scholarly journals 7-Hydroxycoumarin Elicit Anti-Angiogenic Effects Through Cellular Apoptosis in Developing Embryos of Zebrafish (Danio Rerio)

2017 ◽  
Vol 13 (21) ◽  
pp. 53 ◽  
Author(s):  
Narshimamurthy Anegundi ◽  
Katti Pancharatna
Keyword(s):  
Danio Rerio ◽  
Biological Activities ◽  
Developmental Trajectory ◽  
Hydroxy Derivative ◽  
Cardinal Vein ◽  
Angiogenic Potential ◽  
Pharmacological Significance ◽  
Cellular Apoptosis ◽  
Derivatives Of ◽  
Posterior Cardinal Vein

Derivatives of coumarin have diverse biological activities and pharmacological significance. In this study we made an attempt to test one of the hydroxy derivative i.e. 7-hydroxycoumarin (7HC) for its anti-angiogenic potential using embryonic angiogenesis of zebrafish (Danio rerio) as biological model. Developing embryos of D. rerio were cultured in media containing one of the grade (1 mM or 2 mM or 3 mM or 4 mM or 5 mM) of concentration of 7HC from gastrula stage (~6 hrs post fertilization - hpf) until completion of embryonic development and hatching (72 hpf). Developmental trajectory of each post hatched larva was traced for two weeks. Angiogenesis and patterning of major blood vessels occurred in zebrafish embryos/ larvae between 24 - 72 hpf in controls. Exposure to 7HC resulted in an impairment in patterning of inter segmental vessels (ISVs) dorsal aorta (DA), dorsal longitudinal anastomotic vessel (DLAV), posterior cardinal vein (PCV), and common cardinal veins (CCVs) accompanied by increased site specific cellular apoptosis, declined heart rates in a dosedependent manner. 7HC manifest anti-angiogenic effects mediated/ induced through cellular apoptosis, hence may deserve attention and consideration as tumour angiogenesis suppressors in malignancy therapeutics.

Synthesis, characterization and biological activities of 1,3,4-oxadiazole derivatives of nalidixic acid and their copper complexes

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Nalidixic Acid ◽  
Copper Complexes ◽  
Biological Activities ◽  
Bidentate Coordination ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Oxadiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Substituted 1

A series of novel 1, 3, 4-oxadiazole analogues was synthesized from cyclization of hydrazones of substituted 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carbohydrazides were prepared from nalidixic acid. The structures of synthesized oxadiazole derivatives and their copper complexes were elucidated on the basis of FTIR, elemental analyses, 1H-NMR and atomic absorption spectral analysis. It was observed from spectral data that metal ligand ratio was 1:1 in all copper complexes and they were bidentate, coordination was found to be done through oxygen of 4-oxo group and nitrogen of oxadiazole ring. The synthesized compounds were further evaluated with biological activities and compared with parent hydrazones. Copper complexes possess antibacterial and antifungal activities better than the oxadiazoles while they have better antioxidant activity then copper complexes. Parent hydrazones were better in all biological activities than synthesized oxadiazoles.

scholarly journals Synthesis, Antiproliferative Activity and Radical Scavenging Ability of 5-O-Acyl Derivatives of Quercetin

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1608
Author(s):  
Stephen Lo ◽  
Euphemia Leung ◽  
Bruno Fedrizzi ◽  
David Barker
Keyword(s):  
Antiproliferative Activity ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Breast Cancer Cell Lines ◽  
Scavenging Activity ◽  
Plant Materials ◽  
Wide Range ◽  
Derivatives Of ◽  
Acyl Derivatives

Quercetin is a flavonoid that is found in many plant materials, including commonly eaten fruits and vegetables. The compound is well known for its wide range of biological activities. In this study, 5-O-acyl derivatives of quercetin were synthesised and assessed for their antiproliferative activity against the HCT116 colon cancer and MDA-MB-231 breast cancer cell lines; and their radical scavenging activity against the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical species. Four derivatives were found to have improved the antiproliferative activity compared to quercetin whilst retaining radical scavenging activity.

Nodal induces ectopic goosecoid and lim1 expression and axis duplication in zebrafish

Development ◽  
1995 ◽  
Vol 121 (2) ◽  
pp. 383-391 ◽  
Author(s):  
R. Toyama ◽  
M.L. O'Connell ◽  
C.V. Wright ◽  
M.R. Kuehn ◽  
I.B. Dawid
Keyword(s):  
Pattern Formation ◽  
Danio Rerio ◽  
Biological Activities ◽  
Mouse Embryos ◽  
Zebrafish Embryos ◽  
Gene Encoding ◽  
Dorsal Axis ◽  
Vertebrate Embryo ◽  
Mesoderm Formation ◽  
Intercellular Signalling

One of the first intercellular signalling events in the vertebrate embryo leads to mesoderm formation and axis determination. In the mouse, a gene encoding a new member of the TGF-beta superfamily, nodal, is disrupted in a mutant deficient in mesoderm formation (Zhou et al., 1993, Nature 361, 543). nodal mRNA is found in prestreak mouse embryos, consistent with a role in the development of the dorsal axis. To examine the biological activities of nodal, we have studied the action of this factor in eliciting axis determination in the zebrafish, Danio rerio. Injection of nodal mRNA into zebrafish embryos caused the formation of ectopic axes that included notochord and somites. Axis duplication was preceded by the generation of an apparent ectopic shield (organizer equivalent) in nodal-injected embryos, as indicated by the appearance of a region over-expressing gsc and lim1; isolation and expression in the shield of the lim1 gene is reported here. These results suggest a role for a nodal-like factor in pattern formation in zebrafish.

Immobilisation on polystyrene of diazirine derivatives of mono- and disaccharides: biological activities of modified surfaces

2001 ◽  
Vol 9 (11) ◽  
pp. 2943-2953 ◽  
Author(s):  
Y Chevolot ◽  
J Martins ◽  
N Milosevic ◽  
D Léonard ◽  
S Zeng ◽  
...  
Keyword(s):  
Biological Activities ◽  
Modified Surfaces ◽  
Derivatives Of

Identification of promising objects for the synthesis of thiosulphonate derivatives of benzoquinone and hydroquinone

2021 ◽  
Vol 4 (2) ◽  
pp. 47-53
Author(s):  
N. Y. Monka ◽  
◽  
N. E. Stadnytska ◽  
I. R. Buchkevych ◽  
K. O. Kaplia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Experimental Studies ◽  
New Drugs ◽  
Reduced Form ◽  
Free Form ◽  
Wide Range ◽  
On Line ◽  
Living Organisms ◽  
Derivatives Of

Benzoquinone and its reduced form hydroquinone belong to phenolic compounds and are found in living organisms in free form or in glycosides. They are active substances of some medicinal plants and have a pharmacological effect on the human body. Accordingly, their derivatives are important objects for chemical synthesis and development of new drugs. This article presents the findings of the structural design of substances with benzoquinone or hydroquinone fragment and sulfur-containing compound. By use of appropriate on-line programs a predictive screening of the biological activity and cytotoxicity of thiosulfonate derivatives of benzoquinone and hydroquinone has been conducted. It has been found that they have immense methodological potential to be synthesized by substances with a wide range of biological activities and a high value of probable activity, which substantiates the feasibility of conducting experimental studies on their biological activity, particularly anticancer.

Therapeutic Journey of Andrographis paniculata (Burm.f.) Nees from Natural to Synthetic and Nanoformulations

2021 ◽  
Vol 21 ◽  
Author(s):  
Sharuti Mehta ◽  
Anil Kumar Sharma ◽  
Rajesh K. Singh
Keyword(s):  
Biological Activities ◽  
Andrographis Paniculata ◽  
Herbaceous Plant ◽  
Target Tissue ◽  
Active Components ◽  
Essential Information ◽  
Compound Plant ◽  
Therapeutic Activities ◽  
Synthetic Derivatives ◽  
Derivatives Of

: Andrographis paniculata (Burm.f.) Nees (Acanthaceae) is a herbaceous plant and commonly called 'King of Bitters'. It has gained attraction as a potential hepatoprotective agent and a natural molecule with various biological activities viz. anticancer, immunomodulatory, anti-inflammatory, antibacterial, neuroprotective, and so on. The andrographolide is one of the main diterpenoids responsible for the drug's bitter taste and various therapeutic activities. The poor cellular permeability, solubility and short biological half-life of its pure components limit its distribution to the target tissue. To conquer this obstacle, various researchers worldwide have been working on designing the synthetic derivatives of its active components and nanoformulations to improve the drug's efficiency and selectivity to develop more active leads for biomedical applications. This article discussed the recent research on synthetic derivatives, including their possible therapeutic applications and structure-activity relationship (SAR). Additionally, this article also presents the essential information concerning the various nanoformulations developed to increase the delivery of pure compound/plant extract to the target site, thereby improving the drug's efficacy for multiple ailments.

scholarly journals PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

2017 ◽  
Vol 10 (6) ◽  
pp. 237 ◽  
Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar
Keyword(s):  
Acetic Acid ◽  
Cytotoxic Activity ◽  
Glacial Acetic Acid ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

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