A new cytotoxic compound from the leaves of Styrax annamensis Guillaumin

AbstractMechanistic toxicology is gaining weight for human health risk assessment. Different mechanistic assays are available, such as the comet assay, which detects DNA damage at the level of individual cells. However, the conventional alkaline version only detects strand breaks and alkali-labile sites. We have validated two modifications of the in vitro assay to generate mechanistic information: (1) use of DNA-repair enzymes (i.e., formamidopyrimidine DNA glycosylase, endonuclease III, human 8-oxoguanine DNA glycosylase I and human alkyladenine DNA glycosylase) for detection of oxidized and alkylated bases as well as (2) a modification for detecting cross-links. Seven genotoxicants with different mechanisms of action (potassium bromate, methyl methanesulfonate, ethyl methanesulfonate, hydrogen peroxide, cisplatin, mitomycin C, and benzo[a]pyrene diol epoxide), as well as a non-genotoxic compound (dimethyl sulfoxide) and a cytotoxic compound (Triton X-100) were tested on TK-6 cells. We were able to detect with high sensitivity and clearly differentiate oxidizing, alkylating and cross-linking agents. These modifications of the comet assay significantly increase its sensitivity and its specificity towards DNA lesions, providing mechanistic information regarding the type of damage.

Download Full-text

Streptokordin, a New Cytotoxic Compound of the Methylpyridine Class from a Marine-derived Streptomyces sp. KORDI-3238

The Journal of Antibiotics ◽

10.1038/ja.2006.33 ◽

2006 ◽

Vol 59 (4) ◽

pp. 234-240 ◽

Cited By ~ 51

Author(s):

Seong-Yun Jeong ◽

Hee Jae Shin ◽

Tae Sik Kim ◽

Hyi-Seung Lee ◽

Song-kyu Park ◽

...

Keyword(s):

Streptomyces Sp ◽

Cytotoxic Compound

Download Full-text

Identification of norharman as the cytotoxic compound produced by the sponge (Hymeniacidon perleve)-associated marine bacterium Pseudoalteromonas piscicida and its apoptotic effect on cancer cells

Biotechnology and Applied Biochemistry ◽

10.1042/ba20050176 ◽

2006 ◽

Vol 44 (3) ◽

pp. 135 ◽

Cited By ~ 35

Author(s):

Xiaojun Yan ◽

Li Zheng ◽

Xiaotian Han ◽

Haimin Chen ◽

Wei Lin ◽

...

Keyword(s):

Cancer Cells ◽

Marine Bacterium ◽

Cytotoxic Compound ◽

Apoptotic Effect

Download Full-text

Synthesis, structural characterization and cytotoxicity of a new proton transfer compound based on 2,4-diamino-1,3,5-triazine: an experimental and computational study

New Journal of Chemistry ◽

10.1039/d1nj03674b ◽

2021 ◽

Author(s):

Khodayar Gholivand ◽

Leila Sarmadi ◽

Nasrin Fallah ◽

Mohammad Feraghi ◽

Michal Dušek ◽

...

Keyword(s):

Proton Transfer ◽

Structural Characterization ◽

Computational Study ◽

Water Soluble ◽

Cytotoxic Compound ◽

Proton Transfer Compound

In the present study, a new water-soluble proton transfer cytotoxic compound (dpp)(dapt).H2O (Dx) (where dpp = diphenylphosphinate and dapt = 2,6-diamino-4-phenyl-1,3,5-triazin-1-ium ) was synthesized and characterized by IR and NMR...

Download Full-text

Anticancer, antimicrobial and antioxidant potential of sterically tuned bis-N-heterocyclic salts

Zeitschrift für Naturforschung C ◽

10.1515/znc-2018-0095 ◽

2018 ◽

Vol 74 (1-2) ◽

pp. 17-23 ◽

Cited By ~ 2

Author(s):

Noor ul Huda ◽

Shamsul Islam ◽

Muhammad Zia ◽

Kainaat William ◽

Fakhar i Abbas ◽

...

Keyword(s):

Breast Adenocarcinoma ◽

Benzimidazole Derivatives ◽

Alkyl Aryl ◽

Cytotoxic Compound ◽

Sulforhodamine B ◽

Hct 116 ◽

Mrsa Strains ◽

Pharmacological Potential ◽

Derivatives Of ◽

Lipophilic Character

AbstractThe current study was conducted to evaluate the antimicrobial, antioxidant, antileishmanial and cytotoxic potential of designed derivatives of 1,1′-(1,3-phenylenebis(methylene))bis(3-alkyl/aryl-1H-benzimidazol-3-ium) salts. The antibacterial potential of the test compounds was investigated againstStaphylococcus aureus, Pseudomonas aeruginosaand two methicillin-resistantS. aureus(MRSA) strains (MRSA10, MRSA11), where compound6showed the best results. For brine shrimp lethality bioassay (BSLB), compound6again showed up to 100% mortality at 200 μg/mL and 56.7% mortality at 6.25 μg/mL. Antileishmanial assay was performed againstLeishmania tropicaat 20 μg/mL dosage, where6showed the most promising activity with 16.26% survival (83.74% mortality; IC50=14.63 μg/mL). The anticancer potential of the selected benzimidazole derivatives was evaluated against two selected cell lines (human colorectal cancer, HCT-116 and breast adenocarcinoma, MCF-7) using sulforhodamine B (SRB) assay. Compound6was found to be the most effective cytotoxic compound with 75% inhibition of HCT-116 proliferation at 1 mg/mL concentration. Succinctly,6exhibited impressive pharmacological potential that might be attributed to its higher lipophilic character owing to the longer N-substituted alkyl chains when compared to the other test compounds.

Download Full-text

New Protein Vector ApE1 for Targeted Delivery of Anticancer Drugs

Journal of Biomedicine and Biotechnology ◽

10.1155/2012/469756 ◽

2012 ◽

Vol 2012 ◽

pp. 1-5 ◽

Cited By ~ 2

Author(s):

N. V. Pozdniakova ◽

N. V. Gorokhovets ◽

N. V. Gukasova ◽

A. V. Bereznikova ◽

E. S. Severin

Keyword(s):

Targeted Delivery ◽

Tumor Targeting ◽

Drug Loading ◽

Bacterial Biomass ◽

Receptor Binding Domain ◽

Producer Strain ◽

E Coli ◽

Cytotoxic Compound ◽

Soluble State ◽

New Protein

A new chimeric geneApE1encoding the receptor-binding domain of the humanalpha-fetoprotein fused to a sequence of 22 glutamic acid residues was constructed. A new bacterial producer strainE. coliSHExT7 ApE1 was selected for ApE1 production in a soluble state. A simplified method was developed to purify ApE1 from bacterial biomass. It was shown that the new vector protein selectively interacts with AFP receptors on the tumor cell surface and can be efficiently accumulated in tumor cells. In addition, ApE1 was shown to be stable in storage and during its chemical modification. An increased number of carboxyl groups in the molecule allows the production of cytotoxic compound conjugates with higher drug-loading capacity and enhanced tumor targeting potential.

Download Full-text

Resistoflavine, cytotoxic compound from a marine actinomycete, Streptomyces chibaensis AUBN1/7

Microbiological Research ◽

10.1016/j.micres.2006.01.012 ◽

2007 ◽

Vol 162 (4) ◽

pp. 322-327 ◽

Cited By ~ 46

Author(s):

Adinarayana Gorajana ◽

Venkatesan M ◽

Saisha Vinjamuri ◽

Bapiraju V.V.S.N. Kurada ◽

Sujatha Peela ◽

...

Keyword(s):

Cytotoxic Compound ◽

Marine Actinomycete

Download Full-text

Design, synthesis and biological evaluation of novel benzodioxole derivatives as COX inhibitors and cytotoxic agents

BMC Chemistry ◽

10.1186/s13065-020-00706-1 ◽

2020 ◽

Vol 14 (1) ◽

Cited By ~ 1

Author(s):

Mohammed Hawash ◽

Nidal Jaradat ◽

Saba Hameedi ◽

Ahmed Mousa

Keyword(s):

Cancer Cell Line ◽

Biological Evaluation ◽

Cytotoxic Agents ◽

Cervical Cancer Cell Line ◽

Moderate Activity ◽

Selectivity Ratio ◽

Design Synthesis ◽

Cox Inhibitors ◽

Cytotoxic Compound

Abstract Non-steroidal anti-inflammatory drugs are among the most used drugs. They are competitive inhibitors of cyclooxygenase (COX). Twelve novel compounds (aryl acetate and aryl acetic acid groups) were synthesized in this work in order to identify which one was the most potent and which group was most selective towards COX1 and COX2 by using an in vitro COX inhibition assay kit. The cytotoxicity was evaluated for these compounds utilizing MTS assay against cervical carcinoma cells line (HeLa). The synthesized compounds were identified using FTIR, HRMS, 1H-NMR, and 13C-NMR techniques. The results showed that the most potent compound against the COX1 enzyme was 4f with IC50 = 0.725 µM. The compound 3b showed potent activity against both COX1 and COX2 with IC50 = 1.12 and 1.3 µM, respectively, and its selectivity ratio (0.862) was found to be better than Ketoprofen (0.196). In contrast, compound 4d was the most selective with a COX1/COX2 ratio value of 1.809 in comparison with the Ketoprofen ratio. All compounds showed cytotoxic activity against the HeLa Cervical cancer cell line at a higher concentration ranges (0.219–1.94 mM), and the most cytotoxic compound was 3e with a CC50 value of 219 µM. This was tenfold more than its IC50 values of 2.36 and 2.73 µM against COX1 and COX2, respectively. In general, the synthesized library has moderate activity against both enzymes (i.e., COX1 and COX2) and ortho halogenated compounds were more potent than the meta ones.

Download Full-text