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1.
J Family Med Prim Care ; 13(2): 699-703, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38605779

RESUMEN

Background: Approximately 15% of migraine sufferers need preventative medicine because they have more than two episodes each month. Migraine is a regular, persistent condition that frequently makes victims helpless. Numerous drugs from various classes have so far been used in migraine prophylaxis. Their effectiveness is recurrently overshadowed by their side effects because they must be used for a long time, which occasionally necessitates stopping the drug. Materials and Methods: In the tertiary care teaching hospital's department of medicine, a prospective, comparative, open-label study was initiated. Two groups of 80 patients were randomly chosen. For 3 months, the 40 patients in Group A were given a tablet of amitriptyline 10 mg once daily, whereas the 40 patients in Group B were given a tablet of propranolol 20 mg once a day. At the conclusion of the fourth, eighth, and twelfth weeks, the patients' own self-assessment migraine diary and a 4-point pain scale were used to grade the intensity of the headaches. Results: As a result, in Group A, the mean migraine attack severity in periods 1 and 2 was 5.88 2.69 and 5.41 2.48, respectively. In Group B, the mean was 5.15 2.75 in period 1 and 5.66 2.78 in period 2, respectively. The average length of a migraine attack in Group A was 20.30 5.61 h in period 1 and 16.75 5.23 h in period 2. In Group B, the mean was 16.59 3.21 in period 1 and 18.78 5.14 in period 2. Between groups A and B, there was a statistically significant difference. Conclusion: The average number of migraine attacks reduced in the amitriptyline and propranolol groups as the treatment duration increased. Amitriptyline is a popular medication with established effectiveness and manageable levels of negative side effects. It is the tricyclic antidepressant that is most frequently used to prevent headaches. When administered for migraine prevention, it generates a quick response within 3 months. Propranolol is less effective than amitriptyline at reducing the frequency, length, and severity of episodes.

4.
ACS Omega ; 8(50): 48145-48158, 2023 Dec 19.
Artículo en Inglés | MEDLINE | ID: mdl-38144139

RESUMEN

Amphiphilic micelles based on chitosan (CS) were applied as drug carriers of aceclofenac (ACF) as a potential method to induce its bioavailability and therapeutic efficiency. N-octyl-N,O-succinyl CS (OSCS), an amphiphilic CS derivative, was successfully synthesized and loaded physically by ACF at different pH values and using different dosages of ACF, forming ACF-loaded polymeric micelles (PMs). The obtained PMs and ACF-loaded PMs were characterized by different analytical techniques, including AFM, TEM, DLS, UV-vis spectrophotometry, 1H NMR spectroscopy, and FT-IR spectroscopy. The pH 5 sample with a 30% ACF/polymer ratio showed the highest ACF loading capacity (LC) and entrapment efficiency (EE). In vitro release behaviors of pure ACF and ACF-loaded PMs at each release point indicated that the release profile of pH-responsive PMs loaded with ACF demonstrated quicker release rates (94% after 480 min) compared to the release behavior noticed for free ACF (59.56% after 480 min). Furthermore, the release rates exhibit a notable rise when the pH is increased from 1.2 to 4.7. In the carrageenan-induced inflammation model of paw edema in rats, it has been demonstrated that the injection of ACF-loaded PMs (at a dose of 10 mg/kg) resulted in a strengthened inflammatory activity compared to the injection of free ACF at equivalent dosages as well as at time intervals. However, the use of ACF-loaded PMs for a duration of 6 h displayed a notable reduction of paw edema, with an inhibition percentage of 85.09%, in contrast to the 74.9% inhibition percentage observed for the free ACF medication.

5.
Scand J Trauma Resusc Emerg Med ; 31(1): 88, 2023 Nov 28.
Artículo en Inglés | MEDLINE | ID: mdl-38017553

RESUMEN

BACKGROUND: Mass casualty incidents (MCI) pose significant challenges to existing resources, entailing multiagency collaboration. Triage is a critical component in the management of MCIs, but the lack of a universally accepted triage system can hinder collaboration and lead to preventable loss of life. This multinational study uses validated patient cards (cases) based on real MCIs to evaluate the feasibility and effectiveness of a novel Translational Triage Tool (TTT) in primary triage assessment of mass casualty victims. METHODS: Using established triage systems versus TTT, 163 participants (1575 times) triaged five patient cases. The outcomes were statistically compared. RESULTS: TTT demonstrated similar sensitivity to the Sieve primary triage method and higher sensitivity than the START primary triage system. However, the TTT algorithm had a lower specificity compared to Sieve and higher over-triage rates. Nevertheless, the TTT algorithm demonstrated several advantages due to its straightforward design, such as rapid assessment, without the need for additional instrumental interventions, enabling the engagement of non-medical personnel. CONCLUSIONS: The TTT algorithm is a promising and feasible primary triage tool for MCIs. The high number of over-triages potentially impacts resource allocation, but the absence of under-triages eliminates preventable deaths and enables the use of other personal resources. Further research involving larger participant samples, time efficiency assessments, and real-world scenarios is needed to fully assess the TTT algorithm's practicality and effectiveness in diverse multiagency and multinational contexts.


Asunto(s)
Planificación en Desastres , Servicios Médicos de Urgencia , Incidentes con Víctimas en Masa , Humanos , Triaje/métodos , Servicios Médicos de Urgencia/métodos , Algoritmos , Cuidados Paliativos , Planificación en Desastres/métodos
6.
Inflammopharmacology ; 31(6): 2857-2883, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37950803

RESUMEN

Chronic inflammation is a common underlying factor in many major diseases, including heart disease, diabetes, cancer, and autoimmune disorders, and is responsible for up to 60% of all deaths worldwide. Metformin, statins, and corticosteroids, and NSAIDs (non-steroidal anti-inflammatory drugs) are often given as anti-inflammatory pharmaceuticals, however, often have even more debilitating side effects than the illness itself. The natural product-based therapy of inflammation-related diseases has no adverse effects and good beneficial results compared to substitute conventional anti-inflammatory medications. In this review article, we provide a concise overview of present pharmacological treatments, the pathophysiology of inflammation, and the signaling pathways that underlie it. In addition, we focus on the most promising natural products identified as potential anti-inflammatory therapeutic agents. Moreover, preclinical studies and clinical trials evaluating the efficacy of natural products as anti-inflammatory therapeutic agents and their pragmatic applications with promising outcomes are reviewed. In addition, the safety, side effects and technical barriers of natural products are discussed. Furthermore, we also summarized the latest technological advances in the discovery and scientific development of natural products-based medicine.


Asunto(s)
Enfermedades Autoinmunes , Productos Biológicos , Humanos , Productos Biológicos/farmacología , Productos Biológicos/uso terapéutico , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/uso terapéutico , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Enfermedades Autoinmunes/tratamiento farmacológico
7.
Cells ; 12(20)2023 10 18.
Artículo en Inglés | MEDLINE | ID: mdl-37887319

RESUMEN

Binge or chronic alcohol consumption causes neuroinflammation and leads to alcohol use disorder (AUD). AUD not only affects the central nervous system (CNS) but also leads to pathologies in the peripheral and enteric nervous systems (ENS). Thus, understanding the mechanism of the immune signaling to target the effector molecules in the signaling pathway is necessary to alleviate AUD. Growing evidence shows that excessive alcohol consumption can activate neuroimmune cells, including microglia, and change the status of neurotransmitters, affecting the neuroimmune system. Microglia, like peripheral macrophages, are an integral part of the immune defense and represent the reticuloendothelial system in the CNS. Microglia constantly survey the CNS to scavenge the neuronal debris. These cells also protect parenchymal cells in the brain and spinal cord by repairing nerve circuits to keep the nervous system healthy against infectious and stress-derived agents. In an activated state, they become highly dynamic and mobile and can modulate the levels of neurotransmitters in the CNS. In several ways, microglia, enteric glial cells, and macrophages are similar in terms of causing inflammation. Microglia also express most of the receptors that are constitutively present in macrophages. Several receptors on microglia respond to the inflammatory signals that arise from danger-associated molecular patterns (DAMPs), pathogen-associated molecular patterns (PAMPs), endotoxins (e.g., lipopolysaccharides), and stress-causing molecules (e.g., alcohol). Therefore, this review article presents the latest findings, describing the roles of microglia and enteric glial cells in the brain and gut, respectively, and their association with neurotransmitters, neurotrophic factors, and receptors under the influence of binge and chronic alcohol use, and AUD.


Asunto(s)
Eje Cerebro-Intestino , Microglía , Humanos , Microglía/metabolismo , Neuroglía/fisiología , Inflamación/metabolismo , Etanol/metabolismo , Neurotransmisores/metabolismo
8.
Am J Rhinol Allergy ; 37(6): 630-637, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37786364

RESUMEN

BACKGROUND: COVID-19 has been associated with olfactory dysfunction in many infected patients. The rise of calcium levels in the nasal secretions plays an essential role in the olfaction process with a desensitization effect on the olfactory receptor neurons and a negative impact on the olfaction transmission. Ethylene diamine tetra acetic acid (EDTA) is a chelating agent that can bind free calcium in the nasal secretions, thereby reducing the adverse effects of calcium on olfactory function. OBJECTIVES: The objective of this work is to demonstrate the effect of intranasal EDTA on improving olfactory dysfunction following COVID-19. METHODS: Fifty patients with a history of COVID-19 and olfactory dysfunction that persisted for more than 6 months were enrolled in the current prospective randomized clinical trial. Participants were randomized into 2 equal groups. Twenty-five patients were treated with olfactory training only, while the remaining 25 patients received treatment with olfactory training and a topical nasal spray of ethylene diamine tetra acetic acid. The olfactory function was assessed before treatment and 3 months later using the Sniffin' Sticks test. Additionally, the determination of calcium level in the nasal secretions was performed using an ion-selective electrode before treatment and 3 months later. RESULTS: Eighty-eight percent of the patients treated with olfactory training in addition to EDTA exhibited clinical improvement, while 60% showed improvement in patients treated with olfactory training only. Furthermore, a significant decrease in the measured calcium level in the nasal secretions was demonstrated after the use of ethylene diamine tetra compared to patients treated with olfactory training only. CONCLUSION: Ethylene diamine tetra acetic acid may be associated with an improvement of the olfactory function post-COVID-19.


Asunto(s)
COVID-19 , Trastornos del Olfato , Humanos , Olfato/fisiología , Trastornos del Olfato/tratamiento farmacológico , Trastornos del Olfato/etiología , Ácido Acético/farmacología , Ácido Acético/uso terapéutico , Calcio/farmacología , Calcio/uso terapéutico , Ácido Edético/uso terapéutico , Ácido Edético/farmacología , COVID-19/complicaciones , Etilenos/farmacología , Etilenos/uso terapéutico
9.
Int J Pharm ; 646: 123385, 2023 Nov 05.
Artículo en Inglés | MEDLINE | ID: mdl-37678473

RESUMEN

The evolution of a safe and effective therapeutic system to conquer SAR-CoV-2 infection deemed to be a crucial worldwide demand. Curcumin (CUR) is a phytomedicinal polyphenolic drug that exhibited a well-reported anti-SAR-CoV-2. However, the therapeutic activity of CUR is hindered by its poor intestinal permeability and diminished aqueous solubility. Therefore, this study strived to develop D-alpha-tocopheryl polyethylene glycol succinate (TPGS) bilosomes (TPGS-Bs) adopting 23 full factorial designs to improve solubility and intestinal permeability of CUR, hence boosting its anti-SARS-CoV-2 activity. Eight experimental runs were attained considering three independent variables: soybean phosphatidylcholine amount (mg) (SPC amount), bile salt amount (mg) (BS amount), and TPGS amount (mg). The optimum formula (F4) exhibited EE % (88.5 ± 2.4 %), PS (181.5 ± 21.6 nm), and ZP (-34.5 ± 3.7 mV) with desirability value = 0.739 was picked as an optimum formula. Furthermore, the optimum formula (F4) was extra coated with chitosan (CS) to improve permeability and anti-SAR-CoV-2 activity. Caco-2 cell uptake after 2 hr revealed the superiority of CS-F4 and F4 by 6 and 5 folds relative to CUR dispersion, respectively. Furthermore, CS-F4 exhibited a significantly higher anti-SARS-CoV-2 activity with IC50 (0.24 µg/ml) by 8.3 times than F4 (1.99 µg/ml). Besides, the mechanistic study demonstrated that the two formulae imparted antiviral activity by inhibiting the spike protein by virucidal potentialities. In addition, the conducted molecular docking and MD simulations towards the SARS-CoV-2 Mpro enzyme confirmed the interaction of CUR with key residues of the virus enzymes. Based on the preceded, CS-F4 could be assumed to be used to effectively eradicate SARS-CoV-2 infection.

11.
Artículo en Inglés | MEDLINE | ID: mdl-37594095

RESUMEN

INTRODUCTION: The conventional processes of drug discovery are too expensive, time-consuming and the success rate is limited. Searching for alternatives that have evident safety and potential efficacy could save money, time and improve the current therapeutic regimen outcomes. METHOD: Clinical phytotherapy implies the use of extracts of natural origin for prophylaxis, treatment, or management of human disorders. In this work, the potential role of common Fig (Ficus carica) in the management of COVID-19 infections has been explored. The antiviral effects of Cyanidin-3-rhamnoglucoside which is abundant in common Figs have been illustrated on COVID-19 targets. The immunomodulatory effect and the ability to ameliorate the cytokine storm associated with coronavirus infections have also been highlighted. This work involves various computational studies to investigate the potential roles of common figs in the management of COVID-19 viral infections. RESULTS: Two molecular docking studies of all active ingredients in common Figs were conducted starting with MOE to provide initial insights, followed by Autodock Vina for further confirmation of the results of the top five compounds with the best docking score. CONCLUSION: Finally, Molecular dynamic simulation alongside MMPBSA calculations were conducted using GROMACS to endorse and validate the entire work.

12.
Molecules ; 28(15)2023 Jul 27.
Artículo en Inglés | MEDLINE | ID: mdl-37570648

RESUMEN

In the last decade, gypsogenin has attracted widespread attention from medicinal chemists by virtue of its prominent anti-cancer potential. Despite its late identification, gypsogenin has proved itself as a new anti-proliferative player battling for a frontline position among other classic pentacyclic triterpenes such as oleanolic acid, glycyrrhetinic acid, ursolic acid, betulinic acid, and celastrol. Herein, we present the most important reactions of gypsogenin via modification of its four functional groups. Furthermore, we demonstrate insights into the anti-cancer activity of gypsogenin and its semisynthetic derivatives and go further by introducing our perspective to judiciously guide the prospective rational design. The present article opens a new venue for a better exploitation of gypsogenin chemical entity as a lead compound in cancer chemotherapy. To the best of our knowledge, this is the first review article exploring the anti-cancer activity of gypsogenin derivatives.


Asunto(s)
Neoplasias , Ácido Oleanólico , Saponinas , Triterpenos , Humanos , Estudios Prospectivos , Triterpenos Pentacíclicos/química , Triterpenos/química , Saponinas/uso terapéutico , Neoplasias/tratamiento farmacológico
13.
Inflammopharmacology ; 31(5): 2571-2585, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37432554

RESUMEN

Cerium oxide nanoparticles (CONPs), owing to their radical scavenging property, have recently emerged as a therapeutic candidate for oxidative stress-mediated neurological diseases. However, oral and intravenous administration of CONPs is limited due to their poor physicochemical characteristics, low bioavailability, rapid systemic clearance, poor blood-brain penetration and dose-dependent toxicity. To overcome these challenges, we developed intranasal CONPs and evaluated their potential in the experimental PD model. CONPs were prepared by homogenous precipitation using tween 80 as a stabilizer and methanol/water as solvent. The optimization was done using Central Composite Design (CCD). The CONPs synthesis was confirmed by UV and FTIR. The optimized CONPs were small-sized (105.1 ± 5.78 nm), spherical (TEM), uniform (PDI, 0.119 ± 0.006) and stable (ZP, -22.7 ± 1.02 mV). Energy-dispersive X-ray analysis showed characteristic signals of Ce in developed CONPs. The X-ray diffraction pattern described the cubic fluorite structure and nano-crystalline nature of CONPs. The CONP anti-oxidant activity was found to be 93.60 ± 0.32% at 25 µg/mL concentration. Finally, motor manifestation studies like the forced swim test, locomotor test, akinesia, catalepsy, and muscle coordination test were conducted to assess the motor dysfunctions and behavioral activity in all four animal groups. Results of the in vivo motor manifestation studies in the haloperidol-induced PD rat model showed that co-administration of intranasal CONPs along with a half dose of levodopa resulted in significant protection, and results were significantly different from the untreated group but not significantly different from the healthy group. In conclusion, intranasal CONPs can be useful in ameliorating oxidative stress through their antioxidant effect and could be prospective therapeutics for the treatment of motor manifestations in Parkinson's disease.


Asunto(s)
Nanopartículas , Trastornos Parkinsonianos , Ratas , Animales , Haloperidol/farmacología , Estrés Oxidativo
14.
Front Nutr ; 10: 1125106, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37415912

RESUMEN

Introduction: Dietary medicinal plants are among the most sought-after topics in alternative medicine today due to their preventive and healing properties against many diseases. Aim: This study aimed to extract and determine the polyphenols from indigenous plants extracts, i.e., Mentha longifolia, M. arvensis, Tinospora cordifolia, Cymbopogon citratus, Foeniculum vulgare, Cassia absus, Camellia sinensis, Trachyspermum ammi, C. sinensis and M. arvensis, then evaluate the antioxidant, cytotoxicity, and antimicrobial properties, besides enzyme inhibition of isolated polyphenols. Methods: The antioxidant activity was evaluated by DPPH, Superoxide radical, Hydroxyl radical (OH.), and Nitric oxide (NO.) scavenging activity; the antidiabetic activity was evaluated by enzymatic methods, and anticancer activity using MTT assay, while the antibacterial activity. Results: The results showed that tested medicinal plants' polyphenolic extracts (MPPE) exhibited the most significant antioxidant activity in DPPH, hydroxyl, nitric oxide, and superoxide radical scavenging methods because of the considerable amounts of total polyphenol and flavonoid contents. UHPLC profile showed twenty-five polyphenol complexes in eight medicinal plant extracts, categorized into phenolic acids, flavonoids, and alkaloids. The main polyphenol was 3-Feroylquinic acid (1,302 mg/L), also found in M. longifolia, C. absus, and C. sinensis, has a higher phenolic content, i.e., rosmarinic acid, vanillic acid, chlorogenic acid, p-coumaric acid, ferulic acid, gallic acid, catechin, luteolin, 7-O-neohesperideside, quercetin 3,7-O-glucoside, hesperidin, rutin, quercetin, and caffeine in the range of (560-780 mg/L). At the same time, other compounds are of medium content (99-312 mg/L). The phenolics in C. sinensis were 20-116% more abundant than those in M. longifolia, C. absus, and other medicinal plants. While T. cordifolia is rich in alkaloids, T. ammi has a lower content. The MTT assay against Caco-2 cells showed that polyphenolic extracts of T. ammi and C. citratus had maximum cytotoxicity. While M. arvensis, C. sinensis, and F. vulgare extracts showed significant enzyme inhibition activity, C. sinensis showed minor inhibition activity against α-amylase. Furthermore, F. vulgare and C. sinensis polyphenolic extracts showed considerable antibacterial activity against S. aureus, B. cereus, E. coli, and S. enterica. Discussion: The principal component analysis demonstrated clear separation among medicinal plants' extracts based on their functional properties. These findings prove the therapeutic effectiveness of indigenous plants and highlight their importance as natural reserves of phytogenic compounds with untapped potential that needs to be discovered through advanced analytical methods.

15.
Environ Res ; 234: 116562, 2023 10 01.
Artículo en Inglés | MEDLINE | ID: mdl-37419194

RESUMEN

Increased thickness of the skin and hyperproliferation of keratinocyte cell is the main obstacle in the treatment of psoriasis. Gallic Acid (GA) has shown efficacious results against the hyperproliferation of keratinocytes while lipid-polymer loaded hybrid nanoparticles (LPHNs) have an edge over lipidic and polymeric nanoparticles considering drug loading, controlled release, stability, and retention. The LPHNs were optimized using Box-Behnken method and was further characterized by FTIR, DSC and Zetasizer. The optimized preparation demonstrated a size of 170.5 ± 0.087 nm and a PDI of 0.19 ± 0.0015, respectively. The confocal study has suggested that the hybrid nanosystem enhanced the drug penetration into the deeper layer with a higher drug release of 79 ± 0.001% as compared to the gallic acid-loaded gel. In addition, the formulation significantly reduced PASI score and splenomegaly without causing any serious irritation. The morphological study of the spleen suggested that the prepared formulation has well controlled the disease compared to the marketed formulation while maintaining a normal level of immune cells after treatment. Hence GALPHN could be accepted as one of the excellent vehicles for the topical conveyance of GA (gallic acid) due to enhanced penetration, and good retention, along with fewer side effects and higher efficacy of the GALPHN gel against imiquimod (IMQ) induced psoriasis.


Asunto(s)
Quitosano , Nanopartículas , Psoriasis , Humanos , Imiquimod/uso terapéutico , Lecitinas/toxicidad , Lecitinas/uso terapéutico , Ácido Gálico , Psoriasis/inducido químicamente , Psoriasis/tratamiento farmacológico , Tamaño de la Partícula
16.
Mol Cancer ; 22(1): 98, 2023 06 21.
Artículo en Inglés | MEDLINE | ID: mdl-37344887

RESUMEN

Cancer is a grievous disease whose treatment requires a more efficient, non-invasive therapy, associated with minimal side effects. Gold nanoparticles possessing greatly impressive optical properties have been a forerunner in bioengineered cancer therapy. This theranostic system has gained immense popularity and finds its application in the field of molecular detection, biological imaging, cancer cell targeting, etc. The photothermal property of nanoparticles, especially of gold nanorods, causes absorption of the light incident by the light source, and transforms it into heat, resulting in tumor cell destruction. This review describes the different optical features of gold nanoparticles and summarizes the advance research done for the application of gold nanoparticles and precisely gold nanorods for combating various cancers including breast, lung, colon, oral, prostate, and pancreatic cancer.


Asunto(s)
Nanopartículas del Metal , Nanotubos , Neoplasias , Masculino , Humanos , Oro/uso terapéutico , Nanopartículas del Metal/uso terapéutico , Neoplasias/tratamiento farmacológico , Diagnóstico por Imagen , Línea Celular Tumoral
17.
Pharmaceuticals (Basel) ; 16(2)2023 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-37259360

RESUMEN

Triazole-based acetamides serve as important scaffolds for various pharmacologically active drugs. In the present work, structural hybrids of 1,2,4-triazole and acetamides were furnished by chemically modifying 2-(4-isobutylphenyl) propanoic acid (1). Target compounds 7a-f were produced in considerable yields (70-76%) by coupling the triazole of compound 1 with different electrophiles under different reaction conditions. These triazole-coupled acetamide derivatives were verified by physiochemical and spectroscopic (HRMS, FTIR, 13CNMR, and 1HNMR,) methods. The anti-liver carcinoma effects of all of the derivatives against a HepG2 cell line were investigated. Compound 7f, with two methyl moieties at the ortho-position, exhibited the highest anti-proliferative activity among all of the compounds with an IC50 value of 16.782 µg/mL. 7f, the most effective anti-cancer molecule, also had a very low toxicity of 1.190.02%. Molecular docking demonstrates that all of the compounds, especially 7f, have exhibited excellent binding affinities of -176.749 kcal/mol and -170.066 kcal/mol to c-kit tyrosine kinase and protein kinase B, respectively. Compound 7f is recognized as the most suitable drug pharmacophore for the treatment of hepatocellular carcinoma.

18.
Pharmaceuticals (Basel) ; 16(2)2023 Feb 13.
Artículo en Inglés | MEDLINE | ID: mdl-37259428

RESUMEN

In this present research, an attempt has been made to address the influence of drug-coformer stoichiometric ratio on cocrystal design and its impact on improvement of solubility and dissolution, as well as bioavailability of poorly soluble telmisartan. The chemistry behind cocrystallization and the optimization of drug-coformer molar ratio were explored by the molecular docking approach, and theoretical were implemented practically to solve the solubility as well as bioavailability related issues of telmisartan. A new multicomponent solid form, i.e., cocrystal, was fabricated using different molar ratios of telmisartan and maleic acid, and characterized by SEM, DSC and XRD studies. The molecular docking study suggested that specific molar ratios of drug-coformer can successfully cluster with each other and form a specific geometry with favourable energy conformation to form cocrystals. Synthesized telmisartan-maleic acid cocrystals showed remarkable improvement in solubility and dissolution of telmisartan by 9.08-fold and 3.11-fold, respectively. A SEM study revealed the formation of cocrystals of telmisartan when treated with maleic acid. DSC and XRD studies also confirmed the conversion of crystalline telmisartan into its cocrystal state upon treating with maleic acid. Preclinical investigation revealed significant improvement in the efficacy of optimized cocrystals in terms of plasma drug concentration, indicating enhanced bioavailability through improved solubility as well as dissolution of telmisartan cocrystals. The present research concluded that molecular docking is an important path in selecting an appropriate stoichiometric ratio of telmisartan: maleic acid to form cocrystals and improve the solubility, dissolution, and bioavailability of poorly soluble telmisartan.

19.
Saudi Pharm J ; 31(5): 706-726, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-37181141

RESUMEN

Chorisia (syn. Ceiba) species are important ornamental, economic, and medicinal plants that are endowed with a diversity of secondary metabolites; however, their volatile organic compounds (VOCs) have been scarcely studied. Therefore, this work explores and compares the headspace floral volatiles of three common Chorisia species, namely Chorisia chodatii Hassl., Chorisia speciosa A. St.-Hil, and Chorisia insignis H.B.K. for the first time. A total of 112 VOCs of varied biosynthetic origins were identified at different qualitative and quantitative ratios, encompassing isoprenoids, fatty acid derivatives, phenylpropanoids, and others. Flowers of the investigated species showed perceptibly differentiated volatile profiles, with those emitted by C. insignis being dominated by non-oxygenated compounds (56.69 %), whereas oxygenated derivatives prevailed among the volatiles of C. chodatii (66.04 %) and C. speciosa (71.53 %). The variable importance in the projection (VIP) in the partial least-squares-discriminant (PLS-DA) analysis described 25 key compounds among the studied species, of which linalool was verified as the most important aroma compound based on VIP values and significance analysis, and it could represent the most typical VOC among these Chorisia species. Furthermore, molecular docking and dynamics analyses of both the major and the key VOCs displayed their moderate to promising binding interactions with four main proteins of SARS-CoV-2, including Mpro, PLpro, RdRp, and spike S1 subunit RBD. The current results collectively cast new light on the chemical diversity of the VOCs of Chorisia plants as well as their chemotaxonomic and biological relevance.

20.
Mol Cancer ; 22(1): 87, 2023 05 25.
Artículo en Inglés | MEDLINE | ID: mdl-37226188

RESUMEN

The advent of nanotechnology has opened new possibilities for bioimaging. Metal nanoparticles (such as gold, silver, iron, copper, etc.) hold tremendous potential and offer enormous opportunities for imaging and diagnostics due to their broad optical characteristics, ease of manufacturing technique, and simple surface modification. The arginine-glycine-aspartate (RGD) peptide is a three-amino acid sequence that seems to have a considerably greater ability to adhere to integrin adhesion molecules that exclusively express on tumour cells. RGD peptides act as the efficient tailoring ligand with a variety of benefits including non-toxicity, greater precision, rapid clearance, etc. This review focuses on the possibility of non-invasive cancer imaging using metal nanoparticles with RGD assistance.


Asunto(s)
Nanopartículas del Metal , Neoplasias , Humanos , Secuencia de Aminoácidos , Glicina , Oligopéptidos
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