scholarly journals GenusCaulophyllum: An Overview of Chemistry and Bioactivity

2014 ◽  
Vol 2014 ◽  
pp. 1-18 ◽  
Author(s):  
Yong-Gang Xia ◽  
Guo-Yu Li ◽  
Jun Liang ◽  
Bing-You Yang ◽  
Shao-Wa Lü ◽  
...  
Keyword(s):  
Systematic Review ◽  
Cell Membrane ◽  
Mechanisms Of Action ◽  
New Drugs ◽  
Pharmacological Properties ◽  
Cell Membrane Chromatography ◽  
Action Mechanisms ◽  
Naturally Occurring ◽  
Activity Screening ◽  
Point Of Reference

Recently, some promising advances have been achieved in understanding the chemistry, pharmacology, and action mechanisms of constituents from genusCaulophyllum. Despite this, there is to date no systematic review of those of genusCaulophyllum. This review covers naturally occurring alkaloids and saponins and those resulting from synthetic novel taspine derivatives. The paper further discussed several aspects of this genus, including pharmacological properties, mechanisms of action, pharmacokinetics, and cell membrane chromatography for activity screening. The aim of this paper is to provide a point of reference for pharmaceutical researchers to develop new drugs from constituents ofCaulophyllumplants.

scholarly journals A REVIEW OF BENZOPYRAN DERIVATIVES IN PHARMACOTHERAPY OF BREAST CANCER

2018 ◽  
Vol 11 (7) ◽  
pp. 43 ◽  
Author(s):  
Kumar Piyush ◽  
Singh Kuldeep ◽  
Rahman Md. Azizur ◽  
Hasan Syed Misbahul ◽  
Wal Pranay
Keyword(s):  
Breast Cancer ◽  
Natural Products ◽  
Biological Effects ◽  
Mechanisms Of Action ◽  
Ring System ◽  
Pharmacological Properties ◽  
Substitution Pattern ◽  
Naturally Occurring ◽  
Anti Hiv ◽  
Cancer Activity

One of the naturally occurring compounds containing oxygen moiety is benzopyran. Depending on its substitution pattern, different biological effects are shown. The benzopyran ring system is present in many natural products (such as genistein, hesperidin, and warfarin) as well as synthetic products. It displays pharmacological properties such as antitumor, anti-HIV, antimicrobials, anti-inflammatory, and anticoagulants. The sufficient literature support and the fact that benzopyran has potential as a pharmacophore particularly as anti-breast cancer, etc, current research seemed pertinent keeping in view the mechanism of anti-breast cancer activity. Therefore, the objective of this review is to focus on important benzopyran analogs with anti-breast cancer activity and highlight their mechanisms of action.

Ellagic Acid: A Logical Lead for Drug Development?

2018 ◽  
Vol 24 (2) ◽  
pp. 106-122 ◽  
Author(s):  
Abolfazl Shakeri ◽  
Mohammad Reza Zirak ◽  
Amirhossein Sahebkar
Keyword(s):  
Oxidative Stress ◽  
Ellagic Acid ◽  
Therapeutic Agent ◽  
Biological Activities ◽  
Biological Properties ◽  
Mechanisms Of Action ◽  
Human Diseases ◽  
Pharmacological Properties ◽  
Naturally Occurring ◽  
The Subject

Background: Naturally occurring polyphenols are the subject of increasing attention due to their potent antioxidant activity and their marked effects on the prevention of various oxidative stress-associated diseases such as cancer. Ellagic acid (EA) is an herbal polyphenol that is structurally a condensed dimer of gallic acid. Methods: This review aims to provide a comprehensive and updated overview on the biological activities of EA and potential therapeutic applications. Results: EA is found in fruits and nuts, either in the combined form with hexahydroxydiphenic acid or in the bound form (ellagitannins). EA exhibits many biological properties such as antioxidant, anti-diabetic, anticancer and apoptosis-inducing activities. These biological and pharmacological properties are relevant to the treatment of several human diseases. Conclusion: Owing to its multiple mechanisms of action, EA represents a potential therapeutic agent against human diseases particularly cancer.

scholarly journals Involvement of Cholinergic and Opioid System inγ-Terpinene-Mediated Antinociception

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Flávia Franceli de Brito Passos ◽  
Everton Moraes Lopes ◽  
Jonas Moura de Araújo ◽  
Damião Pergentino de Sousa ◽  
Leiz Maria C. Veras ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Structural Similarity ◽  
Mechanisms Of Action ◽  
Sedative Effect ◽  
New Drugs ◽  
Pharmacological Properties ◽  
Depressant Effect ◽  
Muscle Relaxant Activity ◽  
Opioid Systems ◽  
Central Depressant

The literature shows that the monoterpenes are great candidates for the development of new drugs for the treatment of various pathological processes, including painful conditions. The gamma terpinene (γ-TPN) is a monoterpene present in plant species that have multiple pharmacological properties and has structural similarity to antinociceptive monoterpenes, such as limonene and alpha-phellandrene. Theγ-TPN molecular mass was evaluated by mass spectrometry and showed a pseudomolecular ion withm/z137.0 Da. The animals did not present any signs of acute toxicity at 2 g/kg, p.o.γ-TPN (1.562 to 50 mg/kg, p.o.) showed an antinociceptive effect in the formalin, capsaicin, and glutamate tests.γ-TPN has antinociceptive action when administered by others routes in glutamate test. To eliminate a possible sedative effect ofγ-TPN, the open field and rota-rod test were conducted and theγ-TPN did not show muscle relaxant activity or central depressant effect. To investigate the mechanisms of action, the animals were pretreated with naloxone, glibenclamide, atropine, mecamylamine, or L-arginine in the glutamate test.γ-TPN antinociception was inhibited in the presence of naloxone, glibenclamide, atropine, and mecamylamine. The results suggest that theγ-TPN (p.o.) produced antinociceptive effect in models of chemical nociception through the cholinergic and opioid systems involvement.

scholarly journals Ferulic acid and derivatives: molecules with potential application in the pharmaceutical field

2013 ◽  
Vol 49 (3) ◽  
pp. 395-411 ◽  
Author(s):  
Lívia Brenelli de Paiva ◽  
Rosana Goldbeck ◽  
Wanderley Dantas dos Santos ◽  
Fabio Marcio Squina
Keyword(s):  
Ferulic Acid ◽  
Pharmacokinetic Profile ◽  
Mechanisms Of Action ◽  
Therapeutic Effects ◽  
Pharmacological Properties ◽  
Antioxidant Action ◽  
Treatment And Prevention ◽  
Action Mechanisms ◽  
Wide Range ◽  
Coa Reductase

Ferulic acid is a phenolic acid widely distributed in the plant kingdom. It presents a wide range of potential therapeutic effects useful in the treatments of cancer, diabetes, lung and cardiovascular diseases, as well as hepatic, neuro and photoprotective effects and antimicrobial and anti-inflammatory activities. Overall, the pharmaceutical potential of ferulic acid can be attributed to its ability to scavenge free radicals. However, recent studies have revealed that ferulic acid presents pharmacological properties beyond those related to its antioxidant activity, such as the ability to competitively inhibit HMG-CoA reductase and activate glucokinase, contributing to reduce hypercholesterolemia and hyperglycemia, respectively. The present review addresses ferulic acid dietary sources, the pharmacokinetic profile, antioxidant action mechanisms and therapeutic effects in the treatment and prevention of various diseases, in order to provide a basis for understanding its mechanisms of action as well as its pharmaceutical potential.

GABAA receptors: Various stoichiometrics of subunit arrangement in α1β3 and α1β3ε receptors

2018 ◽  
Vol 24 (17) ◽  
pp. 1839-1844 ◽  
Author(s):  
Ahmad Tarmizi Che Has ◽  
Mary Chebib
Keyword(s):  
Central Nervous System ◽  
Gabaa Receptors ◽  
Binding Sites ◽  
New Drugs ◽  
Pharmacological Properties ◽  
Receptor Complex ◽  
The Third ◽  
Γ Subunit ◽  
Subunit Stoichiometry ◽  
The Central Nervous System

GABAA receptors are members of the Cys-loop family of ligand-gated ion channels which mediate most inhibitory neurotransmission in the central nervous system. These receptors are pentameric assemblies of individual subunits, including α1-6, β1-3, γ1-3, δ, ε, π, θ and ρ1-3. The majority of receptors are comprised of α, β and γ or δ subunits. Depending on the subunit composition, the receptors are located in either the synapses or extrasynaptic regions. The most abundant receptors are α1βγ2 receptors, which are activated and modulated by a variety of pharmacologically and clinically unrelated agents such as benzodiazepines, barbiturates, anaesthetics and neurosteroids, all of which bind at distinct binding sites located within the receptor complex. However, compared to αβγ, the binary αβ receptors lack a benzodiazepine α-γ2 interface. In pentameric αβ receptors, the third subunit is replaced with either an α1 or a β3 subunit leading to two distinct receptors that differ in subunit stoichiometry, 2α:3β or 3α:2β. The consequence of this is that 3α:2β receptors contain an α-α interface whereas 2α:3β receptors contain a β-β interface. Apart from the replacement of γ by α1 or β3 in binary receptors, the incorporation of ε subunit into GABAA receptors might be more complicated. As the ε subunit is not only capable of substituting the γ subunit, but also replacing the α/β subunits, receptors with altered stoichiometry and different pharmacological properties are produced. The different subunit arrangement of the receptors potentially constructs novel binding sites which may become new targets of the current or new drugs.

Synthesis and Biological Activity of Embelin and its Derivatives: An Overview

2020 ◽  
Vol 20 (5) ◽  
pp. 396-407 ◽  
Author(s):  
Zhaojun Sheng ◽  
Siyuan Ge ◽  
Min Gao ◽  
Rongchao Jian ◽  
Xiaole Chen ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Effects ◽  
New Drugs ◽  
Hydroxyl Groups ◽  
Carbonyl Groups ◽  
Cellular Mechanisms ◽  
Embelia Ribes ◽  
Naturally Occurring ◽  
Ic50 Value ◽  
Apoptosis Protein

Embelin is a naturally occurring para-benzoquinone isolated from Embelia ribes (Burm. f.) of the Myrsinaceae family, and contains two carbonyl groups, a methine group and two hydroxyl groups. With embelin as the lead compound, more than one hundred derivatives have been reported. Embelin is well known for its ability to antagonize the X-linked inhibitor of apoptosis protein (XIAP) with an IC50 value of 4.1 μM. The potential of embelin and its derivatives in the treatment of various cancers has been extensively studied. In addition, these compounds display a variety of other biological effects: antimicrobial, antioxidant, analgesic, anti-inflammatory, anxiolytic and antifertility activity. This paper reviews the recent progress in the synthesis and biological activity of embelin and its derivatives. Their cellular mechanisms of action and prospects in the research and development of new drugs are also discussed.

Antimicrobial Peptides and their Multiple Effects at Sub-Inhibitory Concentrations

2020 ◽  
Vol 20 (14) ◽  
pp. 1264-1273 ◽  
Author(s):  
Bruno Casciaro ◽  
Floriana Cappiello ◽  
Walter Verrusio ◽  
Mauro Cacciafesta ◽  
Maria Luisa Mangoni
Keyword(s):  
Antimicrobial Peptides ◽  
Inhibitory Concentration ◽  
Multidrug Resistant ◽  
Mechanisms Of Action ◽  
New Drugs ◽  
Lead Compounds ◽  
Bacterial Pathogenicity ◽  
Growth Inhibitory ◽  
Resistant Strains ◽  
Conventional Antibiotics

The frequent occurrence of multidrug-resistant strains to conventional antimicrobials has led to a clear decline in antibiotic therapies. Therefore, new molecules with different mechanisms of action are extremely necessary. Due to their unique properties, antimicrobial peptides (AMPs) represent a valid alternative to conventional antibiotics and many of them have been characterized for their activity and cytotoxicity. However, the effects that these peptides cause at concentrations below the minimum growth inhibitory concentration (MIC) have yet to be fully analyzed along with the underlying molecular mechanism. In this mini-review, the ability of AMPs to synergize with different antibiotic classes or different natural compounds is examined. Furthermore, data on microbial resistance induction are reported to highlight the importance of antibiotic resistance in the fight against infections. Finally, the effects that sub-MIC levels of AMPs can have on the bacterial pathogenicity are summarized while showing how signaling pathways can be valid therapeutic targets for the treatment of infectious diseases. All these aspects support the high potential of AMPs as lead compounds for the development of new drugs with antibacterial and immunomodulatory activities.

scholarly journals Hemisynthesis and Biological Evaluation of Cinnamylated, Benzylated, and Prenylated Dihydrochalcones from a Common Bio-Sourced Precursor

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 620
Author(s):  
Anne Ardaillou ◽  
Jérôme Alsarraf ◽  
Jean Legault ◽  
François Simard ◽  
André Pichette
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Pharmacological Properties ◽  
Cytotoxic Potential ◽  
Naturally Occurring

Several families of naturally occurring C-alkylated dihydrochalcones display a broad range of biological activities, including antimicrobial and cytotoxic properties, depending on their alkylation sidechain. The catalytic Friedel–Crafts alkylation of the readily available aglycon moiety of neohesperidin dihydrochalcone was performed using cinnamyl, benzyl, and isoprenyl alcohols. This procedure provided a straightforward access to a series of derivatives that were structurally related to natural balsacones, uvaretin, and erioschalcones, respectively. The antibacterial and cytotoxic potential of these novel analogs was evaluated in vitro and highlighted some relations between the structure and the pharmacological properties of alkylated dihydrochalcones.

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