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1.
Curr Drug Deliv ; 2024 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-39021184

RESUMO

The eye is a most delicate organ protected by several complex biological barriers that are static and dynamic. The presence of these ocular barriers retards drug absorption from topically applied dosage forms at the conjunctival sac. The efficient topical delivery of the drug into the globe is more difficult to achieve and there is a need to develop a topical formulation that may reduce the use of injections and increase patient compliance with decreased frequency of administration. In the advancements of research in nanotechnology, nanoemulsions can be used as biocompatible carriers to deliver the drug to the ocular cavity. The lipophilic globules can increase the solubility of hydrophobic cargos which provides increased permeation ability and ocular bioavailability which can sustain drug release and corneal retention. Because of their small size, these formulations do not cause blurring of vision. Nanoemulsions (NEs) over the past decade have been used to treat several ocular diseases in the anterior eye segment. This review summarizes the economic burden, pathology of ocular diseases, formulation considerations for ocular formulations, and recent advances of these NEs as effective carriers for ocular drug delivery highlighting their performance in pre-clinical studies.

2.
Artigo em Inglês | MEDLINE | ID: mdl-38939991

RESUMO

BACKGROUND: Non-communicable diseases are chronic systemic inflammation in humans that occurs because of enhanced inflammatory mediators of the arachidonic acid cas-cade. We aimed to explore whether the lead chalcone compounds could exhibit anti-inflam-matory activity via dual blockage of COX-2/5-LOX enzymes and their regulatory mechanism. METHODS: RAW 264.7 macrophages were collected from NCC, Pune, for in-vitro experiments. The IC50 values of chalcone compounds C45 and C64 were calculated. RAW 264.7 macro-phages were treated with C45 and C64 (10%, 5%, 2.5%, 0.125%, and 0.0625% concentration). The cell viability was carried out with an MTT assay. The COX-1, COX-2, 5-LOX, PGE2, and LTB4 levels were detected by ELISA-based kits. The in-vivo evaluation was carried out in Male Wistar rats (250-300 g, 7-8 weeks old) with acute and chronic anti-inflammatory models and histopathological studies on the stomach, liver, and kidney. RESULTS: The present study described the in-vitro and in-vivo biological evaluation of dual COX-2/5-LOX inhibitors in chalcone derivatives (C45 and C64) compounds showed the most effective COX-2 and 5-LOX inhibition with IC50 values 0.092 and 0.136µM respectively. Simultaneously, compound C64 showed comparable selectivity towards COX-2 with a Selec-tivity Index (SI) of 68.43 compared to etoricoxib, with an SI of 89.32. In-vivo carrageenan-induced rat paw oedema activity, the compound C64 showed a significant reduction in oedema with 78.28% compared to indomethacin with 88.07% inhibition. Furthermore, cotton pellet-induced granuloma activity revealed that compound C64 significantly reduced 32.85% com-pared with standard 40.13% granuloma inhibition. CONCLUSION: The chalcone compound C64, (E)-1-(4-Amino-2-hydroxyphenyl)-3-(3,4,5-tri-methoxyphenyl)-prop-2-en-1-one was proved to be a potent and novel Dual COX-2/5-LOX inhibitor with improved gastric safety profiling.

3.
World Neurosurg ; 187: 172-183.e2, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38649027

RESUMO

When noninvasive tests are unable to define the epileptogenic zone in patients, intracranial electroencephalography (iEEG) is a method of localizing the epileptogenic zone. Compared with noninvasive evaluations, it offers more precise information about patterns of epileptiform activity, which results in useful diagnostic information that supports surgical decision-making. The primary aim of the present study was to assess the utility of iEEG for definitive surgery for patients with drug-resistant epilepsy. Online databases such as PubMed, Medline, Embase, Scopus, Cochrane Library, Web of Science, and IEEE Xplore were searched for MeSH terms and free-text keywords. The ROBINS I (risk of bias in non-randomized studies - of interventions) critical appraisal tool was used for quality assessment. The prevalence from different studies was pooled together using the inverse variance heterogeneity method. Egger's regression analysis and funnel plot were used to evaluate publication bias. The systematic review included 18 studies, and the meta-analysis included 10 studies to estimate the prevalence of seizure freedom (Engel class I) in patients undergoing surgery after iEEG. A total of 526 patients were included in the meta-analysis. The follow-up period ranged from 1 to 10 years. The overall pooled estimate of the prevalence of seizure freedom (Engel class I) for patients undergoing surgery after iEEG was 53% (95% confidence interval, 44%-62%). The results additionally demonstrated that 12 studies had a moderate risk of bias and 6 had a low risk. Future studies are crucial to enhance our understanding of iEEG to guide patient choices and unravel their implications.


Assuntos
Epilepsia Resistente a Medicamentos , Humanos , Epilepsia Resistente a Medicamentos/cirurgia , Epilepsia Resistente a Medicamentos/diagnóstico , Epilepsia Resistente a Medicamentos/fisiopatologia , Eletrocorticografia/métodos , Eletroencefalografia/métodos , Procedimentos Neurocirúrgicos/métodos
4.
Artigo em Inglês | MEDLINE | ID: mdl-38551055

RESUMO

Point of Care Diagnostics (POCD) is quintessential in hospitals and the healthcare sector as the secants uplift the quality of medical care and the life of a patient by facilitating quick identification of the underlying pathological condition. Nanotechnology can provide opportunities and has potential in the development of new-age sensing/diagnostic tools. Owing to extraordinary features (e.g., higher density, effective catalysis, good conduction, biocompatibility, inertness, and greater surface-to-volume ratio), gold nanoparticles (AuNPs) are frequently employed in POCT (Point-of-Care-Testing). Gold nanoparticles-based colorimetric methods are widely used in the rapid, sensitive, and selective detection of analytes/target molecules. AuNPs description is critical for their possible utility in prophylaxis, diagnostics, and treatment of an ailment. AuNPs interact with organic/inorganic target molecules to generate colorimetric shift that enables the accurate, precise, and subtle recognition of biologicals (e.g., microorganisms, cellular components, and proteins) and metal ions. This review focused on the need for AuNPs-based colorimetric application in prophylaxis, diagnostics, and treatment in healthcare and reviewed the future outlook of these AuNPs for biological applications. Different synthesis methods of AuNPs, their morphology, and characterization, including their surface functionalization, will be discussed in detail. AuNPs are very much preferable nanomaterials owing to exclusive optical, electrical, and photothermal features. AuNPs-based colorimetric biosensors are simple and possess great utility, yet these offer a robust technique to enable visual, quantitative analysis.

5.
J Skin Cancer ; 2024: 3859066, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38370137

RESUMO

Background: This study presents a comparative analysis of recently published guidelines to manage cutaneous squamous cell carcinoma (cSCC) and cutaneous basal cell carcinoma (cBCC) within the United States (US). Methods: A PubMed database search was performed for the time period between June 1, 2016, and December 1, 2022. A comprehensive comparison was performed in the following clinical interest areas: staging and risk stratification, management of primary tumor and regional nodes with curative intent, and palliative treatment. Results: Guidelines from 3 organizations were analyzed: the American Academy of Dermatology (AAD), the National Comprehensive Cancer Network (NCCN), and the American Society for Radiation Oncology (ASTRO). The guidelines used different methodologies to grade evidence, making comparison difficult. There was agreement that surgery is the preferred treatment for curative cBCC and cSCC. For patients ineligible for surgery, there was a consensus to recommend definitive radiation. AAD and NCCN recommended consideration of other topical modalities in selected low-risk cBCC. Postoperative radiation therapy (PORT) was uniformly recommended in patients with positive margins that could not be cleared with surgery and in patients with nerve invasion. The definition and extent of nerve invasion varied. All guidelines recommended surgery as the primary treatment in patients with lymph node metastases in a curative setting. The criteria used for PORT varied; NCCN and ASTRO used lymph node size, number of nodes, and extracapsular extension for recommending PORT. Both NCCN and ASTRO recommend consideration of systemic treatment along with PORT in patients with extracapsular extension. Conclusion: US guidelines provide contemporary and complementary information on the management of cBCC and cSCC. There are opportunities for research, particularly in the areas of staging, indications for adjuvant treatment in curative settings, extent of nerve invasion and prognosis, and the role of systemic treatments in curative and palliative settings.

6.
Artigo em Inglês | MEDLINE | ID: mdl-37218182

RESUMO

Diabetes is a metabolic disorder that has been reported to increase the mortality rate worldwide. About 40 million people across the globe suffer from diabetes, with people living in developing countries being affected the most due to this deadly disease. Although the therapeutic management of hyperglycaemia can treat diabetes, metabolic disorders associated with this disease are a greater challenge in its treatment. Hence, potential strategies to treat hyperglycaemia and its side effects are needed. In this review, we have summarized several therapeutic targets, like dipeptidyl peptidase-4 (DPP-4), glucagon receptor antagonists, glycogen phosphorylase or fructose-1,6- biphosphatase inhibitors, SGLT inhibitors, 11beta-HSD-1 inhibitors, glucocorticoids receptor antagonists, glucose-6-phosphatase and glycogen phosphorylase inhibitors. These targets can help in designing and developing novel antidiabetic agents.


Assuntos
Diabetes Mellitus Tipo 2 , Inibidores da Dipeptidil Peptidase IV , Hiperglicemia , Humanos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/complicações , Inibidores da Dipeptidil Peptidase IV/farmacologia , Inibidores da Dipeptidil Peptidase IV/uso terapêutico , Hiperglicemia/tratamento farmacológico , Glicogênio Fosforilase
7.
Pharm Pat Anal ; 12(4): 177-191, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37671908

RESUMO

Imidazothiadiazole was discovered around the 1950s era, containing an imidazole ring fused to a thiadiazole ring. Imidazothiadiazole exhibit versatile pharmacological properties including anticonvulsant, cardiotonic, anti-inflammatory, diuretic, antifungal, antibacterial and anticancer. Despite of the being discovered in 1950s, the imidazothiadiazole derivatives are unable to being processed to clinical trials because of lack of bioavailability, efficacy and cytotoxicity. The recent patent literature focused on structural modification of imidazothiadiazole core to overcome these problems. This review limelight a disease-centric perspective on patented imidazothiadiazole from 2015-2023 and to understand their mechanism of action in related diseases. The relevant granted patent applications were located using patent databases, Google Patents, USPTO, EPO, WIPO, Espacenet and Lens.


Assuntos
Tiadiazóis , Tiadiazóis/farmacologia , Tiadiazóis/química , Anti-Inflamatórios
8.
Mini Rev Med Chem ; 2023 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-37694781

RESUMO

Prostate cancer is a disease that is affecting a large population worldwide. Androgen deprivation therapy (ADT) has become a foundation for the treatment of advanced prostate cancer, as used in most clinical settings from neo-adjuvant to metastatic stage. In spite of the success of ADT in managing the disease in the majority of men, hormonal manipulation fails eventually. New molecules are developed for patients with various hormone-refractory diseases. Advancements in molecular oncology have increased understanding of numerous cellular mechanisms which control cell death in the prostate and these insights can lead to the development of more efficacious and tolerable therapies for carcinoma of the prostate. This review is focused on numerous therapies that might be a boon for prostate therapy like signaling inhibitors, vaccines, and inhibitors of androgen receptors. Along with these, various bioactive molecules and their derivatives are highlighted, which act as potential anti-prostate cancer agents. This article also emphasized the recent advances in the field of medicinal chemistry of prostate cancer agents.

9.
Cureus ; 15(7): e41301, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37539397

RESUMO

BACKGROUND: Pectus deformities are commonly seen in chest wall deformities among the pediatric age group. Pectus deformities occur due to defective growth of the sternum and its surrounding cartilage. The Nuss procedure is the technique of choice for correcting the deformity surgically which includes placing a convex bar under the sternum without resection or injury to costal cartilages. Adequate pain control is utmost to improve wound healing, patient satisfaction, short hospital stays, and decrease the financial burden on attendants. Therefore, it is necessary to investigate which analgesic method is more advantageous for the Nuss procedure. OBJECTIVE: To compare the analgesic effects of intravenous patient-controlled analgesia (IVPCA) morphine versus computerized ambulatory delivery device (CADD) epidural morphine on acute post-operative pain management in Nuss procedures. METHODS: A retrospective study was done at Rajiv Gandhi Cancer and Research Hospital, New Delhi from 2015 to 2020 to assess the efficacy and safety between IVPCA morphine and CADD epidural for post-operative analgesia following pectus excavatum repair. A total of 34 cases of Nuss procedures were taken with 17 cases in each group. Group 1 (intravenous PCA morphine) was given 39 ml normal saline + 6 ml morphine (total 45 ml, 2 mg/ml morphine), set at demand dose 0.5 ml, i.e. 1 mg, lockout interval 7 minutes, doses per hour was six and Group 2 (CADD epidural morphine) was given 42 ml normal saline + 3 ml morphine (1 mg/ml morphine) with continuous infusion at the rate of 0.5 ml/hr. Demand dose 0, lockout interval nil. Visual analog pain scores using a scale of 0-10 and Ramsay Sedation Score (RSS) scores were obtained on arrival at the post-anesthesia care unit, at 12, 24, 48, and 72 hours throughout the subsequent hospital stay. RESULTS: This study yielded positive information about our experience with the pectus post-operative pain management. The mean visual analog scale (VAS) score was lower in Group 1 compared to Group 2 but significantly different at 12 and 72 hours only. The mean RSS score was comparable between groups. The mean hospital stay (days) and requirement of rescue analgesia doses were 3.47±0.51 and 0.12±0.33 in Group 1 and 4.76±0.44, 0.59±1.12 in Group 2. CONCLUSION:  Both IVPCA morphine and CADD morphine were effective in controlling post-surgical pain in the Nuss procedure, but IVPCA morphine was better as compared to CADD morphine in this regard because it was noninvasive, safe, and cost-effective with non-significant complications.

10.
Curr Mol Med ; 2023 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-37312440

RESUMO

The ubiquitous pandemic that emerged due to COVID-19 affected the whole planet. People all over the globe became vulnerable to the unpredictable emergence of coronavirus. The sudden emergence of respiratory disease in coronavirus infected several patients. This affected human life drastically, from mild symptoms to severe illness, leading to mortality. COVID-19 is an exceptionally communicable disease caused by SARS-CoV-2. According to a genomic study, the viral spike RBD interactions with the host ACE2 protein from several coronavirus strains and the interaction between RBD and ACE2 highlighted the potential change in affinity from the virus causing the COVID-19 outbreak to a progenitor type of SARS-CoV-2. SARS-CoV-2, which could be the principal reservoir, is phylogenetically related to the SARS-like bat virus. Other research works reported that intermediary hosts for the transmission of viruses to humans could include cats, bats, snakes, pigs, ferrets, orangutans, and monkeys. Even with the arrival of vaccines and individuals getting vaccinated and treated with FDA-approved repurposed drugs like Remdesivir, the first and foremost steps aimed towards the possible control and minimization of community transmission of the virus include social distancing, self-realization, and self-health care. In this review paper, we discussed and summarized various approaches and methodologies adopted and proposed by researchers all over the globe to help with the management of this zoonotic outbreak by following repurposed approaches.

11.
Assay Drug Dev Technol ; 21(3): 110-125, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-37036476

RESUMO

A highly selective, sensitive, rugged, and rapid ultra high-performance liquid chromatography-tandem mass spectrometry method (UPLC-MS/MS) is optimized and validated for reliable quantification of atorvastatin (ATR) and its active metabolites, 2-hydroxy atorvastatin (2-ATR) and 4-hydroxy atorvastatin (4-ATR) in human plasma using atorvastatin-D5 (ATR-D5), 2-hydroxy atorvastatin-D5 (2-ATR-D5), and 4-hydroxy atorvastatin-D5 (4-ATR-D5) as deuterium-labeled internal standards (ISTDs), respectively. Isocratic mode chromatographic separation was used with a reverse-phase C18 Symmetry Shield (150 × 4.6 mm, 5.0 µm) column and a mobile phase of acetonitrile:2 mM ammonium formate (pH-3.0) [65:35%v/v] at a flow rate of 0.7 mL/min. Electrospray ionization technique with positive ion mode polarity was applied to achieve the best signal intensity and stable response. Solid-phase extraction by direct elution method was applied to extract the drugs from the plasma sample. The calibration curve range was validated from a concentration range of 0.500-250 ng/mL for ATR and 2-ATR and 0.200-20 ng/mL for 4-ATR. The within-batch and between-batch precision and accuracy were found to be consistent and reproducible for all the analytes across the validation. Extraction recoveries were >80% for all analytes and ISTDs. All peaks of analytes and the respective ISTDs were eluted within 5.2 min. In this validated method, selective multivariate analytical approaches were utilized such as best fit linearity range for different strength formulations, preventive measures for in vivo and ex vivo autodegradation of metabolites, and shorter analysis time. This validated method can be useful for challenging quantification of ATR and its active metabolites for therapeutic drug monitoring and in high-throughput clinical study sample analysis.


Assuntos
Espectrometria de Massas em Tandem , Humanos , Atorvastatina , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia Líquida/métodos , Espectrometria de Massas em Tandem/métodos , Calibragem , Reprodutibilidade dos Testes
12.
Mini Rev Med Chem ; 23(22): 2130-2141, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37070437

RESUMO

INTRODUCTION: Cyclooxygenase (COX), in literature, known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme that is responsible for the formation of prostanoids, including thromboxane and prostaglandins from arachidonic acid. COX-1 does housekeeping activity, whereas COX- 2 induces inflammation. Continuous rise in COX-2 gives birth to chronic pain-associated disorders, i.e., arthritis, cardiovascular complications, macular degeneration, cancer, and neurodegenerative disorders. Despite their potent anti-inflammatory effects, the detrimental effects of COX-2 inhibitors coexist in healthy tissues. Non-preferential NSAIDs cause gastrointestinal discomfort, whereas selective COX-2 inhibitors exert higher cardiovascular risk and renal impairment on chronic use. METHODS: This review paper covers key patents published between 2012-2022 on NSAIDs and coxibs, highlighting their importance, mechanism of action, and patents related to formulation and drug combination. So far, several drug combinations with NSAIDS have been used in clinical trials to treat chronic pain besides combating the side effects. CONCLUSION: Emphasis has been given on the formulation, drug combination, administration routesmodification, and alternative routes, i.e., parenteral, topical, and ocular DEPOT, improving its riskbenefit ratio of NSAIDs to improvise their therapeutic availability and minimize the adverse effects. Considering the wide area of research on COX-2 and ongoing studies, and future scope of view for the better use of the NSAIDs in treating debilitating disease-associated algesia.

13.
Fitoterapia ; 167: 105492, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-36996945

RESUMO

Genus Leucas (family Lamiaceae) has been used as the traditional medicine for the treatment of a variety of disorders like skin diseases, diabetes, rheumatic pain, wounds, snake bites, etc. Several species of genus Leucas have been explored for their pharmacological activities and found to possess diverse properties like antimicrobial, antioxidant, anti-inflammatory, cytotoxic and anticancer, antinociceptive, antidiabetic, antitussive, wound healing, phytotoxic, etc. Phytochemical investigations of the different plant parts of Genus Leucas have revealed the presence of phytochemicals including terpenoids, flavonoids, lignans, phenolic glycosides, sterols, and essential oils. Terpenoids have been obtained as the major components of the isolated compounds and could be used as the marker compounds for the genus Leucas. The traditional uses of Leucas spp. have been established scientifically and were shown due to the presence of different phytochemicals. Although the pharmacological activities of Leucas plants have been well-documented, further studies are needed to fully understand their mechanisms of action and clinical applications. In conclusion, the phytochemistry and pharmacological activity of genus Leucas make it a promising source of natural products for drug discovery and development. The present review aims to provide a comprehensive note on the phytochemistry and pharmacological properties of the genus Leucas.


Assuntos
Lamiaceae , Medicina Tradicional , Estrutura Molecular , Fitoterapia , Preparações de Plantas/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais , Etnofarmacologia
14.
J Biomol Struct Dyn ; 41(22): 13314-13331, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36724473

RESUMO

A cell surface bile acid receptor TGR5 being considered as a novel target for Type II diabetes found to be expressed in various tissues. A major role for TGR5 is to maintain blood sugar levels and increase in energy expenditure. These benefits make it a potential candidate for the treatment of type 2 diabetes, obesity and other metabolic disorder. To date, many novel TGR5 agonists have been synthesized and evaluated in the literature, but very few in silico computational studies have been reported. The discovery of a high-resolution crystal structure of TGR5 in 2020 provides an excellent opportunity for computational screening of potential agonists. In this study, we, therefore, aim to search novel, less toxic TGR5 agonists by iteratively analyzing molecular docking against TGR5 (PDB ID: 7CFN) by means of structure-based virtual screening. The docking score of the designed coumarin derivatives that have been docked successfully varies between -9.4 and -9.0 kcal/mol. The molecular docking and ADMET profile examinations of compounds D1, D5 and D15 revealed that these have a strong affinity for the active site residues of TGR5. In addition, molecular dynamics simulation (MDS) studies have shown the stability of compounds that bind to TGR5. It can be summarized that designed coumarin derivatives seem to have promising activity as TGR5 agonists.Communicated by Ramaswamy H. Sarma.


Assuntos
Diabetes Mellitus Tipo 2 , Simulação de Dinâmica Molecular , Humanos , Simulação de Acoplamento Molecular , Diabetes Mellitus Tipo 2/tratamento farmacológico , Cumarínicos
15.
Indian J Clin Biochem ; 38(2): 182-192, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35756691

RESUMO

COVID-19, a global pandemic that led to increased morbidity and mortality worldwide since its outcome at the end of the year 2019. A newly discovered variant of severe acute respiratory distress syndrome coronavirus-2 (SARS-CoV-2) was the arbitrator for spreading the syndrome by droplet transmission causing multi-organ failure in many occasions. A post-infection-pro-diabetic disposition was found evident in this study with the persistence of hepato-pancreatic aberrations in respect of reference range of tissue specific bio-markers in hospital admitted COVID-19 cases. The results of this study show that hyperglycemia is a risk factor in precipitating disease oriented complications to the patients with COVID-19 disease. A post-infection follow- up on glycemic-index and related complexities is a vital need to the COVID-19 infected convalescent subjects. Implementation of guidelines on social measure and awareness of anti-viral interventions may be the only way to prevent COVID-19 transmission.

16.
Hum Cell ; 36(1): 98-120, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36334180

RESUMO

Cancer immunotherapy utilizes the immune system and its wide-ranging components to deliver anti-tumor responses. In immune escape mechanisms, tumor microenvironment-associated soluble factors and cell surface-bound molecules are mainly accountable for the dysfunctional activity of tumor-specific CD8+ T cells, natural killer (NK) cells, tumor associated macrophages (TAMs) and stromal cells. The myeloid-derived suppressor cells (MDSCs) and Foxp3+ regulatory T cells (Tregs), are also key tumor-promoting immune cells. These potent immunosuppressive networks avert tumor rejection at various stages, affecting immunotherapies' outcomes. Numerous clinical trials have elucidated that disruption of immunosuppression could be achieved via checkpoint inhibitors. Another approach utilizes enzymes that can restore the body's potential to counter cancer by triggering the immune system inhibited by the tumor microenvironment. These immunotherapeutic enzymes can catalyze an immunostimulatory signal and modulate the tumor microenvironment via effector molecules. Herein, we have discussed the immuno-metabolic roles of various enzymes like ATP-dephosphorylating ectoenzymes, inducible Nitric Oxide Synthase, phenylamine, tryptophan, and arginine catabolizing enzymes in cancer immunotherapy. Understanding the detailed molecular mechanisms of the enzymes involved in modulating the tumor microenvironment may help find new opportunities for cancer therapeutics.


Assuntos
Células Supressoras Mieloides , Neoplasias , Humanos , Linfócitos T CD8-Positivos , Imunoterapia , Neoplasias/terapia , Tolerância Imunológica , Microambiente Tumoral
17.
Curr Res Toxicol ; 3: 100057, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36504921

RESUMO

Bartogenic acid (BA), an active pentacyclic triterpenoid, has been reported for anti-diabetic, anti-inflammatory, anti-arthritic, anti-cancer, and anti-tumor activity. However, toxicity profiling of BA has not been reported till date. Hence, this study is designed to evaluate the single dose (12.5, 25, 50 and 100 mg/kg) and repeated dose (1.5, 6, and 24 mg/kg) intravenous toxicity of BA in BALB/c mice. Control group received vehicle. In single dose toxicity study, two mortalities were observed at 100 mg/kg of BA whereas lower doses were well tolerated. In repeated dose toxicity study, no mortality was observed. 1.5 mg/kg of BA was well tolerated in mice of both sexes. At 6 mg/kg of BA, female mice showed significant reduction in the body weight as compared to the control group however no significant change was observed in male mice. 24 mg/kg of BA showed significant reduction in the body weight in mice of both sexes. Further, these mice showed significant change in the relative organ weight. However, no toxicologically relevant changes were observed in hematology, biochemistry, and histopathology. Based on the findings, No-Observed-Adverse-Effect-Level (NOAEL) for BA were found to be<24 mg/kg for male mice and<6 mg/kg for female mice.

18.
Pharm Pat Anal ; 11(6): 199-212, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36354044

RESUMO

Insulin, on oral administration, is very troublesome because of its limited bioavailability. The evolution of oral insulin delivery formulations is greatly desired for non-invasive therapy by overcoming its low bioavailability, GIT enzymatic deactivation, poor lipophilicity and low stability. Different approaches have been proposed to boost oral insulin bioavailability in insulin-delivery systems and emerging effective therapies by using nanoparticle formulation, nanocapsid, modified chitosan particles, polydopamine microcapsules and nanoliposomes. The present review includes patents and patent applications that were published between 2017 and January 2022.


Assuntos
Quitosana , Nanopartículas , Insulina , Sistemas de Liberação de Medicamentos , Administração Oral
19.
Data Brief ; 43: 108421, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35811649

RESUMO

The data in this article described quantitative values of fractional anisotropy (FA) and apparent diffusion coefficient (ADC) for 23 (46 extremities) normal healthy males and females, for 46 patients with bilateral diabetic peripheral neuropathy. 1.5 Tesla (T) MR System Multiva - Philips magnets (Baltimore, Netherland, Holland) imaging with axial T1WSE, sagittal T2WSE and STIR sequences by means of diffusion weighted neurography b values of 0 and 800 s/mm2. The data obtained as FA and ADC values in healthy adults and patient population can be referred by researchers, clinicians for early diagnosis, to determine intervention effectiveness and patient management.

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