scholarly journals A Comprehensive Review of Aminochalcones

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5381
Author(s):  
Rimsha Irfan ◽  
Shikufa Mousavi ◽  
Meshari Alazmi ◽  
Rahman Shah Zaib Saleem
Keyword(s):  
Cancer Cells ◽  
Biological Activities ◽  
Aromatic Rings ◽  
Amino Groups ◽  
High Potency ◽  
Comprehensive Review ◽  
Current Review ◽  
One Stop ◽  
Anti Inflammatory

Chalcones, members of the flavonoid family, display a plethora of interesting biological activities including but not limited to antioxidant, anticancer, antimicrobial, anti-inflammatory, and antiprotozoal activities. The literature cites the synthesis and activity of a range of natural, semisynthetic, and synthetic chalcones. The current review comprehensively covers the literature on amino-substituted chalcones and includes chalcones with amino-groups at various positions on the aromatic rings as well as those with amino-groups containing mono alkylation, dialkylation, alkenylation, acylation, and sulfonylation. The aminochalcones are categorized according to their structure, and the corresponding biological activities are discussed as well. Some compounds showed high potency against cancer cells, microbes, and malaria, whereas others did not. The purpose of this review is to serve as a one-stop location for information on the aminochalcones reported in the literature in recent years.

scholarly journals Competitive Biological Activities of Chitosan and Its Derivatives: Antimicrobial, Antioxidant, Anticancer, and Anti-Inflammatory Activities

2018 ◽  
Vol 2018 ◽  
pp. 1-13 ◽  
Author(s):  
Suyeon Kim
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
Biological Properties ◽  
Biomedical Science ◽  
Amino Groups ◽  
Chitosan Oligosaccharides ◽  
Primary Amino ◽  
Anti Inflammatory ◽  
Key Functional Groups ◽  
Application Fields

Chitosan is obtained from alkaline deacetylation of chitin, and acetamide groups are transformed into primary amino groups during the deacetylation. The diverse biological activities of chitosan and its derivatives are extensively studied that allows to widening the application fields in various sectors especially in biomedical science. The biological properties of chitosan are strongly depending on the solubility in water and other solvents. Deacetylation degree (DDA) and molecular weight (MW) are the most decisive parameters on the bioactivities since the primary amino groups are the key functional groups of chitosan where permits to interact with other molecules. Higher DDA and lower MW of chitosan and chitosan derivatives demonstrated higher antimicrobial, antioxidant, and anticancer capacities. Therefore, the chitosan oligosaccharides (COS) with a low polymerization degree are receiving a great attention in medical and pharmaceutical applications as they have higher water solubility and lower viscosity than chitosan. In this review articles, the antimicrobial, antioxidant, anticancer, anti-inflammatory activities of chitosan and its derivatives are highlighted. The influences of physicochemical parameters of chitosan like DDA and MW on bioactivities are also described.

scholarly journals Phyllanthin: A Potential Lead Molecule for the Future Needs

2017 ◽  
Vol 9 (08) ◽  
Author(s):  
Mohammed Azam ◽  
Makula Ajitha
Keyword(s):  
Physicochemical Properties ◽  
Biological Activities ◽  
Mechanisms Of Action ◽  
Comprehensive Review ◽  
Toxicity Studies ◽  
Future Needs ◽  
The Future ◽  
Anti Inflammatory

Phyllanthin is an active lignan present in various Phyllanthus species and number of studies revealed that it exhibits various biological activities that include antioxidant, hepatoprotective, anticancer, antidiabetic, immunosuppressant and anti-inflammatory activities. After thorough examination of existing literature it was discovered that there is currently no comprehensive review available on this significant phytocompound. Hence, an attempt was made to present the physicochemical properties, enhancement techniques of yield and bioavailability, synthesis, pharmacological applications and toxicity studies of phyllanthin. This report also highlights semisynthetic derivatives and mechanisms of action of phyllanthin for various biological activities.

Chalcones as Scavengers of HOCl and Inhibitors of Oxidative Burst: Structure-Activity Relationship Studies

2020 ◽  
Vol 17 ◽  
Author(s):  
Thaise Martins ◽  
Vera L.M. Silva ◽  
Artur M.S. Silva ◽  
José L.F.C. Lima ◽  
Eduarda Fernandes ◽  
...  
Keyword(s):  
Oxidative Burst ◽  
Hypochlorous Acid ◽  
Biological Activities ◽  
Chemical Diversity ◽  
Human Neutrophils ◽  
Aromatic Rings ◽  
Structure Activity ◽  
Antioxidant Agents ◽  
Ic50 Values ◽  
Anti Inflammatory

Aims: Evaluate the ability of chalcones to scavenge hypochlorous acid (HOCl) and modulate oxidative burst. Background: The chemistry of chalcones has long been a matter of interest to the scientific community due to the phenolic groups often present and to the various replaceable hydrogens that allow the formation of a broad number of derivatives. Due to this chemical diversity, several biological activities have been attributed to chalcones, namely anti-diabetic, anti-inflammatory and antioxidant. Objectives: Evaluate the ability of a panel of 34 structurally related chalcones to scavenge HOCl and/or suppress its produc-tion through the inhibition of human neutrophils’ oxidative burst, followed by the establishment of the respective structure-activity relationships. Methods: The ability of chalcones to scavenge HOCl was evaluated by fluorimetric detection of the inhibition of dihydro-rhodamine 123 oxidation. The ability of chalcones to inhibit neutrophils’ oxidative burst was evaluated by chemiluminomet-ric detection of the inhibition of luminol oxidation. Results: It was observed that the ability to scavenge HOCl depends on the position and number of hydroxy groups on both aromatic rings. Chalcone 5b was the most active with an IC50 value of 1.0 ± 0.1 μM. The ability to inhibit neutrophils’ oxi-dative burst depends on the presence of a 2’-hydroxy group on A-ring and on other substituents groups, e.g. methoxy, hy-droxy, nitro and/or chlorine atom(s) at C-2, C-3 and/or C-4 on B-ring, as in chalcones 2d, 2f, 2j, 2i, 4b, 2n and 1d, which were the most actives with IC50 values ranging from 0.61 ± 0.02 μM to 1.7 ± 0.2 μM. Conclusion: The studied chalcones showed high activity at a low micromolar range, indicating their potential as antioxidant agents and to be used as a molecular structural scaffold for the design of new anti-inflammatory compounds.

scholarly journals A Review on Synthesis and Biological Activity of Thiazole and its Derivatives

2021 ◽  
Vol 70 (1) ◽  
Author(s):  
Namitha TH ◽  
Saranya S Nair ◽  
Dr.Arun Kumar ◽  
Dr.Vinod B ◽  
Dr.Daisy P A
Keyword(s):  
Biological Activity ◽  
Pharmacological Activity ◽  
Biological Activities ◽  
Synthetic Compounds ◽  
The Past ◽  
Current Review ◽  
Heteroaromatic Ring ◽  
Wide Range ◽  
Anti Inflammatory

Thiazole, a five-membered heteroaromatic ring, is an important framework of a large number of synthetic compounds. Its diverse pharmacological activity is mirrored in many clinically approved thiazole-containing molecules with, wide range of biological activities, such as antibacterial, antifungal, antiviral, anthelmintic, antitumor, and anti-inflammatory effects. The current review provides an overview of the biological activities of thiazole during the past years.

scholarly journals Ethnobotanical uses, phytochemistry and biological activities of Clerodendrum paniculatum L. (Lamiaceae): A comprehensive review

2018 ◽  
Vol 8 (5-s) ◽  
pp. 28-34
Author(s):  
T.R. Prashith Kekuda ◽  
S.J. Sudharshan
Keyword(s):  
Biological Activities ◽  
Pharmacological Properties ◽  
Comprehensive Review ◽  
The Family ◽  
Anti Inflammatory ◽  
Ethnobotanical Uses

Clerodendrum L. is an important genus in the family Lamiaceae in terms of its medicinal values and pharmacological properties. The genus comprises of more than 500 species distributed worldwide. In this review, we present an updated information on ethnobotanical uses, phytochemistry and biological activities of Clerodendrum paniculatum L. (Lamiaceae). The plant is one the most spectacular Clerodendrum species and is grown commonly for ornamental purpose. The plant is reported to have ethnomedicinal importance as the plant is used as remedy for ailments and disorders such as wounds, typhoid, snakebite, jaundice, giddiness, malaria, anemia and hemorrhoids. Various phytochemicals such as rutin, quercetin, β-sitosterol, β-amyrin, lupeol, oleanolic aldehyde acetate, stigmasta-4,25-dien-3-one, and (3β)-stigmasta-4,22,25-trien-3-ol have been identified in C. paniculatum. The plant is shown to exhibit biological activities such as antimicrobial, antioxidant, anthelmintic, anti-inflammatory, antimutagenic, cytotoxic, hypolipidemic, insecticidal and anti-ageing activity. Keywords: Clerodendrum paniculatum L., Ethnobotanical, Traditional, Phytochemicals, Biological activities

scholarly journals Inhibition of TLR4/TRIF/IRF3 Signaling Pathway by Curcumin in Breast Cancer Cells

2019 ◽  
Vol 22 ◽  
pp. 281-291 ◽  
Author(s):  
Gamze Güney Eskiler ◽  
Asuman Deveci Özkan ◽  
Süleyman Kaleli ◽  
Cemil Bilir
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Signaling Pathway ◽  
Breast Cancer Cells ◽  
Biological Activities ◽  
Breast Cancer Cell Lines ◽  
Type I ◽  
Curcumin Treatment ◽  
Anti Inflammatory ◽  
Mcf 7

Purpose: Toll-like receptor 4 (TLR4) is over-expressed in breast tumors and thus contributing to the tumor progression and metastasis. Natural products have drawn attention in cancer immunotherapy due to their various biological activities. Curcumin is well investigated in different types of cancer. However, the mechanisms underlying its anti-inflammatory actions have not been extensively elucidated.  For this purpose, we explored the inhibitory effects of curcumin on lipopolysaccharide (LPS)-induced TLR4 dependent TRIF signaling pathway in two subtypes of breast cancer cell lines (MCF-7 and MDA-MB-231) in this study. Methods: In this context, the cytotoxicity of curcumin and LPS alone and the combination of curcumin with LPS on these cells was evaluated by WST-1 assay.  The expression level of TLR4 and the release of type I interferon (IFN) levels were determined after treatment with curcumin and/or LPS by RT-PCR and ELISA analysis, respectively. Furthermore, the subcellular localization of TLR4 and interferon regulatory factor 3 (IRF3) were detected by immunofluorescence analysis. Results: Curcumin treatment suppressed breast cancer cells viabilities and the activation of TLR4-mediated TRIF signaling pathway by the downregulation of TLR4 and IRF3 expression levels and the inhibition of type I IFN (IFN-α/β) levels induced by LPS. However, curcumin was more efficient in MDA-MB-231 cells than MCF-7 cells owing to its greater inhibitory efficacy in the LPS- enhanced TLR4 signaling pathway. Furthermore, IFN-α/β levels induced by TLR4 and IRF3 were decreased in these cells following curcumin treatment. Conclusions: Consequently, these results demonstrated that the activation of LPS stimulated TLR4/TRIF/IRF3 signaling pathway was mediated by curcumin in breast cancer cells, in vitro. However, more studies are necessary to examine the curcumin’s anti-inflammatory activities on TLR4/MyD88/NF-κB as well as other signaling pathways downstream of TLRs in breast cancer.

scholarly journals Synthetic Routes to Coumarin(Benzopyrone)-Fused Five-Membered Aromatic Heterocycles Built on the α-Pyrone Moiety. Part II: Five-Membered Aromatic Rings with Multi Heteroatoms

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3409
Author(s):  
Eslam Reda El-Sawy ◽  
Ahmed Bakr Abdelwahab ◽  
Gilbert Kirsch
Keyword(s):  
Biological Activities ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Aromatic Rings ◽  
Active Compounds ◽  
Pyrone Ring ◽  
Aromatic Heterocycles ◽  
Current Review ◽  
Synthetic Routes

Coumarins are natural heterocycles that widely contribute to the design of various biologically active compounds. Fusing different aromatic heterocycles with coumarin at its 3,4-position is one of the interesting approaches to generating novel molecules with various biological activities. During our continuing interest in assembling information about fused five-membered aromatic heterocycles, and after having presented mono-hetero-atomic five-membered aromatic heterocycles in Part I. The current review Part II is intended to present an overview of the different synthetic routes to coumarin (benzopyrone)-fused five-membered aromatic heterocycles with multi-heteroatoms built on the pyrone ring, covering the literature from 1945 to 2021.

758: Inflammatory and Anti-Inflammatory Regulators alter Levels of an Inhibitor of Apoptosis (IAP), Survivin, in T-24 Bladder Cancer Cells

2007 ◽  
Vol 177 (4S) ◽  
pp. 254-254
Author(s):  
Justin J. Cohen ◽  
Bayan T. Takizawa ◽  
Hristos Z. Kaimkliotis ◽  
David J. Rosenberg ◽  
Marcia A. Wheeler ◽  
...  
Keyword(s):  
Bladder Cancer ◽  
Cancer Cells ◽  
Inhibitor Of Apoptosis ◽  
Bladder Cancer Cells ◽  
Anti Inflammatory

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Industrial Chemical ◽  
Anti Inflammatory ◽  
Pyridazinone Derivatives

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

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