Bioactive Molecules from the Alpinia Genus: A Comprehensive Review

2020 ◽  
Vol 21 (14) ◽  
pp. 1412-1421 ◽  
Author(s):  
Santwona Dash ◽  
Manasa K. Panda ◽  
Mayanglambam C. Singh ◽  
Bimal P. Jit ◽  
Yengkhom D. Singh ◽  
...  
Keyword(s):  
Enzyme Inhibitors ◽  
Complex Structure ◽  
Biologically Active ◽  
Bioactive Molecules ◽  
Therapeutic Applications ◽  
Traditional Remedies ◽  
Wide Range ◽  
Natural Enzyme ◽  
Unique Nature ◽  
Metabolic Activities

Background: Floral has diversity and unique nature due to the complex structure and component. Alpinia is an important genus of the Zingiberaceae family having complex taxonomical diversity. The presence of many unique bioactive molecules makes this genus, a pharmaceutically important genus. They provide a wide range of medicinal properties, including traditional remedies to modern therapeutic applications. Methods: Extracts of Alpinia mostly contain bioactive molecules and secondary metabolites such as polyphenolics, tannins, flavonoids and other therapeutically important compounds. These bioactive molecules are biologically active, treating against inflammation, cancer, arterial hypertension, and other deadly diseases. Results: These bioactive molecules can act as natural enzyme inhibitors for some of the deadly diseases and can block the pathway for metabolic activities. In addition, these genera have played a major role in multidisciplinary studies of phytochemistry, ethnobotany, and pharmacological aspects in day-to-day life. Conclusion: Therefore, this review highlights the fewer known facts of the genus Alpinia in terms of bioactive molecules and its significant therapeutic applications to help in combating major diseases of humans.

scholarly journals Regiospecific synthesis of 2,3-disubstituted indoles from isatins

2016 ◽  
Author(s):  
Artur Ulikowski ◽  
Anna Jaromin ◽  
Giorgia Brancolini ◽  
Luca Bellucci ◽  
Bartłomiej Furman
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Functional Group ◽  
Enzyme Inhibitors ◽  
Biologically Active ◽  
Special Importance ◽  
Indole Derivatives ◽  
Structural Element ◽  
Wide Range ◽  
Ache Inhibitory Activity

Indoles represent a structural element in a myriad of natural products and biologically active molecules. Of special importance are 2,3-disubstituted indoles. Thus, a number of methods for their synthesis have been described. However, these are often hampered by a number of limitations: they often offer poor regioselectivity and suboptimal functional group tolerance. Also, they can normally be adapted to the procurement of a small subclass of indoles only. We have developed an approach to 2,3-disubstituted indoles overcoming these obstacles. By selectively activating the amide carbonyl in isatin-derived oxindoles, we obtained a number of the title compounds in a regiospecific and functional group-tolerant manner. The methodology is normally characterized by excellent yields. The reaction proceeds by chemoselective partial reduction of the amide moiety to an iminium salt and a subsequent nucleophilic addition followed by dehydration, which furnishes the target indole. A number of nucleophiles, including C- and S-nucleophiles, have been examined. The obtained compounds were studied towards acetylcholinesterase (AChE) inhibitory activity, as the indole skeleton is often seen in the struc-ture of enzyme inhibitors. Cholinesterase inhibitors are used in the treatment of Alzheimer's disease, increasing available acetylcholine by decreasing the AChE activity. For the tested agents, properties like logP, logBBB (Blood-Brain Barier penetration) and Caco2 permeabilities were also calculated. Based on the predicted values, only two of them are able to penetrate into the CNS (central nervous system). Molecular docking was performed on the whole set of the syntesized indole derivatives, resulting in a wide range of AChE inhibitory activity. Molecular docking binding interactions reported the lowest energy conformations of the syntesized compounds and the key amino acid residues at the active binding site of AChE. The current synergy between computations and experiments provided the identification of the indole derivatives exhibiting the highest inhibitory activity. The presented results will provide theoretical guidance for further modification and optimization of the indole derivatives.

scholarly journals Bioactive composites for bone regeneration

2019 ◽  
Vol 1 (1) ◽  
pp. 9-15
Author(s):  
Alexandra-Cristina Burdușel
Keyword(s):  
Glass Ceramics ◽  
Ceramic Materials ◽  
Biologically Active ◽  
Bone Tissue Regeneration ◽  
Organ Protection ◽  
Living Body ◽  
Wide Range ◽  
Living Bone ◽  
Metabolic Activities ◽  
Bioactive Composites

Bone, the organ that separates vertebrates from other living beings, is a complex tissue responsible of mobility, body stability, organ protection, and metabolic activities such as ion storage. Ceramic materials are appropriate candidates to be used in the fabrication of scaffolds for bone healing. Biocompatible ceramic materials may also be created to deliver biologically active substances aimed at maintaining, repairing, restoring, or boosting the function of tissues and organs in the organism. Glass-ceramic materials furnish flexible properties appropriate for some particular applications. Because of the controlled devitrification and the evolution of variable dimensions of crystalline and glassy phases, glass-ceramics considerably overcome the lacunae found in glasses. A wide range of bioactive glass compositions had been developed since the early 1970s to make them appropriate for many clinical applications. Many bioactive ceramic composite materials attach to living bone through an apatite layer, which is developed on their surfaces in the living body. This paper reviews the most used bioactive ceramics for bone tissue regeneration, with specific accentuation on the material characteristics.

scholarly journals PRELIMINARY SCREENING OF PHYTOCHEMICALS AND ANTIPROLIFERATIVE AND ANTI-INFLAMMATORY PROPERTIES OF THESPESIA POPULNEA (L.) SOLAND LEAF EXTRACTS

2018 ◽  
Vol 11 (5) ◽  
pp. 382
Author(s):  
Megha Kb ◽  
Sanith Cheriyamundath ◽  
Joseph Madassery ◽  
Elyas Kk
Keyword(s):  
Leaf Extract ◽  
Chemical Constituents ◽  
Biologically Active ◽  
Bioactive Molecules ◽  
Phytochemical Analysis ◽  
Leaf Extracts ◽  
Thespesia Populnea ◽  
Wide Range ◽  
Anti Inflammatory

Objective: Plant-derived bioactive molecules are providing infinite opportunities for new drug development as they possess a wide range of actions against diseases with lesser side effects. The present study is made to analyze the qualitative phytochemicals and to evaluate in vitro antiproliferative and anti-inflammatory potentials of leaf extracts of Thespesia populnea. Methods: T. populnea leaf extracts were prepared sequentially according to the increasing polarity of the solvents, i.e., petroleum ether, chloroform, ethyl acetate, and methanol. Qualitative phytochemical analysis was performed to identify the chemical constituents of the extracts, and antiproliferative properties were evaluated against different cell lines using the 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide assay. Bovine serum albumin anti-denaturation assay was done to identify the anti-inflammatory activity.Results: Phytochemical analysis of the extracts revealed the presence of alkaloids, terpenoids, glycosides, tannins, flavonoids, and phenolics. The chloroform extract (CHFE) of T. populnea has a dose-dependent antiproliferative effect against acute T-cell leukemia (Jurkat E6-1), prostate Grade IV adenocarcinoma (PC-3), mouse fibroblast (L-929), and monkey kidney normal (Vero) cells. Their inhibitory concentration 50% (IC50) values were found to be 35.73±0.94 μg/ml for Jurkat E6-1, 60.79±1.84 μg/ml for PC-3, 60.88±1.45 μg/ml for L-929, and 83.482±2.05 μg/ml for Vero, respectively. CHFE also displayed the anti-inflammatory potential.Conclusion: The chloroform leaf extract of T. populnea possesses potent antiproliferative and anti-inflammatory activity. These properties present in leaf extract may be explained by the presence of biologically active constituents.

scholarly journals Regiospecific synthesis of 2,3-disubstituted indoles from isatins

2016 ◽  
Author(s):  
Artur Ulikowski ◽  
Anna Jaromin ◽  
Giorgia Brancolini ◽  
Luca Bellucci ◽  
Bartłomiej Furman
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Functional Group ◽  
Enzyme Inhibitors ◽  
Biologically Active ◽  
Special Importance ◽  
Indole Derivatives ◽  
Structural Element ◽  
Wide Range ◽  
Ache Inhibitory Activity

Indoles represent a structural element in a myriad of natural products and biologically active molecules. Of special importance are 2,3-disubstituted indoles. Thus, a number of methods for their synthesis have been described. However, these are often hampered by a number of limitations: they often offer poor regioselectivity and suboptimal functional group tolerance. Also, they can normally be adapted to the procurement of a small subclass of indoles only. We have developed an approach to 2,3-disubstituted indoles overcoming these obstacles. By selectively activating the amide carbonyl in isatin-derived oxindoles, we obtained a number of the title compounds in a regiospecific and functional group-tolerant manner. The methodology is normally characterized by excellent yields. The reaction proceeds by chemoselective partial reduction of the amide moiety to an iminium salt and a subsequent nucleophilic addition followed by dehydration, which furnishes the target indole. A number of nucleophiles, including C- and S-nucleophiles, have been examined. The obtained compounds were studied towards acetylcholinesterase (AChE) inhibitory activity, as the indole skeleton is often seen in the struc-ture of enzyme inhibitors. Cholinesterase inhibitors are used in the treatment of Alzheimer's disease, increasing available acetylcholine by decreasing the AChE activity. For the tested agents, properties like logP, logBBB (Blood-Brain Barier penetration) and Caco2 permeabilities were also calculated. Based on the predicted values, only two of them are able to penetrate into the CNS (central nervous system). Molecular docking was performed on the whole set of the syntesized indole derivatives, resulting in a wide range of AChE inhibitory activity. Molecular docking binding interactions reported the lowest energy conformations of the syntesized compounds and the key amino acid residues at the active binding site of AChE. The current synergy between computations and experiments provided the identification of the indole derivatives exhibiting the highest inhibitory activity. The presented results will provide theoretical guidance for further modification and optimization of the indole derivatives.

Heparin and proteoglycans as anti-inflammatory drugs

1996 ◽  
Vol 16 (01) ◽  
pp. 56-59
Author(s):  
D. J. Tyrrell ◽  
C. P. Page
Keyword(s):  
Inflammatory Diseases ◽  
Therapeutic Applications ◽  
Wide Range ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

SummaryEvidence continues to accumulate that the pleiotropic nature of heparin (beyond its anticoagulant potency) includes anti-inflammatory activities at a number of levels. It is clear that drugs exploiting these anti-inflammatory activities of heparin may offer exciting new therapeutic applications to the treatment of a wide range of inflammatory diseases.

Aspergillus sydowii Strain SCAU066 and Aspergillus versicolor Isolate BAB-6580: Potential Source of Xylanolytic, Cellulolytic and Amylolytic Enzymes

2020 ◽  
Vol 14 (2) ◽  
pp. 15
Author(s):  
Zaidah Zainal ariffin
Keyword(s):  
Extracellular Enzymes ◽  
Biologically Active ◽  
Aspergillus Versicolor ◽  
Aspergillus Sydowii ◽  
Aspergillus Tamarii ◽  
Alternative Source ◽  
Amylolytic Enzymes ◽  
Potato Dextrose Broth ◽  
Wide Range ◽  
Pharmaceutical Industries

Fungi is known to produce a wide range of biologically active metabolites and enzymes. Enzymes produced by fungi are utilized in food and pharmaceutical industries because of their rich enzymatic profile. Filamentous fungi are particularly interesting due to their high production of extracellular enzymes which has a large industrial potential. The aim of this study is to isolate potential soil fungi species that are able to produce functional enzymes for industries. Five Aspergillus species were successfully isolated from antibiotic overexposed soil (GPS coordinate of N3.093219 E101.40269) by standard microbiological method. The isolated fungi were identified via morphological observations and molecular tools; polymerase chain reactions, ITS 1 (5’- TCC GTA GGT GAA CCT GCG G3’) forward primer and ITS 4 (5’-TCC TCC GCT TAT TGA TAT GC-3’) reverse primer. The isolated fungi were identified as Aspergillus sydowii strain SCAU066, Aspergillus tamarii isolate TN-7, Aspergillus candidus strain KUFA 0062, Aspergillus versicolor isolate BAB-6580, and Aspergillus protuberus strain KAS 6024. Supernatant obtained via submerged fermentation of the isolated fungi in potato dextrose broth (PDB) and extracted via centrifugation was loaded onto specific media to screen for the production of xylanolytic, cellulolytic and amylolytic enzymes. The present findings indicate that Aspergillus sydowii strain SCAU066 and Aspergillus versicolor isolate BAB-6580 have great potential as an alternative source of xylanolytic, cellulolytic and amylolytic enzymes.

The content of decenoic acids in drone brood preparations and combined preparations based on it

Biomics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 389-393
Author(s):  
D.V. Mitrofanov ◽  
N.V. Budnikova
Keyword(s):  
Royal Jelly ◽  
Storage Conditions ◽  
Water Soluble ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Strict Adherence ◽  
Drone Brood ◽  
Wide Range ◽  
Active Substances ◽  
Melanin Complex

The drone brood contains a large number of substances with antioxidant activity. These substances require stabilization and strict adherence to storage conditions. Among these substances are unique decenoic acids, the content of which is an indicator of the quality of drone brood and products based on it. The ability of drone brood to reduce the manifestations of oxidative stress is shown. There are dietary supplements for food and drugs based on drone brood, which are used for a wide range of diseases. Together with drone brood, chitosan-containing products, propolis, royal jelly can be used. They enrich the composition with their own biologically active substances and affect the preservation of the biologically active substances of the drone brood. Promising are the products containing, in addition to the drone brood, a chitin-chitosan-melanin complex from bees, propolis, royal jelly. The chitin-chitosan-melanin complex in the amount of 5% in the composition of the adsorbent practically does not affect the preservation of decenic acids, while in the amount of 2% and 10% it somewhat worsens. The acid-soluble and water-soluble chitosan of marine crustaceans significantly worsens the preservation of decenoic acids in the product. Drone brood with royal jelly demonstrates a rather high content of decenoic acids. When propolis is introduced into the composition of the product, the content of decenoic acids increases according to the content of propolis.

Privileged Structures in the Design of Potential Drug Candidates for Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4323-4354 ◽  
Author(s):  
Ana Cristina Lima Leite ◽  
José Wanderlan Pontes Espíndola ◽  
Marcos Veríssimo de Oliveira Cardoso ◽  
Gevanio Bezerra de Oliveira Filho
Keyword(s):  
Biologically Active ◽  
Neglected Diseases ◽  
Financial Return ◽  
Drug Candidates ◽  
Lead Compounds ◽  
Wide Range ◽  
Methods Of Synthesis ◽  
Current Therapies ◽  
Resistant Strains ◽  
Privileged Structures

Background: Privileged motifs are recurring in a wide range of biologically active compounds that reach different pharmaceutical targets and pathways and could represent a suitable start point to access potential candidates in the neglected diseases field. The current therapies to treat these diseases are based in drugs that lack of the desired effectiveness, affordable methods of synthesis and allow a way to emergence of resistant strains. Due the lack of financial return, only few pharmaceutical companies have been investing in research for new therapeutics for neglected diseases (ND). Methods: Based on the literature search from 2002 to 2016, we discuss how six privileged motifs, focusing phthalimide, isatin, indole, thiosemicarbazone, thiazole, and thiazolidinone are particularly recurrent in compounds active against some of neglected diseases. Results: It was observed that attention was paid particularly for Chagas disease, malaria, tuberculosis, schistosomiasis, leishmaniasis, dengue, African sleeping sickness (Human African Trypanosomiasis - HAT) and toxoplasmosis. It was possible to verify that, among the ND, antitrypanosomal and antiplasmodial activities were between the most searched. Besides, thiosemicarbazone moiety seems to be the most versatile and frequently explored scaffold. As well, phthalimide, isatin, thiazole, and thiazolidone nucleus have been also explored in the ND field. Conclusion: Some described compounds, appear to be promising drug candidates, while others could represent a valuable inspiration in the research for new lead compounds.

Exploring siRNA Umpired Nanogels: A Tale of Barrier Combating Carrier

2020 ◽  
Vol 26 (27) ◽  
pp. 3234-3250
Author(s):  
Sushil K. Kashaw ◽  
Prashant Sahu ◽  
Vaibhav Rajoriya ◽  
Pradeep Jana ◽  
Varsha Kashaw ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Biomedical Engineering ◽  
Viral Infections ◽  
Slow Release ◽  
Molecular Level ◽  
Release Kinetics ◽  
Biologically Active ◽  
Release Process ◽  
Rapid Release ◽  
Wide Range

Potential short interfering RNAs (siRNA) modulating gene expression have emerged as a novel therapeutic arsenal against a wide range of maladies and disorders containing cancer, viral infections, bacterial ailments and metabolic snags at the molecular level. Nanogel, in the current medicinal era, displayed a comprehensive range of significant drug delivery prospects. Biodegradation, swelling and de-swelling tendency, pHsensitive drug release and thermo-sensitivity are some of the renowned associated benefits of nanogel drug delivery system. Global researches have also showed that nanogel system significantly targets and delivers the biomolecules including DNAs, siRNA, protein, peptides and other biologically active molecules. Biomolecules delivery via nanogel system explored a wide range of pharmaceutical, biomedical engineering and agro-medicinal application. The siRNAs and DNAs delivery plays a vivacious role by addressing the hitches allied with chronic and contemporary therapeutic like generic possession and low constancy. They also incite release kinetics approach from slow-release while mingling to rapid release at the targets will be beneficial as interference RNAs delivery carriers. Therefore, in this research, we focused on the latest improvements in the delivery of siRNA loaded nanogels by enhancing the absorption, stability, sensitivity and combating the hindrances in cellular trafficking and release process.

Indium Bromide-catalyzed Unprecedented Hydrogenolysis: A Novel One-Pot Synthesis of Per-O-Acetylated β-carboxymethyl O and S-glycosides

2020 ◽  
Vol 24 (8) ◽  
pp. 900-908
Author(s):  
Ram Naresh Yadav ◽  
Amrendra K Singh ◽  
Bimal Banik
Keyword(s):  
Asymmetric Synthesis ◽  
Chiral Auxiliary ◽  
Bioactive Molecules ◽  
One Pot ◽  
Enantiomerically Pure ◽  
Stereoselective Glycosylation ◽  
One Pot Synthesis ◽  
Wide Range

Numerous O (oxa)- and S (thia)-glycosyl esters and their analogous glycosyl acids have been accomplished through stereoselective glycosylation of various peracetylated bromo sugar with benzyl glycolate using InBr3 as a glycosyl promotor followed by in situ hydrogenolysis of resulting glycosyl ester. A tandem glycosylating and hydrogenolytic activity of InBr3 has been successfully investigated in a one-pot procedure. The resulting synthetically valuable and virtually unexplored class of β-CMGL (glycosyl acids) could serve as an excellent potential chiral auxiliary in the asymmetric synthesis of a wide range of enantiomerically pure medicinally prevalent β-lactams and other bioactive molecules of diverse medicinal interest.

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