scholarly journals Preparation, characterization and featuring of an inclusion complex of nerol with β-cyclodextrin

2017 ◽  
Vol 5 (2) ◽  
pp. 195
Author(s):  
Mayara Coêlho ◽  
Herlane Da Silva ◽  
Muhammad Islam ◽  
Vicente Viana ◽  
Ana Amélia Melo-Cavalcante
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Biological Activities ◽  
Aqueous Media ◽  
Limiting Factor ◽  
Thermo Gravimetric ◽  
Drug Molecules ◽  
Complex Cavity ◽  
Nonpolar Molecules ◽  
Low Solubility

Nerol is an acyclic type monoterpene with important biological activities. However, the low solubility in aqueous media is a limiting factor for its user. Cyclodextrins have been widely used in order to improve the solubility, stability and bioavailability of nonpolar molecules through the formation of inclusion complexes. Thus, the present study consists in the development of nerol inclusion complex in combination with the β-cyclodextrin (β-CD) followed by characterizing by thermal analysis and spectrophotometric absorption in the infrared (FTIR). The results suggest a complexation of nerol with β-CD having detours and changed the intensity of various bands. The thermo gravimetric curve of CI found to indicate an output of solvating water molecules from the complex cavity formed for replacement of drug molecules probably included. Thus, it is concluded a possibility to obtain inclusion complexes of nerol monoterpene with β-CD, which will increase its solubility and facilitate delivery process.

scholarly journals α-Mangostin/γ-Cyclodextrin Inclusion Complex: Formation and Thermodynamic Study

Polymers ◽  
2021 ◽  
Vol 13 (17) ◽  
pp. 2890
Author(s):  
Ine Suharyani ◽  
Muchtaridi Muchtaridi ◽  
Ahmed Fouad Abdelwahab Mohammed ◽  
Khaled M. Elamin ◽  
Nasrul Wathoni ◽  
...  
Keyword(s):  
Complex Formation ◽  
Inclusion Complex ◽  
Biological Activities ◽  
Entrapment Efficiency ◽  
Thermodynamic Study ◽  
Solubility In Water ◽  
Solubility Improvement ◽  
Poorly Soluble ◽  
Anti Fungal ◽  
Low Solubility

α-Mangostin (α-M) has various biological activities, such as anti-cancer, antibacterial, anti-fungal, anti-tyrosin, anti-tuberculosis, anti-inflammatory, and antioxidant. However, it has very low solubility in water. The formulation of this compound requires high amounts of solubilizers, which limits its clinical application. In addition, its low solubility in water is a barrier to the distribution of this drug, thus affecting its potency. Cyclodextrin (CD) is widely used as a solubility enhancer of poorly soluble drugs. This study aimed to increase the solubility of α-M in water through complex formation with CD. The complex of α-Mangostin and γ-Cyclodextrin (α-M/γ-CD CX) was prepared by the solubilization method, resulting in a solubility improvement of α-M in water. Characterization of α-M/γ-CD CX by using FTIR-Spectrometry, XRD, H-, C-, and HMBC-NMR showed that α-M was able to form an inclusion complex with γ-CD. The complex yielded an entrapment efficiency of 84.25 and the thermodynamic study showed that the α-M/γ-CD CX was formed spontaneously, based on the negative values of Gibbs energy and ΔH. Interestingly, the solubility of α-M/γ-CD CX significantly increased by 31.74-fold compared with α-M. These results suggest that α-M/γ-CD CX has the potential in the formulation of water-based preparation for clinical applications.

NMR Studies of the Inclusion Complexes Between Ezetimibe and Cyclodextrins

2018 ◽  
Vol 69 (7) ◽  
pp. 1838-1841
Author(s):  
Hajnal Kelemen ◽  
Angella Csillag ◽  
Bela Noszal ◽  
Gabor Orgovan
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Water Solubility ◽  
Solution Nmr ◽  
Spectroscopic Techniques ◽  
Nmr Studies ◽  
The Poor ◽  
Poor Water Solubility

Ezetimibe, the antihyperlipidemic drug of poor bioavailability was complexed with native and derivatized cyclodextrins.The complexes were characterized in terms stability, stoichiometry and structure using various 1D and 2D solution NMR spectroscopic techniques. The complexes were found to be of moderate stability (logK[3). The least stable inclusion complex is formed with b-cyclodextrin, while the ezetimibe-methylated-b--cyclodextrin has a 7-fold higher stability. The results can be useful to improve the poor water-solubility and the concomitant bioavailability of ezetimibe.

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.

Medicinal Chemistry of Alternative Therapeutics: Novelty and Hopes with Genus Ammannia

2019 ◽  
Vol 19 (10) ◽  
pp. 784-794 ◽  
Author(s):  
Harish C. Upadhyay
Keyword(s):  
Traditional Medicine ◽  
Biological Activities ◽  
World Health ◽  
Biologically Relevant ◽  
Traditional Medicines ◽  
Drug Molecules ◽  
Health Organization ◽  
Tract Infections ◽  
Pharmacologically Active ◽  
Herbal Formulations

The plants have formed the basis of folklore remedy since the beginning of human civilization. The cumulative human endeavor and experience over a period of thousands of years developed into well to organize traditional medicine systems viz. Ayurvedic, Unani, Chinese amongst others. Across the world, traditional medicine is either the mainstay of health care or serves as a complement to modern drugs. In view of worldwide use of traditional medicines, World Health Organization launched ‘WHO-Traditional Medicine Strategy 2014-2023’ for the development of strong policies regarding knowledge-base, safety, quality-control and effectiveness of traditional/alternative therapeutics for national health systems. Besides their use in traditional medicine, plants have always been a good source of modern drug/pharmacologically active molecules. More than half of the modern pharmaceuticals are either plant isolates or their derivatives. The plant-based drugs are not only effective, but have better compatibility with human biological systems because of more biologically relevant chemistry, hence lesser side effects. Some of the species of genus Ammannia (Lythraceae) have been reported for their magical medicinal values. Many herbal formulations containing Ammannia spp. have been patented for treatment of serious diseases/disorders like cancer, spinal disease, human female infertility, chronic tonsillitis, pelvic inflammatory disease, treatment of bladder stones, urinary tract infections, dermatitis etc. The uses of Ammannia spp. in traditional medicine have been further verified by the biological activities of their extracts as well as isolation of bioactive phytomolecules. The current review provides details about Ammannia spp.; its use in folklore remedy, herbal formulations, biological activities of extracts, isolation of bioactive phytomolecules and SAR study of semi-synthetic derivatives to analyze the possibility of new drug molecules of plant origin.

Combinatorial Design of Molecule using Activity-Linked Substructural Topological Information as Applied to Antitubercular Compounds

2018 ◽  
Vol 15 (1) ◽  
pp. 67-81 ◽  
Author(s):  
Chandan Raychaudhury ◽  
Md. Imbesat Hassan Rizvi ◽  
Debnath Pal
Keyword(s):  
Biological Activities ◽  
Combinatorial Design ◽  
Combinatorial Structure ◽  
Potential Drug ◽  
Structure Generation ◽  
Topological Information ◽  
Active Compounds ◽  
Antitubercular Drugs ◽  
Topological Distance ◽  
Drug Molecules

Background: Generating a large number of compounds using combinatorial methods increases the possibility of finding novel bioactive compounds. Although some combinatorial structure generation algorithms are available, any method for generating structures from activity-linked substructural topological information is not yet reported. Objective: To develop a method using graph-theoretical techniques for generating structures of antitubercular compounds combinatorially from activity-linked substructural topological information, predict activity and prioritize and screen potential drug candidates. </P><P> Methods: Activity related vertices are identified from datasets composed of both active and inactive or, differently active compounds and structures are generated combinatorially using the topological distance distribution associated with those vertices. Biological activities are predicted using topological distance based vertex indices and a rule based method. Generated structures are prioritized using a newly defined Molecular Priority Score (MPS). Results: Studies considering a series of Acid Alkyl Ester (AAE) compounds and three known antitubercular drugs show that active compounds can be generated from substructural information of other active compounds for all these classes of compounds. Activity predictions show high level of success rate and a number of highly active AAE compounds produced high MPS score indicating that MPS score may help prioritize and screen potential drug molecules. A possible relation of this work with scaffold hopping and inverse Quantitative Structure-Activity Relationship (iQSAR) problem has also been discussed. The proposed method seems to hold promise for discovering novel therapeutic candidates for combating Tuberculosis and may be useful for discovering novel drug molecules for the treatment of other diseases as well.

scholarly journals The guest polymer effect on the dissolution of drug–polymer crystalline inclusion complexes

RSC Advances ◽  
2021 ◽  
Vol 11 (22) ◽  
pp. 13091-13096
Author(s):  
Lu Chen ◽  
Yanbin Huang
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Significant Influence ◽  
Crystalline Inclusion ◽  
Complex Crystals

Guest polymers have significant influence on the dissolution of drug–polymer inclusion complex crystals.

The influence of the host–guest interaction on the oxidation of natural flavonoid dyes

2011 ◽  
Vol 76 (12) ◽  
pp. 1651-1667 ◽  
Author(s):  
Šárka Ramešová ◽  
Romana Sokolová ◽  
Ilaria Degano ◽  
Magdaléna Hromadová ◽  
Miroslav Gál ◽  
...  
Keyword(s):  
Cyclic Voltammetry ◽  
Inclusion Complex ◽  
Fluorescence Intensity ◽  
Oxidation Product ◽  
Aqueous Media ◽  
Electrochemical Methods ◽  
Redox Potentials ◽  
Decomposition Products ◽  
Degradation Processes ◽  
Bioorganic Compounds

The influence of the molecular cavity protection on degradation processes of bioorganic compounds quercetin and luteolin used as the original dyes in old tapestries was studied. The degradation processes were studied by electrochemical methods in aqueous media. The products of the exhaustive electrolysis were separated and identified by GC-MS analysis. Cyclic voltammetry characteristics indicate that the inclusion complex is formed. The inclusion affects the redox potentials of both oxidation waves related to the different dissociation forms of the flavonoid molecule. It was shown that decomposition products formed by the oxidation of quercetin are stabilized in the cavity of β-cyclodextrin, including the main oxidation product 2(3′,4′-dihydroxybenzoyl)-2,4,6-trihydroxybenzofuran-3(2H)-one. The formation of the 1:1 inclusion complex of luteolin with β-cyclodextrin is supported by the enhancement of fluorescence intensity. In the case of quercetin, a decrease of fluorescence intensity occurs when 1:1 inclusion complex with β-cyclodextrin is formed.

Oxygen-Enriched Gas in Bioleaching Stirred Reactors and its Impact on the Consortium Behaviour

2015 ◽  
Vol 1130 ◽  
pp. 214-217
Author(s):  
Catherine Joulian ◽  
Jérôme Jacob ◽  
Mickaël Beaulieu ◽  
Patrick d’Hugues ◽  
Anne Gwénaëlle Guézennec
Keyword(s):  
Primary Objective ◽  
Community Diversity ◽  
Limiting Factor ◽  
Gas Transfer ◽  
Heat Management ◽  
Bacterial Leaching ◽  
Partial Pressures ◽  
Process Operation ◽  
Low Solubility ◽  
Stirred Reactors

In bioleaching processes, gas transfer is often considered as one of the key mechanisms that will influence the leaching efficiency and more precisely the leaching rate. Oxygen can be a limiting factor in bacterial leaching because of its low solubility. One way to overcome this phenomenon consists in increasing the oxygen partial pressure in the gas stream supplied to the leach pulp. The primary objective of this work was to investigate the use of oxygen-enriched gas in bioleaching stirred reactors and its impact on the consortium dynamics. First tests were performed at lab scale in four successive series of 2-L bioreactors alimented either with air or with oxygen enriched gas. The microbial consortium used has proven its efficiency on several ores such as cobaltiferous pyrite and polymetallic ores in former research projects (BioMine, BioShale, ProMine). The community diversity was remarkably reproducible irrespective of the type of gas supply, in each of the successive series of reactors. Only minor changes occurred after subculturing from one batch series to the next one, highlighting the high stability of the established consortium. Different oxygen partial pressures (from 20% to 50%) were then tested in a 20-L continuous reactors pilot experiment. There was no impact on the community diversity, showing the high tolerance to oxygen of the bioleaching strains and their capacity to easily survive 50% oxygen input. The bioleaching efficiency in terms of rate and metal leaching did not seem to be changed. The use of enriched oxygen gas is not detrimental to the bioleaching strains and may be used in order to improve process operation (gas transfer, heat management...).

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