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.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

Coumarin Compounds in Medicinal Chemistry: Some Important Examples from the Last Years

2018 ◽  
Vol 18 (2) ◽  
pp. 124-148 ◽  
Author(s):  
Thiago Moreira Pereira ◽  
Daiana Portella Franco ◽  
Felipe Vitorio ◽  
Arthur Eugen Kummerle
Keyword(s):  
Medicinal Chemistry ◽  
Chemical Space ◽  
Noncovalent Interactions ◽  
Biological Activities ◽  
Fluorescent Sensors ◽  
Coumarin Derivatives ◽  
Research Projects ◽  
Wide Range ◽  
Coumarin Compounds ◽  
Treatment And Diagnosis

Coumarins are natural products characterized as 1,2 benzopyrones widely distributed in plants, as well as, in many species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert noncovalent interactions with many enzymes and receptors in live organisms lead the coumarins to exhibit a wide range of biological activities and applications. Then, this manuscript provides an overview of the use of coumarins compounds in medicinal chemistry in treating many diseases. Important examples of the last years have been selected concerning the activities of coumarins as anticoagulant, anticancer, antioxidant, antiviral, anti-diabetics, anti-inflammatory, antibacterial, antifungal and anti-neurodegerative agents. Additionally, it also includes applications of coumarins as fluorescent sensors for biological systems. Thus, this work aims to contribute to the development of new rational research projects for the treatment and diagnosis of pathologies using coumarin derivatives.

scholarly journals Phytochemicals and Biological Activities of Garcinia morella (Gaertn.) Desr.: A Review

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5690
Author(s):  
Hosakatte Niranjana Murthy ◽  
Dayanand Dalawai ◽  
Yaser Hassan Dewir ◽  
Abdullah Ibrahim
Keyword(s):  
Organic Acids ◽  
Bioactive Compounds ◽  
Phenolic Acids ◽  
Biological Activities ◽  
Active Constituents ◽  
Evergreen Tree ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Larvicidal Activities ◽  
Seed Extracts

Garcinia morella (Gaertn.) Desr. is an evergreen tree that yields edible fruits, oil, and resin. It is a source of “gamboge”, a gum/resin that has a wide range of uses. The fruits, leaves, and seeds of this tree are rich in bioactive compounds, including xanthones, flavonoids, phenolic acids, organic acids, and terpenoids. Evidence from different studies has demonstrated the antioxidant, antifungal, antiviral, hepatoprotective, anticancer, anti-inflammatory, antibacterial, and larvicidal activities of the fruit, leaf, and seed extracts of G. morella. This review summarizes the information on the phytochemicals of G. morella and the biological activities of its active constituents.

Coumarin: A Promising Scaffold for Design and Development of Bioactive Agents

2020 ◽  
Vol 16 (6) ◽  
pp. 837-852 ◽  
Author(s):  
Hanan M. Alshibl ◽  
Ebtehal S. Al-Abdullah ◽  
Hamad M. Alkahtani
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
Present Review ◽  
Coumarin Derivatives ◽  
Design And Development ◽  
Strong Potential ◽  
Starting Point ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Bioactive Agents

Background: As coumarin derivatives are known to prevent and treat various diseases, they have attracted the attention of medicinal chemists. They have strong potential as drugs because their benzopyrone structure can interact noncovalently with numerous enzymes and receptors. Methods: The aim of this review was to summarize the most recently published literature on coumarin derivatives in terms of their antioxidant, antimicrobial, anti-inflammatory, anticancer, and other miscellaneous properties. Results: Coumarin derivatives have a wide range of biological activities. They exhibit antioxidant, antimicrobial, anti-inflammatory, anticancer, anti-coagulant, and anti-Alzheimer effects. Conclusion: The coumarin nucleus is an interesting starting point for the design and development of novel bioactive agents. The present review may help medicinal chemists design biologically active molecules based on the coumarin nucleus.

scholarly journals Review Article: Various Biological Activities of Coumarin and Oxadiazole Derivatives.

2017 ◽  
Vol 10 (7) ◽  
pp. 38 ◽  
Author(s):  
Sunny Jalhan
Keyword(s):  
Biological Activities ◽  
Biochemical Properties ◽  
Review Article ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Methylene Groups ◽  
Anti Oxidant ◽  
Oxadiazole Derivatives ◽  
Anti Inflammatory ◽  
Derivatives Of

In this review article data is collected regarding the various derivatives of coumarin and oxadiazole as both these have wide range of biological activities and they can be further modified to synthesize more effective and potent drugs. Coumarin class of organic compounds consists of 1,2-benzopyrone ring system as a basic parent scaffold. These benzopyrones are subdivided into alpha-benzopyrones and gamma benzopyrones; with coumarin class of compounds belonging to alpha-benzopyrones. Since the last few years, coumarins were synthesized in many of their derivative forms. Their pharmacological, therapeutic and biochemical properties depend upon their pattern of substitution. Coumarins exhibit a wide range of pharmacological activities, which includes anti-diabetic, anti-viral, anti-microbial, anticancer, anti-oxidant, anti-parasitic, anti-helminthic, anti-proliferative, anti-convulsant, anti-inflammatory and antihypertensive activities. 1,3,4-Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring. It is derived from furan by substitution of two methylene groups (=CH) with two pyridine type nitrogens (-N=). There are three known isomers: 1,2,4-oxadiazole, 1,2,3-oxadiazole and 1,2,5- oxadiazole. Oxadiazole moiety shows antimicrobial, anticancer and anti-inflammatory activity and suitably substituted 1,3,4-oxadiazole having biological activities like antimicrobial, anticancer and other biological activities.

Piperonal: The Journey so Far

2020 ◽  
Vol 20 (18) ◽  
pp. 1846-1856
Author(s):  
Jain Akash ◽  
Chaudhary Dushyant ◽  
Chaudhary Jasmine
Keyword(s):  
Benzene Ring ◽  
Aromatic Aldehyde ◽  
Search Engines ◽  
Biological Activities ◽  
Structural Features ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
Related Information ◽  
Wide Range ◽  
Made In

Piperonal, an important aromatic aldehyde containing the benzene ring fused to 1, 3- dioxolane moiety, widely occurred in nature and known for its fragrance similar to vanillin and cherry. Alterations in its structural features led to the access of a wide range of piperonal derivatives viz. pyrazolines, chalcones, benzothiazepines, benzoxazoles, triazoles etc. having remarkable pharmacological properties like antimicrobial, anticancer, antidiabetic, antitubercular activities, etc. Therefore, the present study has been designed to highlight the progress made in the area of piperonal and its derivatives till date with respect to their synthesis and pharmacological activities. This may facilitate the synthesis of more novel derivatives with improved biological activities. Various search engines like google, Pubmed, Scopus etc. were used to gather the related information using different keywords.

Chain-breaking/Preventive Antioxidant, Urate-lowering, and Anti-inflammatory Effects of Pure Curcumin

2020 ◽  
Vol 17 (1) ◽  
pp. 66-74
Author(s):  
Seghira Bisset ◽  
Widad Sobhi ◽  
Chawki Bensouici ◽  
Abdelhalim Khenchouche
Keyword(s):  
Uric Acid ◽  
Xanthine Oxidase ◽  
Acid Production ◽  
Biological Activities ◽  
Antioxidant Effect ◽  
Metal Chelating ◽  
Wide Range ◽  
Chain Breaking ◽  
Pharmaceutical Industries ◽  
Anti Inflammatory

Background: Several researches have shown that therapeutic compounds or phytochemicals from natural sources are important in the food as it is valuable in pharmaceutical industries due to their fewer side effects and potent against various diseases. Curcumin, a major polyphenol derived from turmeric spice, which used in many foods, has a wide range of biological activities, with quite a safety. Objective: The goal of this study was to investigate the antioxidant, urate-lowering, and antiinflammatory effects of pure curcumin. Methods: The antioxidant activity was evaluated for chain-breaking antioxidant effect (radicalscavenging and reducing abilities assays) and for preventive antioxidant effect with metal chelating assay, the urate-lowering was assayed on aspectrophotometer by measuring the inhibition of uric acid production by xanthine oxidase (XO) enzyme, and the anti-inflammatory effect was estimated using in vitro albumin denaturation inhibition. Results: Curcumin showed a significant and good chain-breaking antioxidant effect, both in free radical- scavenging assays (Galvinoxyl radical, ABTS, and hydroxyl radical), and in reducing abilities methods (reducing power, Cupric ion reducing antioxidant capacity and O-phenanthroline assays). In preventive antioxidant effect, assessed with the metal chelating assay, curcumin showed significant effect but with high concentration compared with standard. In the xanthine/xanthine oxidase system, curcumin significantly inhibited uric acid production (IC50=0.71 ± 0.06 mg/mL). Regarding antiinflammatory activity, curcumin showed significant inhibition of albumin denaturation with an IC50 value of 1181.69 ± 1.11μg/mL. Conclusion: These results indicated that curcumin showed promising antioxidant, anti-gout and antiinflammatory properties and might be used as potential, natural drugs against oxidative and inflammation- related diseases.

scholarly journals Identifying bioactive phytochemicals in spent coffee grounds for cosmetic application through global metabolite analysis

2017 ◽  
Author(s):  
◽  
Jihyun Park
Keyword(s):  
Bioactive Compounds ◽  
Raw Materials ◽  
Costa Rican ◽  
Raw Material ◽  
Spent Coffee Grounds ◽  
Metabolite Analysis ◽  
Coffee Grounds ◽  
Chemical Profiles ◽  
Anti Oxidant ◽  
Anti Inflammatory

Annually, more than 6 million tons of spent coffee grounds (SCG) are generated worldwide. The present study explores the possible use of spent coffee grounds as the raw materials for cosmetics industry. The main objective of this project are to investigate the chemical profiles and identify the bioactive compounds for cosmetics application through global metabolite analysis. The compounds extracted from SCG of Ethiopia coffee (Yirgacheffe), Costa Rican coffee (Tarrazu) and Hawaiian coffee (Kona) were analyzed by ultra-high pressure liquid chromatography coupled with mass spectrometry (UPLC-MS). The ion chromatograms were submitted to XCMS platform operated by Center for Metabolomics at the Scripps Research Institute. The peak detection, peak grouping, spectra extraction, and retention alignment were processed by XCMS. The spectra were annotated and the compounds were identified and categorized by integration with METLIN, the world's largest metabolite database. Multivariate and univariate statistical analysis including PCA and cloud-plot were performed by XCMS to compare the chemical profiles between the three coffee cultivars. These analyses indicated that each cultivar showed a specific cluster. Over 200 compounds related to anti-oxidant, anti-inflammatory, anti-tyrosinase and anti-tumor for skin care application were identified by XCMS. Therefore, the presence of bioactive compounds in SCG makes it a potential source of raw material for cosmetic application (e.g., anti-oxidant, anti-inflammatory, skin-whiting, and anti-aging).

scholarly journals A IMPORTÂNCIA DAS CUMARINAS PARA A QUÍMICA MEDICINAL E O DESENVOLVIMENTO DE COMPOSTOS BIOATIVOS NOS ÚLTIMOS ANOS

Química Nova ◽  
2020 ◽  
Author(s):  
Daiana Franco ◽  
Thiago Pereira ◽  
Felipe Vitorio ◽  
Nathalia Nadur ◽  
Renata Lacerda ◽  
...  
Keyword(s):  
Chemical Space ◽  
Biological Activities ◽  
Research Projects ◽  
Wide Range ◽  
Non Covalent Interactions ◽  
Iupac Nomenclature ◽  
Living Organisms ◽  
Coumarin Compounds ◽  
New Treatments ◽  
Covalent Interactions

Coumarins are natural products characterized as 2H-chromen-2-one, according to IUPAC nomenclature, largely distributed in plants, as well as, in species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert non-covalent interactions with many enzymes an receptors in living organisms lead the coumarins to exhibit a wide range of biological activities and applications. Then, this manuscript provides an overview of the use of coumarin compounds in medicinal chemistry in treating many diseases. Important examples of the last years have been selected concerning the activities of coumarins as anticoagulant, anticancer, antioxidant, antiviral, antidiabetics, anti-inflammatory, antibacterial, antifungal, and anti-neurodegenerative agents. Thus, this work aims at contributing to the development of new rational research projects searching for new treatments and bioactive compounds for many pathologies using coumarin derivatives.

scholarly journals Enhanced Recovery of Antioxidant Compounds from Hazelnut (Corylus avellana L.) Involucre Based on Extraction Optimization: Phytochemical Profile and Biological Activities

Antioxidants ◽  
2019 ◽  
Vol 8 (10) ◽  
pp. 460 ◽  
Author(s):  
Rusu ◽  
Fizeșan ◽  
Pop ◽  
Gheldiu ◽  
Mocan ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Enhanced Recovery ◽  
Biological Activities ◽  
Natural Antioxidants ◽  
Antioxidant Compounds ◽  
Cancerous Cell ◽  
Wide Range ◽  
Quantitative Analyses ◽  
Corylus Avellana L

Tree nut by-products could contain a wide range of phytochemicals, natural antioxidants, which might be used as a natural source for dietary supplements. The aim of the present study was to evaluate the phenolic and sterolic composition, as well as the antioxidant and other biological activities, of hazelnut involucre (HI) extracts. Experimental designs were developed in order to select the optimum extraction conditions (solvent, temperature, time) using turbo-extraction by Ultra-Turrax for obtaining extracts rich in bioactive compounds. Qualitative and quantitative analyses were performed by LC-MS and LC-MS/MS and they revealed important amounts of individual polyphenols and phytosterols, molecules with antioxidant potential. The richest polyphenolic HI extract with the highest antioxidant activity by TEAC assay was further evaluated by other in vitro antioxidant tests (DPPH, FRAP) and enzyme inhibitory assays. Additionally, the cytotoxic and antioxidant effects of this extract on two cancerous cell lines and on normal cells were tested. This is the first study to analyze the composition of both hydrophilic and lipophilic bioactive compounds in HI extracts. Our findings reveal that this plant by-product presents strong biological activities, justifying further research, and it could be considered an inexpensive source of natural antioxidants for food, pharmaceutical, or cosmetic industry.

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