scholarly journals Germacrone: Occurrence, Synthesis, Chemical Transformations and Biological Properties

2008 ◽  
Vol 3 (4) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
Alejandro F. Barrero ◽  
M. Mar Herrador ◽  
Pilar Arteaga ◽  
Julieta V. Catalán
Keyword(s):  
Essential Oils ◽  
Chemical Reactivity ◽  
Biological Activities ◽  
Biological Properties ◽  
Chemical Transformations ◽  
Cyclization Reactions ◽  
Cns Depressant ◽  
Complete Synthesis ◽  
Wide Range ◽  
Total Oil

Germacrone (1) forms part of a great number of essential oils, in some of them comprising more than 20% of the total oil. This compound presents a wide range of biological activities (CNS depressant, antiinflammatory, antiulcer, antifeedant, antibacterial, antifungal, antitumor, antitussive, vasodilator, choleretic, hepatoprotector), which are analyzed. The chemical reactivity of germacrone, including cyclization reactions, and complete synthesis are presented.

Chemistry and Pharmacological Activities of Biginelli Product- A Brief Overview

2019 ◽  
Vol 16 (2) ◽  
pp. 127-134 ◽  
Author(s):  
Namy George ◽  
Asha Asokan Manakkadan ◽  
Ajish Ariyath ◽  
Surya Maniyamma ◽  
Vishnu Vijayakumar ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Biological Activities ◽  
Biginelli Reaction ◽  
Structural Similarity ◽  
Biological Properties ◽  
Synthetic Methods ◽  
Molecular Formula ◽  
Chemical Transformations ◽  
Dna And Rna ◽  
Wide Range

Dihydropyrimidinones are extremely advantageous small sized molecules owning adaptable pharmaceutical properties. With a molecular formula C4H6N2O, they hold a wide range of biological activities. It is a heterocyclic moiety having two N-atoms at positions 1 and 3. They are derivatives of pyrimidine containing an additional ketone group. They have inspired development of a wide range of synthetic methods for preparation and chemical transformations. Taking into consideration their structural similarity and involvement with DNA and RNA, they have become very imperative in the world of synthetic organic chemistry. Aryl substituted moieties and their derivatives are significant class of substances in medicinal and organic chemistry. Many alkaloids from natural marine sources comprising dihydropyrimidinones core have been isolated which possess fascinating biological properties. Intensive explorations have been carried out on these compounds because they possess close similitude to clinically used nifedipine, nicardipine etc. which are also Biginelli product analogues. Due to the interesting pharmacological properties associated with the privileged DHPM structures, the Biginelli reaction and related procedures have received increasing attention in recent years.

A Review on Synthesis and Pharmacological Activity of Coumarins and Their Analogs

2020 ◽  
Vol 16 (6) ◽  
pp. 818-836 ◽  
Author(s):  
Moustafa A. Gouda ◽  
Mohammed A. Salem ◽  
Mohamed H. Helal
Keyword(s):  
Knoevenagel Condensation ◽  
Chemical Reactivity ◽  
Biological Activities ◽  
Vitamin K Antagonists ◽  
Biological Properties ◽  
Synthetic Approach ◽  
Wide Range ◽  
Perkin Reaction ◽  
Coumarin Ring ◽  
Substituted Coumarins

Background: Coumarins were reported to possess antimicrobial, antiinflammatory, antiplasmodial, antimalarial, and enzyme inhibitory properties. Furthermore, coumarins are a type of vitamin K antagonists. Coumarins had been first organized through perkin reaction; besides Knoevenagel condensation was mentioned as a critical synthetic approach for the synthesis of 3-substituted coumarins. Moreover, Pechmann, Reformatasky and Witting reactions were stated for the preparation of coumarins. Methods: We undertook a structured search of the method of preparation, the chemical reactivity and biological properties that are associated with coumarins and their analogous. Results: Coumarins display a wide range of Src Kinase and cholinesterase inhibitor activities and application of coumarins as antidiabetic, antipsychotic and antiproliferative agents has been addressed. Other properties of coumarins such as their role in antitumor, anticancer, and as antioxidants have also been reviewed. Conclusion: This review concluded that coumarin ring was mixed with other rings, a synergistic effect for each of the ring in their biological activities was obtained, such compounds were exploited to improve various important molecules which provide scaffolds for drug improvement. These compounds were used to broaden a special molecule that gives scaffolds for drug improvement.

scholarly journals Rose Flowers—A Delicate Perfume or a Natural Healer?

Biomolecules ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 127
Author(s):  
Milka Mileva ◽  
Yana Ilieva ◽  
Gabriele Jovtchev ◽  
Svetla Gateva ◽  
Maya Margaritova Zaharieva ◽  
...  
Keyword(s):  
Essential Oils ◽  
Food Industry ◽  
Raw Materials ◽  
Biological Activities ◽  
Biological Properties ◽  
Rosa Damascena ◽  
Oil Sand ◽  
Rosa Gallica ◽  
Therapeutic Properties ◽  
Phytochemical Profile

Plants from the Rosacea family are rich in natural molecules with beneficial biological properties, and they are widely appreciated and used in the food industry, perfumery, and cosmetics. In this review, we are considering Rosa damascena Mill., Rosa alba L., Rosa centifolia L., and Rosa gallica L. as raw materials important for producing commercial products, analyzing and comparing the main biological activities of their essential oils, hydrolates, and extracts. A literature search was performed to find materials describing (i) botanical characteristics; (ii) the phytochemical profile; and (iii) biological properties of the essential oil sand extracts of these so called “old roses” that are cultivated in Bulgaria, Turkey, India, and the Middle East. The information used is from databases PubMed, Science Direct, and Google Scholar. Roses have beneficial healing properties due to their richness of beneficial components, the secondary metabolites as flavonoids (e.g., flavones, flavonols, anthocyanins), fragrant components (essential oils, e.g., monoterpenes, sesquiterpenes), and hydrolysable and condensed tannins. Rose essential oils and extracts with their therapeutic properties—as respiratory antiseptics, anti-inflammatories, mucolytics, expectorants, decongestants, and antioxidants—are able to act as symptomatic prophylactics and drugs, and in this way alleviate dramatic sufferings during severe diseases.

scholarly journals Monoterpenes and Sesquiterpenes of Essential Oils from Psidium Species and Their Biological Properties

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 965
Author(s):  
Renan Campos e Silva ◽  
Jamile S. da Costa ◽  
Raphael O. de Figueiredo ◽  
William N. Setzer ◽  
Joyce Kelly R. da Silva ◽  
...  
Keyword(s):  
Essential Oils ◽  
Biological Activities ◽  
Biological Properties ◽  
Chemical Diversity ◽  
New Drugs ◽  
Natural Sources ◽  
Biological Potential ◽  
The World ◽  
Review Reports ◽  
Collection Sites

Psidium (Myrtaceae) comprises approximately 266 species, distributed in tropical and subtropical regions of the world. Psidium taxa have great ecological, economic, and medicinal relevance due to their essential oils’ chemical diversity and biological potential. This review reports 18 Psidium species growing around the world and the chemical and biological properties of their essential oils. Chemically, 110 oil records are reported with significant variability of volatile constituents, according to their seasonality and collection sites. Monoterpenes and sesquiterpenes with acyclic (C10 and C15), p-menthane, pinane, bisabolane, germacrane, caryophyllane, cadinane, and aromadendrane skeleton-types, were the primary constituents. The essential oils showed various biological activities, including antioxidant, antifungal, antibacterial, phytotoxic, larvicidal, anti-inflammatory, and cytotoxic properties. This review contributes to the Psidium species rational and economic exploration as natural sources to produce new drugs.

Steroidal pyrazolines as a promising scaffold in drug discovery

2020 ◽  
Vol 12 (10) ◽  
pp. 949-959
Author(s):  
Ranju Bansal ◽  
Ranjit Singh
Keyword(s):  
Drug Discovery ◽  
Broad Spectrum ◽  
Chemical Reactivity ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Review Article ◽  
Pharmacological Activities ◽  
Neuroprotective Effects ◽  
Wide Range

Steroidal pyrazolines constitute an interesting and promising scaffold for drug discovery as they display diverse chemical reactivity and a wide range of biological activities. Literature reports indicate potent anticancer potential of steroidal pyrazolines along with broad-spectrum antimicrobial activities. Strong neuroprotective effects with steroids possessing pyrazoline moiety have also been observed. Among all the therapeutically active steroidal pyrazolines, D-ring-substituted derivatives are highly potent and the least toxic. The current and futuristic research approaches in this area are focused towards the exploration of this promising scaffold to develop molecules with widespread pharmacological activities. This review article mainly covers the synthetic and pharmacological aspects of steroidal pyrazolines, which will assist the medicinal chemists working in this area in their scientific endeavors.

scholarly journals Chemical Composition and Biological Activities of Essential Oils of Pinus patula

2011 ◽  
Vol 6 (10) ◽  
pp. 1934578X1100601 ◽  
Author(s):  
Ismail Amri ◽  
Hamrouni Lamia ◽  
Samia Gargouri ◽  
Mohsen Hanana ◽  
Mariem Mahfoudhi ◽  
...  
Keyword(s):  
Gas Chromatography ◽  
Essential Oils ◽  
Biological Activities ◽  
Pathogenic Fungi ◽  
Plant Diseases ◽  
Gas Chromatography Mass Spectrometry ◽  
Pinus Patula ◽  
Flame Ionization ◽  
Total Oil

Essential oils isolated from needles of Pinus patula by hydrodistillation were analyzed by gas chromatography-flame ionization detection (GC-FID) and gas chromatography mass spectrometry (GC-MS). Thirty-eight compounds were identified, representing 98.3% of the total oil. The oil was rich in monoterpene hydrocarbons (62.4%), particularly α-pinene (35.2%) and β-phellandrene (19.5%). The in vitro antifungal assay showed that P. patula oil significantly inhibited the growth of 9 plant pathogenic fungi. The oil, when tested on Sinapis arvensis, Lolium rigidum, Phalaris canariensis and Trifolium campestre, completely inhibited seed germination and seedling growth of all species. Our preliminary results showed that P. patula essential oil could be valorized for the control of weeds and fungal plant diseases.

scholarly journals Exploitation of Cytotoxicity of Some Essential Oils for Translation in Cancer Therapy

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Rossella Russo ◽  
Maria Tiziana Corasaniti ◽  
Giacinto Bagetta ◽  
Luigi Antonio Morrone
Keyword(s):  
Multidrug Resistance ◽  
Essential Oils ◽  
Biological Activities ◽  
Complex Mixtures ◽  
Antitumor Drugs ◽  
Wide Range ◽  
Growing Body ◽  
Anticancer Treatment

Essential oils are complex mixtures of several components endowed with a wide range of biological activities, including antiseptic, anti-inflammatory, spasmolytic, sedative, analgesic, and anesthetic properties. A growing body of scientific reports has recently focused on the potential of essential oils as anticancer treatment in the attempt to overcome the development of multidrug resistance and important side effects associated with the antitumor drugs currently used. In this review we discuss the literature on the effects of essential oils in  in vitroandin vivomodels of cancer, focusing on the studies performed with the whole phytocomplex rather than single constituents.

scholarly journals Essential oil from Piperaceae as a potential for biopesticide agents: a review

Food Research ◽  
2020 ◽  
Vol 4 (S5) ◽  
pp. 1-10
Author(s):  
N.A. Abdullah ◽  
W.Z.W.M. Zain ◽  
H.A. Hamid ◽  
N.W. Ramli
Keyword(s):  
Secondary Metabolites ◽  
Essential Oils ◽  
Biological Activities ◽  
The United States ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Present Information ◽  
United States Food ◽  
Synthetic Pesticide ◽  
States Food

This review is aimed to present information on the properties of Piperaceae which can be potentially used as a biopesticide. The chemical compounds involved in were different as each species consist of different amount of secondary metabolites which then leads to different properties. In recent years, several reports have been published regarding the composition and the biological activities of the essential oils of Piper species. These studies have highlighted the existence of marked chemical differences among oils extracted from different species or varieties. Analysis of volatile constituents from Piperaceae species has revealed the presence of monoterpenes, sesquiterpenes and arylpropanoids that have shown interesting biological properties including cytotoxic, fungistatic, insecticide, molluscicidal, antioxidant and antimicrobial activities. Essential oils are natural complex secondary metabolites characterized by strong odour, volatility and have generally lower density than water. Due to their volatility, essential oils are environmentally non-persistent. On top of that, essential oils are ‘generally recognized as safe’ by the United States Food and Drug Administration (FDA). Since technology has become more advanced, people started to replace synthetic pesticide with bio-pesticide. The demand for EO has increased as it has biological properties that can be used to replace synthetic pesticide

scholarly journals SYNTHESIS, CHARACTERIZATION, ANTIFUNGAL ACTIVITY AND STRUCTURE– ACTIVITY RELATIONSHIPS: STUDY OF SOME MONO- AND DI-SCHIFF BASES

2020 ◽  
Vol 17 (34) ◽  
pp. 528-540
Author(s):  
Ekhlas Q JASIM ◽  
Hawraa K DHAIF ◽  
Munther A MUHAMMAD-ALI
Keyword(s):  
Antifungal Activity ◽  
Schiff Bases ◽  
Density Functional ◽  
Chemical Reactivity ◽  
Biological Activities ◽  
Analytical Techniques ◽  
Carbonyl Oxygen ◽  
Proton Nuclear Magnetic Resonance ◽  
Mulliken Charge ◽  
Wide Range

Schiff bases (SB) are an important type of organic compounds and have a wide range of biological activities due to commercial and pharmaceutical trading uses. The different activities of these compounds induced the researchers to synthesized and studied new types of these compounds. Two series of Schiff base derivatives were synthesized by the condensation reactions of substituted aldehydes salicylaldehyde, 4-(N,Ndimethylamino) benzaldehyde or 2,4-dimethoxybenzaldehyde with 2-amino-5-iodobenzoic acid (1:1) or with 3,5- diamenobenzoic acid (1:2) in ethanol absolute as a solvent. Different analytical techniques characterized the structure of the synthesized Schiff bases; for instance, Fourier transform infrared FT-IR and proton nuclear magnetic resonance 1H-NMR. The purity of the synthesized compounds was tested by elemental microanalysis CHN and thin layer chromatography TLC. The structural properties of the studied molecules were investigated theoretically by performing density functional theory (DFT) using the HyperChem software. The lipophilicity of the tested compounds showed that the compounds 2c, 2b, 2a, and 1c have logP values less than (5), 2.90, 3.78, 3.82 and 4.57, respectively, whereas, 1b and 1a have logP values higher than (5), 5.01 and 5.03, respectively. The Mulliken charge distribution showed that the carbonyl oxygen atom of the carboxylic group is more negative (~ - 0.4) as compared to other oxygen atoms (~ -0.3) in all selected compounds. Frontier molecular orbitals energy diagram and their bandgap provided indications about chemical reactivity and kinetic stability of the molecules. The synthesized compounds were tested for antifungal effects against Aspergillus niger and Candida albicans, which indicated that the compounds had good antifungal activity.

scholarly journals Characterization of Andean Blueberry in Bioactive Compounds, Evaluation of Biological Properties and in vitro Bioaccessibility

2020 ◽  
Author(s):  
Nieves Baenas ◽  
Jenny Ruales ◽  
Diego A. Moreno ◽  
Daniel Alejandro Barrio ◽  
Carla M. Stinco ◽  
...  
Keyword(s):  
Antioxidant Capacity ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
In Vitro Digestion ◽  
Biological Properties ◽  
Wide Range ◽  
Zebrafish Embryogenesis

Andean blueberries are wild berries grown and consumed in Ecuador which contain high values of bioactive compounds, mainly anthocyanins, with powerful antioxidant activity. The aim of this study was to evaluate the profile and contents of (poly)phenols and carotenoids in Andean blueberry by HPLC-DAD-MSn and determine a wide range of its biological activities. The antioxidant capacity of this fruit was evaluated in vitro by three different methods and in vivo using the zebrafish animal model, also the toxicity effect was determined by the zebrafish embryogenesis test. Besides, the antimicrobial activity and the capacity of Andean blueberry to produce hemagglutination in blood cells were evaluated. Finally, the bioaccessibility of (poly)phenols and related antioxidant capacity were determined in the different phases of an in vitro digestion. The global results indicated no toxicity of Andean blueberry, weakly bacteriostatic activity, and high contents of anthocyanins and antioxidant capacity, which were partially bioaccesible in vitro (~ 50 % at the final intestinal step), contributing to the knowledge of its health benefits for consumers and its potential use in the food and pharmaceutical industry as functional ingredient.

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