scholarly journals An Update on Pharmacological Potential of Boswellic Acids against Chronic Diseases

2019 ◽  
Vol 20 (17) ◽  
pp. 4101 ◽  
Author(s):  
Nand Kishor Roy ◽  
Dey Parama ◽  
Kishore Banik ◽  
Devivasha Bordoloi ◽  
Amrita Khwairakpam Devi ◽  
...  
Keyword(s):  
Chronic Diseases ◽  
Biological Activities ◽  
Boswellic Acid ◽  
Pentacyclic Triterpene ◽  
Boswellia Serrata ◽  
Wide Range ◽  
Molecular Mechanism Of Action ◽  
Inflammatory Bowel ◽  
Pharmacological Potential ◽  
Significant Attention

Natural compounds, in recent years, have attracted significant attention for their use in the prevention and treatment of diverse chronic diseases as they are devoid of major toxicities. Boswellic acid (BA), a series of pentacyclic triterpene molecules, is isolated from the gum resin of Boswellia serrata and Boswellia carteri. It proved to be one such agent that has exhibited efficacy against various chronic diseases like arthritis, diabetes, asthma, cancer, inflammatory bowel disease, Parkinson’s disease, Alzheimer’s, etc. The molecular targets attributed to its wide range of biological activities include transcription factors, kinases, enzymes, receptors, growth factors, etc. The present review is an attempt to demonstrate the diverse pharmacological uses of BA, along with its underlying molecular mechanism of action against different ailments. Further, this review also discusses the roadblocks associated with the pharmacokinetics and bioavailability of this promising compound and strategies to overcome those limitations for developing it as an effective drug for the clinical management of chronic diseases.

Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Justyna Żwawiak ◽  
Anna Pawełczyk ◽  
Dorota Olender ◽  
Lucjusz Zaprutko
Keyword(s):  
Biological Activities ◽  
Anticancer Activities ◽  
Drug Molecule ◽  
Pentacyclic Triterpene ◽  
Formation Pathway ◽  
Chemical Systems ◽  
Drug Molecules ◽  
Wide Range ◽  
Anti Hiv ◽  
Structure And Activity

: Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.

scholarly journals Organotin(IV) Dithiocarbamate Complexes: Chemistry and Biological Activity

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2571 ◽  
Author(s):  
Jerry Adeyemi ◽  
Damian Onwudiwe
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Molecular Structures ◽  
Tin Sulfide ◽  
Single Source ◽  
Hybrid Complex ◽  
Wide Range ◽  
Diverse Application ◽  
The Individual ◽  
Significant Attention

Significant attention has been given to organotin(IV) dithiocabamate compounds in recent times. This is due to their ability to stabilize specific stereochemistry in their complexes, and their diverse application in agriculture, biology, catalysis and as single source precursors for tin sulfide nanoparticles. These complexes have good coordination chemistry, stability and diverse molecular structures which, thus, prompt their wide range of biological activities. Their unique stereo-electronic properties underline their relevance in the area of medicinal chemistry. Organotin(IV) dithiocabamate compounds owe their functionalities and usefulness to the individual properties of the organotin(IV) and the dithiocarbamate moieties present within the molecule. These individual properties create a synergy of action in the hybrid complex, prompting an enhanced biological activity. In this review, we discuss the chemistry of organotin(IV) dithiocarbamate complexes that accounts for their relevance in biology and medicine.

Synthetic Methods and Pharmacological Potential of Different Oxazine Analogs

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohammad Asif ◽  
Mohd. Imran
Keyword(s):  
Organic Chemistry ◽  
Drug Resistance ◽  
Sodium Hydroxide ◽  
Crucial Role ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Wide Range ◽  
Different Types ◽  
Pharmacological Potential

: Oxazine analog is a vital class of heterocyclic compounds and has attracted synthetic interest owing to their wide range of biological activities. Oxazine analogs are valuable in medicinal organic chemistry and exhibited different varieties of biological activities such as antimicrobial, anticancer, antimalarial, antitubercular, sedative, anticonvulsant, analgesic, anti-inflammatory, antipyretic, etc. Oxazine can be derived from benzene by appropriate substitution of carbon atoms of the ring by nitrogen and oxygen atoms. Nowadays, the development of drug resistance is a key problem, and to defeat this problem, it is crucial to synthesize novel compounds. So novel oxazine analogs may play a crucial role to overcome these problems. Oxazine analogs are prepared by reaction of chalcone derivatives with thiourea in the presence of alcohol and sodium hydroxide. The present aims of this review to give an outline of some different synthetic methods and different types of biological activities of oxazine analogs. We hope that this review will be motivating for researchers concerned with oxazine analogs.

scholarly journals BOSWELLIA SERRATA ROXB. – A BIOACTIVE HERBS WITH VARIOUS PHARMACOLOGICAL ACTIVITIES

2020 ◽  
pp. 33-39
Author(s):  
SUDHANSHU MISHRA ◽  
RAM SINGH BISHNOI ◽  
RAHUL MAURYA ◽  
DEEPTI JAIN
Keyword(s):  
Biological Activities ◽  
Herbal Medicines ◽  
Boswellic Acid ◽  
Active Constituent ◽  
Pharmacological Activities ◽  
Boswellia Serrata ◽  
Medicinal Uses ◽  
Assisted Extraction ◽  
Extraction Processes ◽  
Phytochemical Components

Herbal medicine has become a medicinal as well as the economic aspect of global significance. While the use of these herbal medicines has increased, there are several questions about their consistency, protection, and effectiveness in different countries. Boswellic acid (BA) is one of the active constituents obtained from plant Boswellia serrata (BS) family Burseraceae. The oleoresin gum of the plant is also known as Salai guggul, Indian olibanum, or Indian frankincense. Boswellia species comprises a variety of phytochemical components, essential oil, BA such as keto-BA, beta-BA, or acetyl keto-BA. This variety of constituents isolated from the plant using various extraction processes such as hydrodistillation, percolation, and ultraviolet-assisted extraction or solvent extraction. The active constituent has different biological activities such as antidiuretic, anticancer, anti-inflammatory, or antitumor activity. This review seeks to update information on plant BS with its medicinal uses, isolation process in the traditional or Indian system of medicine, and justify its use on modern scientific parameters.

scholarly journals Potential Implications of Quercetin in Autoimmune Diseases

2021 ◽  
Vol 12 ◽  
Author(s):  
Pan Shen ◽  
Weiji Lin ◽  
Xuan Deng ◽  
Xin Ba ◽  
Liang Han ◽  
...  
Keyword(s):  
Autoimmune Diseases ◽  
Lupus Erythematosus ◽  
Biological Activities ◽  
Low Cost ◽  
Beneficial Effects ◽  
Positive Effects ◽  
Wide Range ◽  
Inflammatory Bowel ◽  
Anti Inflammation ◽  
Pharmacological Application

Autoimmune diseases are a worldwide health problem with growing rates of morbidity, and are characterized by breakdown and dysregulation of the immune system. Although their etiology and pathogenesis remain unclear, the application of dietary supplements is gradually increasing in patients with autoimmune diseases, mainly due to their positive effects, relatively safety, and low cost. Quercetin is a natural flavonoid that is widely present in fruits, herbs, and vegetables. It has been shown to have a wide range of beneficial effects and biological activities, including anti-inflammation, anti-oxidation, and neuroprotection. In several recent studies quercetin has reportedly attenuated rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis, and systemic lupus erythematosus in humans or animal models. This review summarizes the evidence for the pharmacological application of quercetin for autoimmune diseases, which supports the view that quercetin may be useful for their prevention and treatment.

scholarly journals Synthesis, Characterization and Biological Studies of Some Organotin Compounds: (A-Review)

2020 ◽  
Vol 36 (05) ◽  
pp. 871-878
Author(s):  
Priyanka Siwacha ◽  
Surbhi Soni ◽  
Harish Kumar Sharmaa ◽  
Manoj Kumara
Keyword(s):  
Amino Acids ◽  
Biological Activities ◽  
Organometallic Compounds ◽  
Molecular Structures ◽  
Organotin Compounds ◽  
Single Source ◽  
Biological Studies ◽  
Hybrid Complex ◽  
Wide Range ◽  
Significant Attention

Significant attention has been given to organotin (IV) amino acids compounds in recent years. Organometallic compounds are better known for their potentiality to stabilize peculiar stereochemistry of their complexes and application in agriculture, catalysis and as single source precursors. Due to the better stability and diverse molecular structures the complexes own a wide range of biological activities. These individual properties create an alliance of action in the hybrid complex. In this review, we discuss the chemistry of organotin (IV) complexes and their different aspects in various fields. The aim of the present review is to evaluate the synthesis, characterization and biological activities of organotin compounds.

scholarly journals Synthesis and Therapeutic Applications of Iminosugars in Cystic Fibrosis

2020 ◽  
Vol 21 (9) ◽  
pp. 3353 ◽  
Author(s):  
Anna Esposito ◽  
Daniele D’Alonzo ◽  
Maria De Fenza ◽  
Eliana De Gregorio ◽  
Anna Tamanini ◽  
...  
Keyword(s):  
Cystic Fibrosis ◽  
Biological Activities ◽  
Transmembrane Conductance Regulator ◽  
Medical Interventions ◽  
Processing Enzymes ◽  
Wide Range ◽  
Pharmacological Potential ◽  
Cf Transmembrane Conductance Regulator

Iminosugars are sugar analogues endowed with a high pharmacological potential. The wide range of biological activities exhibited by these glycomimetics associated with their excellent drug profile make them attractive therapeutic candidates for several medical interventions. The ability of iminosugars to act as inhibitors or enhancers of carbohydrate-processing enzymes suggests their potential use as therapeutics for the treatment of cystic fibrosis (CF). Herein we review the most relevant advances in the field, paying attention to both the chemical synthesis of the iminosugars and their biological evaluations, resulting from in vitro and in vivo assays. Starting from the example of the marketed drug NBDNJ (N-butyl deoxynojirimycin), a variety of iminosugars have exhibited the capacity to rescue the trafficking of F508del-CFTR (deletion of F508 residue in the CF transmembrane conductance regulator), either alone or in combination with other correctors. Interesting results have also been obtained when iminosugars were considered as anti-inflammatory agents in CF lung disease. The data herein reported demonstrate that iminosugars hold considerable potential to be applied for both therapeutic purposes.

scholarly journals Harmine and its derivatives: Biological activities and therapeutic potential in human diseases

2018 ◽  
Vol 13 (3) ◽  
pp. 203 ◽  
Author(s):  
Maria Javeed ◽  
Azhar Rasul ◽  
Ghulam Hussain ◽  
Farhat Jabeen ◽  
Bilal Rasool ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Biological Profile ◽  
Bioactive Component ◽  
Wide Range ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Molecular Mechanism Of Action ◽  
Reported Data

<p>This review article aims to provide an update on the sources, pharmaco-logical and biological profile of a β-carboline alkaloid, harmine which is a major bioactive component of various plants mainly Peganum harmala. Harmine’s wide range of pharmacological properties has been well-documented as anti-cancer, anti-inflammatory, anti-oxidant, neuroprotective, anti-depressant, and antimicrobial. Although reported data suggests a multifunctional pharmacological role of harmine but farther experimentation on its molecular mechanism of action, synthetic chemistry approaches, and preclinical studies are yet obligatory to fully uncover its pharmacological efficacy.</p>

Defined Structure-Activity Relationships of Boswellic Acids Determine Modulation of Ca2+ Mobilization and Aggregation of Human Platelets by Boswellia serrata Extracts

Planta Medica ◽  
2017 ◽  
Vol 83 (12/13) ◽  
pp. 1020-1027 ◽  
Author(s):  
Ulf Siemoneit ◽  
Lars Tausch ◽  
Daniel Poeckel ◽  
Michael Paul ◽  
Hinnak Northoff ◽  
...  
Keyword(s):  
Human Platelets ◽  
Boswellic Acid ◽  
Structural Determinants ◽  
Pentacyclic Triterpene ◽  
Experimental Conditions ◽  
Boswellia Serrata ◽  
Thromboxane A2 Receptor ◽  
Boswellic Acids ◽  
Risk Patients ◽  
Aggregation Of Platelets

AbstractBoswellic acids constitute a group of unique pentacyclic triterpene acids from Boswellia serrata with multiple pharmacological activities that confer them anti-inflammatory and anti-tumoral properties. A subgroup of boswellic acids, characterized by an 11-keto group, elevates intracellular Ca2+ concentrations [Ca2+]i and causes moderate aggregation of human platelets. How different BAs and their mixtures in pharmacological preparations affect these parameters in activated platelets has not been addressed, so far. Here, we show that boswellic acids either antagonize or induce Ca2+ mobilization and platelet aggregation depending on defined structural determinants with inductive effects predominating for a B. serrata gum resin extract. 3-O-Acetyl-11-keto-β-boswellic acid potently suppressed Ca2+ mobilization (IC50 = 6 µM) and aggregation (IC50 = 1 µM) when platelets were activated by collagen or the thromboxane A2 receptor agonist U-46619, but not upon thrombin. In contrast, β-boswellic acid and 3-O-acetyl-β-boswellic acid, which lack the 11-keto moiety, were weak inhibitors of agonist-induced platelet responses, but instead they elicited elevation of [Ca2+]i and aggregation of platelets (≥ 3 µM). 11-Keto-β-boswellic acid, the structural intermediate between 3-O-acetyl-11-keto-β-boswellic acid and β-boswellic acid, was essentially inactive independent of the experimental conditions. Together, our study unravels the complex agonizing and antagonizing properties of boswellic acids on human platelets in pharmacologically relevant preparations of B. serrata gum extracts and prompts for careful evaluation of the safety of such extracts as herbal medicine in cardiovascular risk patients.

scholarly journals Aucuboside Inhibits the Generation of Th17 Cells in Mice Colitis

2021 ◽  
Vol 12 ◽  
Author(s):  
Chenxue Mei ◽  
Xiao Wang ◽  
Fanxiang Meng ◽  
Xiaoqing Zhang ◽  
Ling Chen ◽  
...  
Keyword(s):  
Th17 Cells ◽  
Inflammatory Responses ◽  
Activity Index ◽  
Biological Activities ◽  
Disease Activity Index ◽  
Treg Cells ◽  
Trinitrobenzene Sulfonic Acid ◽  
Wide Range ◽  
Inflammatory Bowel ◽  
Colitis Model

Aucuboside is an iridoid glycoside extracted from traditional Chinese medicine such as Rehmannia glutinosa, possessing a wide range of biological activities, including antioxidant, anti-aging, anti-inflammatory, and anti-fibrotic effects. The effects of aucuboside on inflammatory bowel disease (IBD) have not been studied. Therefore, the effects of aucuboside on the generation of Foxp3+ regulatory T (Treg) cells and IL-17–producing T helper (Th17) cells in colitis were studied. A mouse colitis model was established by intracolonic administration of 2,4,6-trinitrobenzene sulfonic acid (TNBS) to mimic human IBD. The generation of Treg and Th17 cells was evaluated by flow cytometry. Aucuboside significantly alleviated colitis symptoms, including weight loss, high disease activity index, and inflammatory responses. The generation of Th17 cells in colitis was significantly inhibited by aucuboside and accompanied by the suppression of IL-17 expression. In Raw264.7 cells, the LPS-induced increase in IL-17 expression was also suppressed by aucuboside, which was significantly blocked by the RORγt inhibitor sr2211. In addition, the decrease in the proportion of Treg cells was also partially reversed by aucuboside, which may reflect the aucuboside-induced inhibition of Th17 cells. This previously unrecognized immunoregulatory function of aucuboside may have clinical applications in IBD.

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