Functional potential of chitosan-metal nanostructures: Recent developments and applications.

Chitosan (Cs), a naturally occurring biopolymer, has garnered significant interest due to its inherent biocompatibility, biodegradability, and minimal toxicity. This study investigates the effectiveness of various reaction strategies, including acylation, acetylation, and carboxymethylation, to enhance the solubility profile of Cs. This review provides a detailed examination of the rapidly developing field of Cs-based metal complexes and nanoparticles. It delves into the diverse synthesis methodologies employed for their fabrication, specifically focusing on ionic gelation and in-situ reduction techniques. Furthermore, the review offers a comprehensive analysis of the characterization techniques utilized to elucidate the physicochemical properties of these complexes. A range of analytical techniques are utilized, including Ultraviolet-Visible Spectroscopy (UV-Vis), Fourier-Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM) and others. By comprehensively exploring a wide range of applications, the review emphasizes the significant potential of Cs in various scientific disciplines. Diagrams, figures, and tables effectively illustrate the synthesis processes, promoting a clear understanding for the reader. Chitosan-metal nanostructures/nanocomposites significantly enhance antimicrobial efficacy, drug delivery, and environmental remediation compared to standard chitosan composites. The integration of metal nanoparticles, such as silver or gold, improves chitosan's effectiveness against a range of pathogens, including resistant bacteria. These nanocomposites facilitate targeted drug delivery and controlled release, boosting therapeutic bioavailability. Additionally, they enhance chitosan's ability to absorb heavy metals and dyes from wastewater, making them effective for environmental applications. Overall, chitosan-metal nanocomposites leverage chitosan's biocompatibility while offering improved functionalities, making them promising materials for diverse applications. This paper sheds light on recent advancements in the applications of Cs metal complexes for various purposes, including cancer treatment, drug delivery enhancement, and the prevention of bacterial and fungal infections.

Synthesis, Carbonic Anhydrase II/IX/XII Inhibition, DFT, and Molecular Docking Studies of Hydrazide-Sulfonamide Hybrids of 4-Methylsalicyl- and Acyl-Substituted Hydrazide.

Carbonic anhydrases (CAs and EC 4.2.1.1) are the Zn2+ containing enzymes which catalyze the reversible hydration of CO2 to carbonate and proton. If they are not functioning properly, it would lead towards many diseases including tumor. Synthesis of hydrazide-sulfonamide hybrids (19-36) was carried out by the reaction of aryl (10-11) and acyl (12-13) hydrazides with substituted sulfonyl chloride (14-18). Final product formation was confirmed by FT-IR, NMR, and EI-MS. Density functional theory (DFT) calculations were performed on all the synthesized compounds to get the ground-state geometries and compute NMR properties. NMR computations were in excellent agreement with the experimental NMR data. All the synthesized hydrazide-sulfonamide hybrids were in vitro evaluated against CA II, CA IX, and CA XII isozymes for their carbonic anhydrase inhibition activities. Among the entire series, only compounds 22, 32, and 36 were highly selective inhibitors of hCA IX and did not inhibit hCA XII. To investigate the binding affinity of these compounds, molecular docking studies of compounds 32 and 36 were carried out against both hCA IX and hCA XII. By using BioSolveIT's SeeSAR software, further studies to provide visual clues to binding affinity indicate that the structural elements that are responsible for this were also studied. The binding of these compounds with hCA IX was highly favorable (as expected) and in agreement with the experimental data.

Synthesis, antimicrobial, antioxidant, cytotoxic, antiurease and molecular docking studies of N-(3-trifluoromethyl)benzoyl-N'-aryl thiourea derivatives.

An irrefutable advancement has been noted for the infectious diseases caused due to ureolytic bacteria through the development of various drugs. Keeping in mind the extremely valuable synthetic utility and medicinal significance of thiourea derivatives, synthesis of new 3-trifluoromethyl benzoic acid thiourea derivatives (3a-j) were carried out. The biological potential of all compounds in terms of antimicrobial, antioxidant, cytotoxic and antiurease activities were studied. The compounds 3a, 3c and 3i with dichloro and methoxy groups substitution on the aryl group showed significant activity against all strain of bacteria while moderate to no activity was observed in remaining compounds. Whereas the antifungal evaluation showed that all compounds were active againts C. Albican and no activity was observed against C. Prapsilosis. The cytotoxic findings revealed the non-toxic nature of these compounds as IC50 values of majority of the compounds are above 100 µm except for compounds 3f and 3g. In addition, these compounds exhibited better antioxidant potential as 100 µm concentration inhibited >50% reactive oxygen species (ROS) production except compounds 3e, 3f and 3j. The compound 3a proved to be the most potent urease inhibitor showing the highest enzyme % inhibition (93.1%) with IC50 value of 8.17 ±â€¯0.24 µM and found more active as compare to standard followed by compound 3e (92.6%), 3h (91.6%), 3d (90.8%), 3b (90.6%) and 3f (90.0%) with their respective IC50 values. All the synthesized compounds were docked into the binding cavity of Urease (PDB ID: 4ubp). The most active compound 3a was also ranked as top on the docking score as it was found to show valuable interactions with the target protein along with good docking scores. Hence our results revealed that the synthesized compounds have potential to be used as potent urease inhibitors after further detailed mechanistic studies.

Honokiol: An anticancer lignan.

BACKGROUND: Honokiol ((3',5-di-(2-propenyl)-1,1'-biphenyl-2,2'-diol), a lignan, is a promising antitumor compound, having exerted activity against a number of human cancer cell lines. Honokiol has inhibitory role on the proliferation, invasion and survival of cancer cells in in vitro as well as in vivo studies. It interferes with signaling pathways components in order to elicit the anticancer effect. SCOPE AND APPROACH: In present review, the published data on the efficacy of honokiol against various cancer cell lines and tumor-bearing animal models has been presented and discussed. KEY FINDINGS AND CONCLUSIONS: Honokiol lowers the expression of pluripotency-factors, the formation of mammosphere, P-glycoprotein expression, receptor CXCR4 level, c-FLIP, steroid receptor coactivator-3 (SRC-3), Twist1, matrix metalloproteinases, class I histone deacetylases, H3K27 methyltransferase among numerous other anticancer functions. It increases bone morphogenetic protein 7 (BMP7), Bax protein, among others. It does so by interfering with the major checkpoints such as nuclear factor kappa B (NF-κB), and activator of transcription 3 (STAT3), mammalian target of rapamycin (m-TOR), epidermal growth factor receptor (EGFR), Sonic hedgehog (SHH). It promotes the efficacy of several anticancer drugs and radiation tolerance. The derivatization of honokiol results in compounds with interesting attributes in terms of cancer control. This review will shed light on the scopes and hurdles in the relevance of the bioactive lignan honokiol in cancer management.

Gastrointestinal Motility and Acute Toxicity of Pistagremic Acid Isolated from the Galls of Pistacia integerrima.

BACKGROUND: Pistacia integerrima has many medicinal uses in therapeutic as well as folk medicine. P. integerrima has been used for the treatment of different ailments such as blood purifier, anti-inflammatory, and as remedy for gastrointestinal disorders such as vomiting and diarrhea, expectorant, cough, asthma and fever. OBJECTIVE: The main objective of this research work was to evaluate the effect of pistagremic acid (PA) isolated from the galls of Pistacia integerima in acute toxicity and gastrointestinal (GIT) motility tests. METHODS: Compound 1 namely pistagremic acid (PA) (at 10, 50, 100 mg/kg i.p) were assessed for their in-vivo gastrointestinal motility test using charcoal screening model. RESULTS: Results revealed that pretreatment of PA exhibited substantial safety in acute toxicity test up to the dose of 500 mg/kg p.o. However, when studied in charcoal meal GI transit test, PA caused significant (p < 0.05) attenuation of GIT motility and an increase in intestinal transit time, comparable to atropine (a muscarinic receptor blocking agent). CONCLUSION: In conclusion, PA displayed a strong dose-dependent reduction in GIT motility with considerable safety.

PHARMACOLOGICAL ASSESSMENT OF HISPIDULIN - A NATURAL BIOACTIVE FLAVONE.

Hispidulin is well-known natural bioactive flavone on behalf of its pharmacological aspects. This review contains data on isolation, synthetic methodology, pharmacokinetics and bioactivities of hispidulin. The article provides a critical assessment of present knowledge about hispidulin with some clear conclusions, perspectives and directions for future research in potential applications.

Inhibitory mechanism against oxidative stress of caffeic acid.

The purpose of this article is to summarize the reported antioxidant activities of a naturally abundant bioactive phenolic acid, caffeic acid (CA, 3,4-dihydroxycinnamic acid), so that new avenues for future research involving CA can be explored. CA is abundantly found in coffee, fruits, vegetables, oils, and tea. CA is among the most potential and abundantly found in nature, hydroxycinnamic acids with the potential of antioxidant behavior. Reactive oxygen species produced as a result of endogenous processes can lead to pathophysiological disturbances in the human body. Foods containing phenolic substances are a potential source for free radical scavenging; these chemicals are known as antioxidants. This review is focused on CA's structure, availability, and potential as an antioxidant along with its mode of action. A brief overview of the literature published about the prooxidant potential of caffeic acid as well as the future perspectives of caffeic acid research is described. CA can be effectively employed as a natural antioxidant in various food products such as oils.

CHLOROGENIC ACID: A PHARMACOLOGICALLY POTENT MOLECULE.

Chlorogenic acid (CGA; (IS,3R,4R.5R)-3-{[(2Z)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy}-1,4,5-trihydroxycyclohexanecarboxylic acid) is a naturally occurring polyphenol mostly present in vegetables and fruits. CGA is a prominent component of Traditional Chinese Medicines and is known for various pharmacological activities such as antioxidant, antimicrobial, anti-inflammatory and hepatoprotective etc. This mini-review is an attempt to summarize the available literature in the last decade and to point out future perspectives in this area of research.

PHARMACOLOGICAL ASSESSMENT OF HISPIDULIN--A NATURAL BIOACTIVE FLAVONE.

Hispidulin is well-known natural bioactive flavone on behalf of its pharmacological aspects. This review contains data on isolation, synthetic methodology, pharmacokinetics and bioactivities of hispidulin. The article provides a critical assessment of present knowledge about hispidulin with some clear conclusions, perspectives and directions for future research in potential applications.

Recent pharmacological advancements in schiff bases: a review.

Schiff bases are the biologically privileged scaffolds in organic chemistry, commonly synthesized from the condensation reaction of carbonyl functional group with amines. Naturally occurring and synthetically prepared Schiff bases are active molecules with many pharmacological activities like antibacterial, anti-cancer, anti-fungal, anti-malarial, antioxidant and many more. This review article summarizes pharmacological developments in the recent few years and gives a brief overview of their therapeutic potential.

Pharmacological importance of an ethnobotanical plant: Capsicum annuum L.

Capsicum annuum L., a fruit plant from tropical and subtropical regions, contains a range of essential nutrients and bioactive compounds which are known to exhibit a range of bioactivities including free radical scavenging (antioxidant), antimicrobial, antiviral, anti-inflammatory and anticancer. This review aims to give a comprehensive overview of the literature published on pharmacological behaviours of C. annuum L.

Recent pharmacological developments in ß-carboline alkaloid "harmaline".

Peganum harmala (L) is a perennial plant which is native of eastern Iranian and west of India but also found in different regions of western USA. A number of ß-carboline compounds with therapeutic importance and different pharmacological effects, are present in this plant. Among other alkaloids, such as, harmine, harmalol and vasicine, isolated from various parts of the plant, harmaline is considered as most valuable with reference to its medicinal importance. Harmaline has been extensively studied in last decade and known to exert multiple pharmacological effects including antileishmanial, antimicrobial, antiplatelet, antiplasmodial, antitumoral, hypothermic and vasorelaxant activity. The proposed work is intended to highlight the recent pharmacological aspects of ß-carboline alkaloid "harmaline".