmed the particle morphology of the composite derivative. The thermal stability of GMABX-PA was determined by TG-DTG. Molecular docking was further performed to study the combination mode of the GMABX-PA into the active site of two lung cancer proteins (5XNV, 2EB2) and a blood cancer protein (2M6N). In addition, tumor cell proliferation inhibition assays for BX, GMABX-PA were carried out using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetraz -olium bromide (MTT) method. The results showed that various reaction conditions exhibited favorable gradient curves, and that a maximum G of 56% for the graft copolymerization and a maximum DS of 0.267 can be achieved. The thermal stability was significantly improved, as demonstrated by the fact that there was still 60% residual at 800 °C. The molecular docking software generated satisfactory results with regard to the evaluated binding energy and combining sites. The inhibition ratio of GMABX-PA on NCI-H460 (lung cancer cells) reached 29.68% ± 4.45%, which is five times higher than that of BX. Therefore, the material was shown to be a potential candidate for biomedical applications as well as for use as a heat resistant material.

Antifungal metabolites from Chaetomium globosum, an endophytic fungus in Ginkgo biloba

2011 ◽  
Vol 39 (4-6) ◽  
pp. 876-879 ◽  
Author(s):  
Hu-Qiang Li ◽  
Xiao-Jun Li ◽  
You-Lin Wang ◽  
Qiang Zhang ◽  
An-Ling Zhang ◽  
...  
Keyword(s):  
Ginkgo Biloba ◽  
Endophytic Fungus ◽  
Chaetomium Globosum ◽  
Antifungal Metabolites

Bioactive metabolites from the desert plant-associated endophytic fungus Chaetomium globosum (Chaetomiaceae)

2021 ◽  
Vol 185 ◽  
pp. 112701
Author(s):  
Xiao-Yan Zhang ◽  
Xiang-Mei Tan ◽  
Meng Yu ◽  
Jian Yang ◽  
Bing-Da Sun ◽  
...  
Keyword(s):  
Endophytic Fungus ◽  
Chaetomium Globosum ◽  
Bioactive Metabolites ◽  
Desert Plant

scholarly journals Secondary Metabolites of the Endophytic Fungus Chaetomium globosum Isolated From Coptis chinensis

2021 ◽  
Vol 16 (9) ◽  
pp. 1934578X2110445
Author(s):  
Jia-Cheng Ji ◽  
Pan-Pan Wei ◽  
Xiao-Yang Han ◽  
Zheng-Hui Li ◽  
Hong-Lian Ai ◽  
...  
Keyword(s):  
Endophytic Fungus ◽  
Early Childhood Development ◽  
Childhood Development ◽  
Chaetomium Globosum ◽  
Resonance Spectroscopy ◽  
Ionization Mass ◽  
Two Dimensional ◽  
Coptis Chinensis ◽  
Relative Configuration ◽  
One Dimensional

A new steroid, chaetglotone (1), together with 3 known compounds (2-4), were isolated from Chaetomium globosum, which is an endophytic fungus isolated from the root of Coptis chinensis Franch . The new compound was characterized by one-dimensional and two-dimensional nuclear magnetic resonance spectroscopy and high-resolution electrospray ionization mass spectrometer. The relative configuration and absolute configuration of 1 were further determined via the DP4 + and Early Childhood Development protocols, separately.

scholarly journals Synthesis and biological evaluation of fluoro-substituted spiro-isoxazolines as potential anti-viral and anti-cancer agents

RSC Advances ◽  
2020 ◽  
Vol 10 (50) ◽  
pp. 30223-30237
Author(s):  
Prasanta Das ◽  
Sarah Boone ◽  
Dipanwita Mitra ◽  
Lindsay Turner ◽  
Ritesh Tandon ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Biological Evaluation ◽  
Biological Relevance ◽  
Anti Cancer ◽  
Synthesis And Biological Evaluation

The synthetic efficacy and biological relevance extend an opportunity to further drug-discovery development of fluoro-spiro-isoxazolines as novel anti-viral and anti-cancer agents.

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