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1.
Molecules ; 27(23)2022 Nov 29.
Article in English | MEDLINE | ID: mdl-36500409

ABSTRACT

Traditional remedies for the treatment of various ailments are gaining popularity. Traditionally, one of the most valuable therapeutic herbs has been Picrorhiza kurroa Royle ex Benth. Traditional and folk uses of P. kurroa include chronic constipation, skin-related problems, burning sensation, chronic reoccurring fever, jaundice, heart problems, breathing, digestion, allergy, tuberculosis, blood-related problems, prediabetes and obesity, laxative, cholagogue, and liver stimulatory. Phytoconstituents such as glycosides, alkaloids, cucurbitacins, iridoids, phenolics, and terpenes in P. kurroa have shown promising pharmacological potential. In order to uncover novel compounds that may cure chronic illnesses, such as cardiovascular, diabetes, cancer, respiratory, and hepatoprotective diseases, the screening of P. kurroa is essential. This study comprehensively evaluated the ethnopharmacological efficacy, phytochemistry, pharmacological activity, dose, and toxicity of P. kurroa. This review provides comprehensive insights into this traditional medication for future research and therapeutic application. The purpose of this review article was to determine the pharmacological effects of P. kurroa on a variety of disorders. P. kurroa may be a natural alternative to the standard treatment for eradicating newly evolving diseases. This study is intended as a resource for future fundamental and clinical investigations.


Subject(s)
Picrorhiza , Picrorhiza/chemistry , Cinnamates/chemistry , Glycosides , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Plant Extracts/chemistry , Treatment Outcome
2.
Saudi Pharm J ; 30(7): 954-963, 2022 Jul.
Article in English | MEDLINE | ID: mdl-35903527

ABSTRACT

Background: The continuing expansion of the pharmacist's role necessitates continuous evaluation of current practice to identify strategies for improvements. The International Pharmaceutical Federation (FIP) has developed tools to support stakeholders in identifying development needs and planning advancement strategies. The aim of this research was to utilise the FIP Global Competency Framework, version 2 (GbCF v2), and FIP Development Goals (DGs) to evaluate competencies related to pharmacy practice in Saudi Arabia, and to understand the strategies needed to develop and improve the current practice. Methods: The study involved four phases. Phase 1 involved translation of the FIP GbCF v2 into the Arabic language. Phase 2 was a consensus panel validation to establish the initial relevance of the competencies to current practice. Phase 3 included a national survey distributed to all registered pharmacists in Saudi Arabia. The final phase was conducted through mapping 'not relevant' competencies to FIP DGs to identify priorities. Results: The translation phase yielded a bilingual framework that could be utilized by pharmacists in Saudi Arabia. The initial validation phase identified 61 behavioral statements (from 124 in the GbCF v2) as 'highly relevant' or 'relevant' to pharmacy practice. Findings from the national survey identified a list of 'not relevant' competencies that could highlight gaps in current practice. The final mapping phase generated a list of three FIP DG priorities: DG5 (competency development), DG8 (working with others) and DG11 (impact and outcomes). Conclusion: The study indicated that competencies in the GbCF v2 were relevant to pharmacists practicing in the country. However, some competencies were perceived as 'not relevant' to current practice and these highlighted gaps in the current practice that need attention. Mapping 'not relevant' competencies to FIP DGs should be used as a starting point towards developing strategies, systems, and protocols to advance pharmacy practice in Saudi Arabia.

3.
Bioorg Med Chem Lett ; 44: 128117, 2021 07 15.
Article in English | MEDLINE | ID: mdl-34015500

ABSTRACT

One of the major challenges in the community and healthcare was an impedance of pathogenic bacteria to antibiotics. This work developed 2-aminothiophene derivatives as novel antimicrobial agents. Various 2-aminothiophene derivatives (3a-f, 5a-c, 6a, b, 7, 8a, b and 9) with cyclic and heterocyclic moieties at 5-position were synthesized, and characterized using NMR, IR, and mass spectroscopic techniques. The newly synthesized compounds were evaluated for their antimicrobial activity against bacteria S. pneumoniae, B. subtilis, P. aeruginosa, E. coli, and fungi A. fumigatus, S. mracemosum, G. candidum, C. albicans. Compound 3a with OH group at para position of phenyl ring exhibited significant antibacterial activity stronger than that of the drug standards Ampicillin and Gentamicin. Compound 6b possess pyrazole ring and compound 9 bearing pyridine ring showed promising antifungal activity compare to the standard drug Amphotericin B. The remaining compounds exhibited good to moderate inhibitory activities. In summary, the results suggest that the compounds from 2-aminothiophene derivatives can be used as antimicrobial agents.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Bacteria/drug effects , Drug Design , Fungi/drug effects , Thiophenes/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Dose-Response Relationship, Drug , Microbial Sensitivity Tests , Molecular Structure , Structure-Activity Relationship , Thiophenes/chemical synthesis , Thiophenes/chemistry
4.
Molecules ; 26(13)2021 Jul 05.
Article in English | MEDLINE | ID: mdl-34279434

ABSTRACT

Respiratory tract infections are underestimated, as they are mild and generally not incapacitating. In clinical medicine, however, these infections are considered a prevalent problem. By 2030, the third most comprehensive reason for death worldwide will be chronic obstructive pulmonary disease (COPD), according to the World Health Organization. The current arsenal of anti-inflammatory drugs shows little or no benefits against COPD. For thousands of years, herbal drugs have been used to cure numerous illnesses; they exhibit promising results and enhance physical performance. Ginseng is one such herbal medicine, known to alleviate pro-inflammatory chemokines and cytokines (IL-2, IL-4, IFN-γ, TNF-α, IL-5, IL-6, IL-8) formed by macrophages and epithelial cells. Furthermore, the mechanisms of action of ginsenoside are still not fully understood. Various clinical trials of ginseng have exhibited a reduction of repeated colds and the flu. In this review, ginseng's structural features, the pathogenicity of microbial infections, and the immunomodulatory, antiviral, and anti-bacterial effects of ginseng were discussed. The focus was on the latest animal studies and human clinical trials that corroborate ginseng's role as a therapy for treating respiratory tract infections. The article concluded with future directions and significant challenges. This review would be a valuable addition to the knowledge base for researchers in understanding the promising role of ginseng in treating respiratory tract infections. Further analysis needs to be re-focused on clinical trials to study ginseng's efficacy and safety in treating pathogenic infections and in determining ginseng-drug interactions.


Subject(s)
Ginsenosides/pharmacology , Panax/chemistry , Phytotherapy/methods , Respiratory Tract Infections/drug therapy , Animals , Complementary Therapies , Humans
5.
Molecules ; 26(17)2021 Sep 04.
Article in English | MEDLINE | ID: mdl-34500816

ABSTRACT

The pharmacological activities of thiazole and pyrazole moieties as antimicrobial and anticancer agents have been thoroughly described in many literature reviews. In this study, a convenient synthesis of novel pyrazolo[5,1-b]thiazole-based heterocycles was carried out. The synthesized compounds were characterized by IR, 1H and 13C NMR spectroscopy and mass spectrometry. Some selected examples were screened and evaluated for their antimicrobial and anticancer activities and showed promising results. These products could serve as leading compounds in the future design of new drug molecules.


Subject(s)
Anti-Bacterial Agents/chemical synthesis , Antineoplastic Agents/chemical synthesis , Anti-Bacterial Agents/toxicity , Antineoplastic Agents/toxicity , HCT116 Cells , Hep G2 Cells , Humans , Pyrazoles/chemistry , Thiazoles/chemistry
6.
Molecules ; 25(24)2020 Dec 11.
Article in English | MEDLINE | ID: mdl-33322431

ABSTRACT

Diabetes is a major health problem that is associated with high risk of various complications. Medicinal plants hold great promise against diabetes. The traditional use of Cleome droserifolia as an antidiabetic agent was correlated to its flavonol glycosides content. In the current study, five major flavonol glycosides appeared on the RP-HPLC chromatogram of the aqueous extract namely; quercetin-3-O-ß-d-glucosyl-7-O-α-rhamnoside (1), isorhamnetin-7-O-ß-neohesperidoside (2), isorhamnetin-3-O-ß-d-glucoside (3) kaempferol-4'-methoxy-3,7-O-α-dirhamnoside (4), and isorhamnetin-3-O-α-(4″-acetylrhamnoside)-7-O-α-rhamnoside (5). The inhibitory activities of these compounds were tested in vitro against several enzymes involved in diabetes management. Only the relatively less polar methoxylated flavonol glycosides (4, 5) showed mild to moderate α-amylase and α-glucosidase inhibitory activities. Compounds 1-4 displayed remarkable inhibition of dipeptidyl peptidase IV (DPPIV) enzyme (IC50 0.194 ± 0.06, 0.573 ± 0.03, 0.345 ± 0.02 and 0.281 ± 0.05 µg/mL, respectively) comparable to vildagliptin (IC50 0.154 ± 0.02 µg/mL). Moreover, these compounds showed high potential in preventing diabetes complications through inhibiting aldose reductase enzyme and combating oxidative stress. Both isorhamnetin glycoside derivatives (2, 3) exhibited the highest activities in aldose reductase inhibition and compound 2 (IC50 5.45 ± 0.26 µg/mL) was even more potent than standard quercetin (IC50 7.77 ± 0.43 µg/mL). Additionally, these flavonols exerted excellent antioxidant capacities through 2, 2-diphenyl-1-picrylhydrazil (DPPH) and ferric reducing antioxidant (FRAP) assays.


Subject(s)
Dipeptidyl Peptidase 4/chemistry , Dipeptidyl-Peptidase IV Inhibitors/chemistry , Glycosides/pharmacology , Aldehyde Reductase/chemistry , Aldehyde Reductase/metabolism , Antioxidants/chemistry , Biphenyl Compounds/chemistry , Chemistry, Pharmaceutical/methods , Chromatography, High Pressure Liquid , Cleome , Drug Design , Free Radical Scavengers , Humans , Hypoglycemic Agents , In Vitro Techniques , Inhibitory Concentration 50 , Magnetic Resonance Spectroscopy , Models, Chemical , Oxidative Stress , Picrates/chemistry , Vildagliptin/pharmacology , alpha-Amylases/chemistry , alpha-Glucosidases/metabolism
7.
Molecules ; 25(2)2020 01 20.
Article in English | MEDLINE | ID: mdl-31968561

ABSTRACT

Kleinia pendula (Forssk.) DC. is a prostrate or pendent dark green succulent herb found in the southwestern mountain regions of Saudi Arabia. The literature survey of the plant reveals a lack of phytochemical and pharmacological studies, although traditional uses have been noted. The objective of the present work was to assess the in vivo analgesic and anti-inflammatory activities, as well as, the in vitro cytotoxic potential of the fractions of Kleinia pendula, and correlate these activities to the plant metabolites. The methanolic extract of Kleinia pendula was subjected to fractionation with n-hexane, ethyl acetate, chloroform, n-butanol, and water. The fractions were screened for their analgesic and anti-inflammatory activities, as well as cytotoxic activity against breast, liver, and colon cancer cell lines. The n-hexane and chloroform fractions of Kleinia pendula showed significant cytotoxic activity against all three cancer cell lines tested. The ethyl acetate and chloroform fractions showed significant analgesic and anti-inflammatory activities. The metabolites in these three active fractions were determined using UPLC-PDA-ESI-MS. Thus, the analgesic and anti-inflammatory activities of the plant were attributed to its phenolic acids (caffeoylquinic acid derivatives, protocatechuic, and chlorogenic acids). While fatty acids and triterpenoids such as (tormentic acid) in the hexane fraction are responsible for the cytotoxic activity; thus, these fractions of Kleinia pendula may be a novel source for the development of new plant-based analgesic, anti-inflammatory, and anticancer drugs.


Subject(s)
Analgesics/pharmacology , Anti-Inflammatory Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Fabaceae/chemistry , Phytochemicals/pharmacology , Analgesics/chemistry , Anti-Inflammatory Agents/chemistry , Antineoplastic Agents, Phytogenic/chemistry , Cell Proliferation/drug effects , Cell Survival/drug effects , Chromatography, High Pressure Liquid , HCT116 Cells , Hep G2 Cells , Humans , MCF-7 Cells , Mass Spectrometry , Phytochemicals/chemistry , Plant Extracts/chemistry , Saudi Arabia , Senecio
8.
Pharmacol Res ; 146: 104314, 2019 08.
Article in English | MEDLINE | ID: mdl-31229564

ABSTRACT

Epithelial-to-mesenchymal transition (EMT) is an orchestrated event where epithelial cells progressively undergo biochemical changes and transition into mesenchymal-like cells by gradually losing their epithelial characteristics. EMT plays a crucial pathologic role in renal abnormalities, especially renal fibrosis. A number of bench studies suggest the potential involvement of renin-angiotensin-aldosterone system (RAAS) in renal EMT process and associated renal abnormalities. EMT appears to be an important pathologic mechanism for the deleterious renal effects of angiotensin II and aldosterone, the two major RAAS components. Mechanistically, the renal RAAS-TGF-ß-Smad3 signalling pathway plays an important pathologic role in EMT-associated renal abnormalities. Intriguingly, the RAAS antagonists such as losartan, telmisartan, eplerenone, and spironolactone have the potential to prevent renal EMT in bench studies. This review describes the key mechanistic role of RAAS overactivation in EMT-induced renal abnormalities. Moreover, drugs interrupting the RAAS at different levels in the cascade ameliorating the EMT-associated renal abnormalities are described.


Subject(s)
Aldosterone/metabolism , Epithelial-Mesenchymal Transition/physiology , Kidney Diseases/metabolism , Kidney Diseases/physiopathology , Renin-Angiotensin System/physiology , Animals , Epithelial Cells/metabolism , Epithelial Cells/physiology , Humans , Signal Transduction/physiology
9.
Pharmacol Res ; 144: 132-141, 2019 06.
Article in English | MEDLINE | ID: mdl-30970278

ABSTRACT

The activation of peroxisome proliferator-activated receptor α (PPARα) is a key pharmacological drug target for dyslipidemic management. Dyslipidemia is associated with abnormal serum lipid profiles viz. elevated total cholesterol, high triglyceride, elevated low-density lipoprotein cholesterol, and reduced high-density lipoprotein cholesterol levels. Fenofibrate, a third-generation fibric acid derivative, is an activator of PPARα indicated for the treatment of mixed dyslipidemia and hypertriglyceridemia in adults. Fenofibrate is considered an important lipid-lowering medication employed in patients afflicted with atherogenic dyslipidemia. Intriguingly, recent bench studies have demonstrated an array of cardiovascular and renal pleiotropic beneficial activities of fenofibrate, besides its foremost lipid-lowering action. The activation of PPARα by fenofibrate could negatively regulate the cardiomyocyte hypertrophy. In addition, fenofibrate has been suggested to have a protective effect against experimental ischemia/reperfusion injury in the myocardium in part via endoplasmic reticulum stress inhibition. Fenofibrate has also been shown to suppress arrhythmias in isolated rat hearts subjected to ischemic/reperfusion-induced cardiac injury. Moreover, in a rat model of metabolic syndrome and myocardial ischemia, fenofibrate therapy has been shown to restore antioxidant protection and improve myocardial insulin resistance. Furthermore, studies have highlighted the pleiotropic vascular endothelial protective and antihypertensive actions of fenofibrate. Interestingly, recent bench studies have demonstrated renoprotective actions of fenofibrate by implicating diverse mechanisms. This review sheds light on the current perspectives and molecular mechanistic aspects pertaining to the cardiovascular pleiotropic actions of fenofibrate. Additionally, the renal pleiotropic actions of fenofibrate by focusing its possible modulatory role on renal fibrosis, inflammation and renal epithelial-to-mesenchymal transition have been enlightened.


Subject(s)
Fenofibrate/therapeutic use , Hypolipidemic Agents/therapeutic use , Animals , Cardiovascular Diseases/drug therapy , Cardiovascular Diseases/metabolism , Dyslipidemias/drug therapy , Dyslipidemias/metabolism , Fenofibrate/pharmacology , Humans , Hypolipidemic Agents/pharmacology , Kidney Diseases/drug therapy , Kidney Diseases/metabolism , Molecular Targeted Therapy
10.
Mar Drugs ; 17(8)2019 Aug 09.
Article in English | MEDLINE | ID: mdl-31395834

ABSTRACT

In the present study, LC-HRESIMS-assisted dereplication along with bioactivity-guided isolation led to targeting two brominated oxindole alkaloids (compounds 1 and 2) which probably play a key role in the previously reported antibacterial, antibiofilm, and cytotoxicity of Callyspongia siphonella crude extracts. Both metabolites showed potent antibacterial activity against Gram-positive bacteria, Staphylococcus aureus (minimum inhibitory concentration (MIC) = 8 and 4 µg/mL) and Bacillus subtilis (MIC = 16 and 4 µg/mL), respectively. Furthermore, they displayed moderate biofilm inhibitory activity in Pseudomonas aeruginosa (49.32% and 41.76% inhibition, respectively), and moderate in vitro antitrypanosomal activity (13.47 and 10.27 µM, respectively). In addition, they revealed a strong cytotoxic effect toward different human cancer cell lines, supposedly through induction of necrosis. This study sheds light on the possible role of these metabolites (compounds 1 and 2) in keeping fouling organisms away from the sponge outer surface, and the possible applications of these defensive molecules in the development of new anti-infective agents.


Subject(s)
Alkaloids/pharmacology , Callyspongia/chemistry , Oxindoles/pharmacology , Animals , Anti-Infective Agents/pharmacology , Antiprotozoal Agents/pharmacology , Bacteria/drug effects , Biofilms/drug effects , Cell Line, Tumor , HT29 Cells , Halogenation , Humans , Indian Ocean , Microbial Sensitivity Tests/methods
11.
Int J Health Plann Manage ; 34(1): e583-e593, 2019 Jan.
Article in English | MEDLINE | ID: mdl-30265404

ABSTRACT

BACKGROUND: Saudi Arabia has shown rapid growth in its pharmacy workforce and pharmacy education over the last decade. The health indicators demonstrate an increased need for medications and, thus, the accessibility of pharmacies. Since pharmacists are considered the most accessible health care professionals, the country has experienced a continuous demand to produce more pharmacists. OBJECTIVES: The objectives of the study are to evaluate the pharmacy workforce in Saudi Arabia and to identify pharmaceutical manpower issues. METHODS: A retrospective cross-sectional approach was used. Data were obtained from the latest version of the Health Statistical Yearbook-Kingdom of Saudi Arabia, 2016; Saudi Commission for Health Specialties publications, 2018. RESULTS: In general, the exponential increase in the number of pharmacy schools has produced more pharmacists in the rural areas of the country, but inequitable distribution of the workforce still exists. The reliance on nonindigenous pharmacists, especially in the private sector, is substantial. Employed male pharmacists outnumber females, mainly due to the cultural and social factors that limit the participation of women in community pharmacy, which is the largest employment sector. The employment rate shows limited opportunities for Saudi pharmacists at MOH, as they have already Saudised almost all pharmacy positions at their health care facilities. However, the private sector needs to assume responsibility for their share of the renationalisation of the profession in order to provide jobs for local pharmacists. CONCLUSIONS: Regular, more detailed profiling of the pharmacy workforce is an essential step to achieving effective pharmacy workforce planning. Currently, a large gap exists in our knowledge of the country's workforce.


Subject(s)
Health Workforce , Pharmacies , Cross-Sectional Studies , Databases, Factual , Health Workforce/statistics & numerical data , Humans , Retrospective Studies , Saudi Arabia
12.
Molecules ; 24(9)2019 Apr 26.
Article in English | MEDLINE | ID: mdl-31035531

ABSTRACT

A series of new thiazoline derivatives were synthesized. Structure analyses were accomplished employing 1H-NMR, 13C-NMR, X-ray and MS techniques. The in vitro antitumor activities were assessed against human hepatocellular carcinoma (HepG-2) and colorectal carcinoma (HCT-116) cell lines. The results revealed that the thiazolines 5b and 2c exhibited significant activity against the two cell lines. The in vitro antimicrobial screening showed that the thiazolines 2c, 5b and 5d showed promising inhibition activity against Salmonella sp. Additionally, the inhibition activity of thiazolines 2e and 5b against Escherichia coli was comparable to that of the reference compound gentamycin.


Subject(s)
Chemistry Techniques, Synthetic , Molecular Docking Simulation , Organic Chemicals/chemistry , Organic Chemicals/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cell Survival/drug effects , Dose-Response Relationship, Drug , Humans , Hydrogen Bonding , Molecular Structure , Organic Chemicals/chemical synthesis , Spectrum Analysis , Structure-Activity Relationship
13.
Molecules ; 24(18)2019 Sep 06.
Article in English | MEDLINE | ID: mdl-31500095

ABSTRACT

Twelve new Schiff base derivatives have been prepared by the condensation reaction of different amino substituted compounds (aniline, pyridin-2-amine, o-toluidine, 2-nitrobenzenamine, 4-aminophenol, and 3-aminopropanol) and substituted aldehydes such as nicotinaldehyde, o,m,p-nitrobenzaldehyde, and picolinaldehyde in ethanol using acetic acid as a catalyst. The envisaged structures of the all the synthesized ligands have been confirmed on the basis of their spectral analysis FT-IR, mass spectroscopy, 1H- and 13C-NMR. In vitro screening of their antibacterial and antifungal potential against Escherichia coli bacterium and Fusarium oxysporum f.sp albedinis (F.o.a) fungus, respectively, revealed that all the ligands showed no significant antibacterial activity, whereas most of them displayed good antifungal activity. Homology modeling and docking analysis were performed to explain the antifungal effect of the most and least active compound against two F.o.a fungus proteins.


Subject(s)
Anti-Bacterial Agents/chemistry , Coordination Complexes/chemistry , Escherichia coli/drug effects , Fusarium/drug effects , Aminophenols/chemistry , Aniline Compounds/chemistry , Anti-Bacterial Agents/pharmacology , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Escherichia coli/pathogenicity , Fusarium/pathogenicity , Humans , Ligands , Microbial Sensitivity Tests , Molecular Docking Simulation , Molecular Structure , Schiff Bases/chemistry
14.
BMC Complement Altern Med ; 18(1): 274, 2018 Oct 09.
Article in English | MEDLINE | ID: mdl-30301463

ABSTRACT

BACKGROUND: Cucumis prophetarum var. prophetarum is used in Saudi folk medicine for treating liver disorders and grows widely between Abha and Khamis Mushait City, Saudi Arabia. METHODS: Bioassay-guided fractionation and purification were used to isolate the main active constituents of Cucumis prophetarum var. prophetarum fruits. These compounds were structurally elucidated using NMR spectroscopy, mass spectral analyses and x-ray crystallography. All fractions, sub-fractions and pure compounds were screened for their anticancer activity against six cancer cell lines. RESULTS: The greatest cytotoxic activity was found to be in the ethyl acetate fraction, resulting in the isolation of five cucurbitacin compounds [E, B, D, F-25 acetate and Hexanorcucurbitacin D]. Among the cucurbitacins that were isolated and tested cucurbitacin B and E showed potent cytotoxicity activities against all six human cancer cell lines. CONCLUSION: Human breast cancer cell lines were found to be the most sensitive to cucurbitacins. Preliminary structure activity relationship (SAR) for cytotoxic activity of Cucurbitacins against human breast cancer cell line MDA-MB-231 has been reported.


Subject(s)
Antineoplastic Agents, Phytogenic/isolation & purification , Cucumis/chemistry , Cucurbitacins/isolation & purification , Plant Extracts/chemistry , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Biological Assay/methods , Cell Line, Tumor , Chemical Fractionation/methods , Cucurbitacins/chemistry , Cucurbitacins/pharmacology , Humans
15.
Colloids Surf B Biointerfaces ; 234: 113728, 2024 Feb.
Article in English | MEDLINE | ID: mdl-38183872

ABSTRACT

Wounds are a physical manifestation of injury to the skin causing it to rupture or tear. The process of wound healing naturally restores skin integrity while minimizing the extent of the damage. Hesperidin (HPN) is a natural polyphenolic flavonoid and is effective in treating wounds due to its ability to reduce inflammation and stimulate angiogenesis. However, its use is limited by its poor physicochemical attributes such as poor solubility in water. Recently, nanoparticles, particularly Cubosomes, are found to be promising candidates for advancing wound-healing therapies, owing to their unique properties. The present study was conducted to develop a hydrogel system based on Cubosomes encapsulating HPN (HPN-Cubogel), with the potential to mitigate full-thickness wounds. The therapeutic efficacy of the formulation assessed in the animal model showed that the HPN-Cubogel formulation group exhibited a wound closure rate of 98.96 ± 1.50% after 14 days post-wounding compared to 89.12 ± 2.6% in the control group suggesting superior wound contraction activity. Collagen synthesis was superior in the formulation compared to the control group, as determined through MT staining. In summary, the HPN-Cubogel formulation was found to be the most effective in enhancing full-thickness wound healing.


Subject(s)
Hesperidin , Animals , Hesperidin/pharmacology , Wound Healing , Skin , Hydrogels/pharmacology , Hydrogels/chemistry , Models, Animal
16.
J Biomol Struct Dyn ; : 1-11, 2024 Mar 26.
Article in English | MEDLINE | ID: mdl-38529911

ABSTRACT

Hematopoietic cell kinase (HCK) has emerged as a potential target for therapeutic intervention in cancer and HIV infection because of its critical role in critical signaling pathways. Repurposing FDA-approved drugs offers an efficient strategy to identify new treatment options. Here, we address the need for novel therapies in cancer and HIV by investigating the potential of repurposed drugs against HCK. Our goal was to identify promising drug candidates with high binding affinities and specific interactions within the HCK binding pocket. We employed an integrated computational approach combining molecular docking and extensive molecular dynamics (MD) simulations. Initially, we analyzed the binding affinities and interaction patterns of a library of FDA-approved drugs sourced from DrugBank. After careful analysis, we focused on two compounds, Nilotinib and Radotinib, which exhibit exceptional binding affinities and specificity to the HCK binding pocket, including the active site. Additionally, we assessed the pharmacological properties of Nilotinib and Radotinib, making them attractive candidates for further drug development. Extensive all-atom MD simulations spanning 200 nanoseconds (ns) elucidated the conformational dynamics and stability of the HCK-Nilotinib and HCK-Radotinib complexes. These simulations demonstrate the robustness of these complexes over extended timescales. Our findings highlighted the potential of Nilotinib and Radotinib as promising candidates against HCK that offer valuable insights into their binding mechanisms. This computational approach provides a comprehensive understanding of drug interactions with HCK and sets the stage for future experimental validation and drug development endeavors.Communicated by Ramaswamy H. Sarma.

17.
Int J Pharm ; 656: 124099, 2024 May 10.
Article in English | MEDLINE | ID: mdl-38614431

ABSTRACT

Diabetic wounds (DWs) pose a significant health burden worldwide, with their management presenting numerous challenges. Biopolymeric formulations have recently gained attention as promising therapeutic approaches for diabetic wound healing. These formulations, composed of biocompatible and biodegradable polymers, offer unique properties such as controlled drug release, enhanced wound closure, and reduced scarring. In this review, we aim to provide a comprehensive overview of the current state of research and future prospects regarding the application of biopolymeric formulations for diabetic wound healing. The review begins by highlighting the underlying pathophysiology of DWs, including impaired angiogenesis, chronic inflammation, and compromised extracellular matrix (ECM) formation. It further explores the key characteristics of biopolymeric materials, such as their biocompatibility, biodegradability, and tunable physicochemical properties, which make them suitable for diabetic wound healing applications. The discussion further delves into the types of biopolymeric formulations utilized in the treatment of DWs. These include hydrogels, nanoparticles (NP), scaffolds, films, and dressings. Furthermore, the review addresses the challenges associated with biopolymeric formulations for diabetic wound healing. In conclusion, biopolymeric formulations present a promising avenue for diabetic wound healing. Their unique properties and versatility allow for tailored approaches to address the specific challenges associated with DWs. However, further research and developments are required to optimize their therapeutic efficacy, stability, manufacturing processes, and regulatory considerations. With continued advancements in biopolymeric formulations, the future holds great promise for improving the management and outcomes of DWs.


Subject(s)
Wound Healing , Wound Healing/drug effects , Humans , Biopolymers/chemistry , Biopolymers/administration & dosage , Animals , Diabetes Mellitus/drug therapy , Hydrogels/chemistry , Hydrogels/administration & dosage , Bandages , Biocompatible Materials/chemistry , Biocompatible Materials/administration & dosage , Nanoparticles/chemistry
18.
Int J Pharm ; 658: 124212, 2024 Jun 10.
Article in English | MEDLINE | ID: mdl-38723730

ABSTRACT

Liposomes are nanosized, spherical vesicles consisting of an aqueous core encircled by one or more phospholipid bilayer shells. Liposomes have found extensive use in numerous biomedicine and nanomedicine applications due to their excellent biocompatibility, adaptable chemical composition, ease of preparation, and diverse structural characteristics. These applications include nanocarriers for drug delivery, immunoassays, nutraceuticals, tissue engineering, clinical diagnostics, and theranostics formulations. These applications stimulated significant efforts toward scaling up formation processes in anticipation of appropriate industrial advancement. Despite the advancements in conventional methods and the emergence of new approaches for liposome production, their inherent susceptibility to chemical and mechanical influences contributes to critical challenges, including limited colloidal stability and decreased efficiency in encapsulating cargo molecules. With this context, the current review provides brief insights into liposomes conventional and novel industrial production techniques. With a special focus on the structural parameters, and pivotal elements influencing the synthesis of an appropriate and stable formulation, followed by the various regulatory aspects of industrial production.


Subject(s)
Liposomes , Humans , Drug Compounding/methods , Drug Delivery Systems/methods , Chemistry, Pharmaceutical/methods , Drug Industry/methods , Animals
19.
Int J Pharm ; 652: 123808, 2024 Mar 05.
Article in English | MEDLINE | ID: mdl-38224758

ABSTRACT

The malignancy of the prostate is a complicated ailment which impacts millions of male populations around the globe. Despite the multitude of endeavour accomplished within this domain, modalities that are involved in the ameliorative management of predisposed infirmity are still relent upon non-specific and invasive procedures, thus imposing a detrimental mark on the living standard of the individual. Also, the orchestrated therapeutic interventions are still incompetent in substantiating a robust and unabridged therapeutic end point owing to their inadequate solubility, low bioavailability, limited cell assimilation, and swift deterioration, thereby muffling the clinical application of these existing treatment modalities. Nanotechnology has been employed in an array of modalities for the medical management of malignancies. Among the assortment of available nano-scaffolds, nanocarriers composed of a bio-decomposable and hybrid polymeric material like PLGA hold an opportunity to advance as standard chemotherapeutic modalities. PLGA-based nanocarriers have the prospect to address the drawbacks associated with conventional cancer interventions, owing to their versatility, durability, nontoxic nature, and their ability to facilitate prolonged drug release. This review intends to describe the plethora of evidence-based studies performed to validate the applicability of PLGA nanosystem in the amelioration of prostate malignancies, in conjunction with PLGA focused nano-scaffold in the clinical management of prostate carcinoma. This review seeks to explore numerous evidence-based studies confirming the applicability of PLGA nanosystems in ameliorating prostate malignancies. It also delves into the role of PLGA-focused nano-scaffolds in the clinical management of prostate carcinoma, aiming to provide a comprehensive perspective on these advancements.


Subject(s)
Carcinoma , Prostatic Neoplasms , Male , Humans , Polylactic Acid-Polyglycolic Acid Copolymer , Prostatic Neoplasms/drug therapy , Polymers , Nanotechnology
20.
Heliyon ; 10(7): e29058, 2024 Apr 15.
Article in English | MEDLINE | ID: mdl-38623202

ABSTRACT

Anemia is a severe health issue that affects around one-third of the global population. Therefore, the present study aims to conduct a bibliometric analysis to investigate the research trends regarding advancements on iron formulations in treating iron deficiency anemia via oral or parenteral route. This study adopts thematic and bibliometric methods on existing research on novel iron formulations. It also provides perspective into the existing understanding on treatment strategies for iron deficiency anemia. This study is conducted on 543 papers on various ferrous and ferric formulations used in the treatment of iron deficiency anemia. The study period is from 1977 to 2022, and the papers are identified from the Scopus database. The bibliometric analysis was carried out using the R tool's Bibliometrix package. The study discusses performance analysis, including annual publications, geographic analysis, relevant affiliations, journal analysis, and citation analysis. In addition, the conceptual structure, including the co-occurrence network, thematic map, thematic evolution, intellectual structure highlighting co-citation analysis, and social structure depicting the collaboration network and collaboration world map, are presented. The results showed increased research on formulation strategies for the treatment of iron deficiency anemia from 2010 onwards. The top 5 contributing countries are the USA, Italy, India, Germany, and the UK, and peer-reviewed journals from the area of nutrition. The most trending areas of study are iron deficiency anemia in pregnancy, chronic kidney diseases, inflammatory bowel diseases, and various intravenous formulations used in its treatment. The authors from Europe collaborate the most with authors from other countries. The study concludes that a safer and more effective iron formulation is needed to reduce the prevalence of anemia. The findings of the study are helpful in advancing research on innovative formulations for treating iron deficiency anemia. The insights from the study are helpful to policymakers in designing specific health policies and investing more in research and development of novel formulations for the treatment of iron deficiency anemia.

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