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1.
Drug Res (Stuttg) ; 74(6): 269-279, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38968950

ABSTRACT

Every year, the World Health Organization reports 500,000 new cases of drug-resistant tuberculosis (TB), which poses a serious global danger. The increased number of XDR-TB and MDR-TB cases reported worldwide necessitates the use of new therapeutic approaches. The main issues with the antitubercular medications now in use for the treatment of multidrug-resistant tuberculosis are their poor side effect profile, reduced efficacy, and antimicrobial resistance. One possible remedy for these problems is bedaquiline. The need for better treatment strategies is highlighted by the strong minimum inhibitory concentrations that bedaquiline (BDQ), a novel anti-TB medicine, exhibits against both drug-resistant and drug-susceptible TB. Bedaquiline may be able to help with these problems. Bedaquiline is a medication that is first in its class and has a distinct and particular mode of action. Bedaquiline is an ATP synthase inhibitor that is specifically directed against Mycobacterium tuberculosis and some nontuberculous mycobacteria. It is metabolized by CYP3A4. Bedaquiline preclinical investigations revealed intralesional drug biodistribution. The precise intralesional and multi-compartment pharmacokinetics of bedaquiline were obtained using PET bioimaging and high-resolution autoradiography investigations. Reduced CFU counts were observed in another investigation after a 12-week course of therapy. Meta-analyses and systematic reviews of phase II trials on bedaquiline's efficacy in treating drug-resistant tuberculosis in patients reported higher rates of cure, better culture conversion, and lower death rates when taken in conjunction with a background regimen. Here is a thorough medication profile for bedaquiline to aid medical professionals in treating individuals with tuberculosis.


Subject(s)
Antitubercular Agents , Diarylquinolines , Mycobacterium tuberculosis , Tuberculosis, Multidrug-Resistant , Tuberculosis, Pulmonary , Diarylquinolines/therapeutic use , Diarylquinolines/pharmacokinetics , Humans , Antitubercular Agents/therapeutic use , Antitubercular Agents/pharmacokinetics , Antitubercular Agents/pharmacology , Antitubercular Agents/administration & dosage , Tuberculosis, Multidrug-Resistant/drug therapy , Tuberculosis, Pulmonary/drug therapy , Tuberculosis, Pulmonary/microbiology , Mycobacterium tuberculosis/drug effects , Microbial Sensitivity Tests , Animals
2.
Curr Drug Metab ; 2024 May 16.
Article in English | MEDLINE | ID: mdl-38757314

ABSTRACT

Curcumin is a naturally occurring polyphenolic compound extracted from the rhizomes of Curcuma longa, commonly known as turmeric. It has been used for centuries in traditional medicine and is gaining increasing attention in modern medicine owing to its potential therapeutic benefits. Psoriasis is a chronic inflammatory disease characterized by red scaly patches on the skin. Curcumin has been found to be effective in treating psoriasis by inhibiting the activity of various enzymes and proteins involved in the inflammation and proliferation of psoriatic skin cells. Nanogel preparation of curcumin has been found to be a promising approach for the delivery of compounds to treat psoriasis. Nanogels are composed of biocompatible and biodegradable crosslinked hydrogels. The nanogel formulation of curcumin increases its solubility, stability, and bioavailability, indicating that a lower dose is needed to achieve the same therapeutic effect. This review article suggests that the nanogel preparation of curcumin can be a better alternative for psoriasis treatment as it increases the bioavailability and stability of curcumin and also reduces the required dosage. This study suggests that curcumin nanogel preparations are promising alternatives to traditional psoriasis treatments and could potentially be used as a more effective and safe treatment option. This article highlights the need for further research to fully understand the potential of curcumin nanogel preparations for psoriasis treatment in humans.

3.
ACS Appl Mater Interfaces ; 16(13): 16788-16799, 2024 Apr 03.
Article in English | MEDLINE | ID: mdl-38520339

ABSTRACT

Smart wearables with the capability for continuous monitoring, perceiving, and understanding human tactile and motion signals, while ensuring comfort, are highly sought after for intelligent healthcare and smart life systems. However, concurrently achieving high-performance tactile sensing, long-lasting wearing comfort, and industrialized fabrication by a low-cost strategy remains a great challenge. This is primarily due to critical research gaps in novel textile structure design for seamless integration with sensing elements. Here, an all-in-one biaxial insertion knit architecture is reported to topologically integrate sensing units within double-knit loops for the fabrication of a large-scale tactile sensing textile by using low-cost industrial manufacturing routes. High sensitivity, stability, and low hysteresis of arrayed sensing units are achieved through engineering of fractal structures of hierarchically patterned piezoresistive yarns via blistering and twisting processing. The as-prepared tactile sensing textiles show desirable sensing performance and robust mechanical property, while ensuring excellent conformability, tailorability, breathability (288 mm s-1), and moisture permeability (3591 g m-2 per day) for minimizing the effect on wearing comfort. The multifunctional applications of tactile sensing textiles are demonstrated in continuously monitoring human motions, tactile interactions with the environment, and recognizing biometric gait. Moreover, we also demonstrate that machine learning-assisted sensing textiles can accurately predict body postures, which holds great promise in advancing the development of personalized healthcare robotics, prosthetics, and intelligent interaction devices.


Subject(s)
Robotics , Wearable Electronic Devices , Humans , Textiles , Motion , Touch
4.
Curr Diabetes Rev ; 20(2): e270423216247, 2024.
Article in English | MEDLINE | ID: mdl-37102490

ABSTRACT

Diabetes is a chronic condition that has an impact on a huge part of the world. Both animals and humans have been demonstrated to benefit from natural goods, and organisms (animals, or microbes). In 2021, approximately 537 million adults (20-79 years) are living with diabetes, making it the one of the biggest cause of death worldwide. Various phytoconstituent preserved ß- cells activity helps to prevent the formation of diabetes problems. As a result, ß-cells mass and function are key pharmaceutical targets. The purpose of this review is to provide an overview of flavonoids' effects on pancreatic ß-cells. Flavonoids have been demonstrated to improve insulin release in cell lines of isolated pancreatic islets and diabetic animal models. Flavonoids are thought to protect ß-cells by inhibiting nuclear factor-κB (NF-κB) signaling, activating the phosphatidylinositol 3-kinase (PI3K) pathway, inhibiting nitric oxide production, and lowering reactive oxygen species levels. Flavonoids boost ß-cells secretory capacity by improving mitochondrial bioenergetic function and increasing insulin secretion pathways. Some of the bioactive phytoconstituents such as S-methyl cysteine sulfoxides stimulate insulin synthesis in the body and increase pancreatic output. The berberine increased insulin secretion in the HIT-T15 and Insulinoma 6 (MIN6) mouse cell line. Epigallocatechin-3-Gallate protects against toxicity accrued by cytokines, reactive oxygen species (ROS), and hyperglycemia. Quercetin has been proven to boost insulin production by Insulinoma 1 (INS-1) cells and also protect cell apoptosis. Overall flavonoids have beneficial effects on ß-cells by prevented their malfunctioning or degradation and improving synthesis or release of insulin from ß-cells.


Subject(s)
Diabetes Mellitus , Insulin-Secreting Cells , Insulinoma , Pancreatic Neoplasms , Mice , Animals , Humans , Insulin/metabolism , Flavonoids/pharmacology , Flavonoids/therapeutic use , Flavonoids/metabolism , Reactive Oxygen Species/metabolism , Phosphatidylinositol 3-Kinases/metabolism , Insulin-Secreting Cells/metabolism , NF-kappa B , Diabetes Mellitus/drug therapy , Diabetes Mellitus/metabolism , Apoptosis
5.
Biomater Sci ; 12(2): 218-251, 2024 Jan 16.
Article in English | MEDLINE | ID: mdl-38108438

ABSTRACT

Microfluidic technologies have garnered significant attention due to their ability to rapidly process samples and precisely manipulate fluids in assays, making them an attractive alternative to conventional experimental methods. With the potential for revolutionary capabilities in the future, this concise review provides readers with insights into the fascinating world of microfluidics. It begins by introducing the subject's historical background, allowing readers to familiarize themselves with the basics. The review then delves into the fundamental principles, discussing the underlying phenomena at play. Additionally, it highlights the different aspects of microfluidic device design, classification, and fabrication. Furthermore, the paper explores various applications, the global market, recent advancements, and challenges in the field. Finally, the review presents a positive outlook on trends and draws lessons to support the future flourishing of microfluidic technologies.


Subject(s)
Lab-On-A-Chip Devices , Microfluidics
6.
Article in English | MEDLINE | ID: mdl-37867264

ABSTRACT

Diabetic neuropathy (DN) is a common and debilitating complication of diabetes mellitus that affects the peripheral nerves and causes pain, numbness, and impaired function. The pathogenesis of DN involves multiple molecular mechanisms, such as oxidative stress, inflammation, and pathways of advanced glycation end products, polyol, hexosamine, and protein kinase C. Phytochemicals are natural compounds derived from plants that have various biological activities and therapeutic potential. Flavonoids, terpenes, alkaloids, stilbenes, and tannins are some of the phytochemicals that have been identified as having protective potential for diabetic neuropathy. These compounds can modulate various cellular pathways involved in the development and progression of neuropathy, including reducing oxidative stress and inflammation and promoting nerve growth and repair. In this review, the current evidence on the effects of phytochemicals on DN by focusing on five major classes, flavonoids, terpenes, alkaloids, stilbenes, and tannins, are summarized. This compilation also discusses the possible molecular targets of numerous pathways of DN that these phytochemicals modulate. These phytochemicals may offer a promising alternative or complementary approach to conventional drugs for DN management by modulating multiple pathological pathways and restoring nerve function.

7.
Phytother Res ; 37(11): 5058-5079, 2023 Nov.
Article in English | MEDLINE | ID: mdl-37528656

ABSTRACT

The immune system is one of the essential defense mechanisms. Immune system inadequacy increases the risk of infections and cancer diseases, whereas over-activation of the immune system causes allergies or autoimmune disorders. Immunomodulators have been used in the treatment of immune-related diseases. There is growing interest in using herbal medicines as multicomponent agents to modulate the complex immune system in immune-related diseases. Many therapeutic phytochemicals showed immunomodulatory effects by various mechanisms. This mechanism includes stimulation of lymphoid cell, phagocytosis, macrophage, and cellular immune function enhancement. In addition increased antigen-specific immunoglobulin production, total white cell count, and inhibition of TNF-α, IFN-γ, NF-kB, IL-2, IL-6, IL-1ß, and other cytokines that influenced the immune system. This review aims to overview, widely investigated plant-derived phytoconstituents by targeting cells to modulate cellular and humoral immunity in in vivo and in vitro. However, further high-quality research is needed to confirm the clinical efficacy of plant-based immunomodulators.


Subject(s)
Cytokines , Immunologic Factors , Immunologic Factors/pharmacology , Adjuvants, Immunologic/pharmacology , Immunity, Humoral , Immune System
8.
Curr Issues Mol Biol ; 45(7): 5752-5764, 2023 Jul 10.
Article in English | MEDLINE | ID: mdl-37504279

ABSTRACT

With more than a million deaths each year, breast cancer is the top cause of death in women. Around 70% of breast cancers are hormonally responsive. Although several therapeutic options exist, cancer resistance and recurrence render them inefficient and insufficient. The major key reason behind this is the failure in the regulation of the cell death mechanism. In addition, ROS was also found to play a major role in this problem. The therapeutic benefits of Smac mimetic compound (SMC) BV6 on MCF7 were examined in the current study. Treatment with BV6 reduces viability and induces apoptosis in MCF7 breast cancer cells. BV6 suppresses autophagy and has demonstrated a defensive role in cancer cells against oxidative stress caused by H2O2. Overall, the present investigation shows that SMC has therapeutic and cytoprotective potential against oxidative stress in cancer cells. These Smac mimetic compounds may be used as anti-cancer drugs as well as antioxidants alone or in conjunction with other commonly used antioxidants.

9.
Curr Hypertens Rev ; 19(2): 79-92, 2023.
Article in English | MEDLINE | ID: mdl-37309769

ABSTRACT

BACKGROUND: Medicinal plants have been found beneficial in the control and therapy of many ailments as they contain bioactive compounds, and many of them are used as precursors in the biosynthesis of natural medicines. Diuretics are used as a primary treatment in patients with edema associated with liver cirrhosis and kidney diseases, hyperkalemia, hypertension, heart failure, or renal failure. Furthermore, they are also used to increase the excretion of sodium and reduce blood volume. Due to various adverse events associated with synthetic diuretics, there is a need to investigate alternate plant-based bioactive components that have effective diuretic activity with minimal side effects. OBJECTIVE: This review compiled the reported bioactive compounds from different plant sources along with their mechanisms of diuretic activity. METHODS: Different sources were used to collect information regarding herbal plants with therapeutic value as diuretics. These included published peer-reviewed journal articles, scholarly articles from StatPearls, and search engines like Google Scholar, PubMed, Scopus, Springer, ScienceDirect, Wiley, etc. Results: In this review, it was found that flavonoids like rutin, acacetin, naringenin, etc. showed significant diuretic activity in experimental models by various mechanisms, but mostly by blocking the sodium-potassium-chloride co-transporter, while some bioactive compounds showed diuretic actions via other mechanisms as well. CONCLUSION: Research on clinical trials of these isolated bioactive compounds needs to be further conducted. Thus, this review provides an understanding of the potential diuretic bioactive compounds of plants for further research and pharmaceutical applications.


Subject(s)
Hypertension , Kidney Diseases , Humans , Diuretics/adverse effects , Diuresis , Hypertension/diagnosis , Hypertension/drug therapy , Hypertension/chemically induced , Sodium/therapeutic use
10.
Clin Ophthalmol ; 17: 693-700, 2023.
Article in English | MEDLINE | ID: mdl-36880022

ABSTRACT

Objective: To evaluate the long-term visual acuity and retinal thickness changes after pars plana vitrectomy (PPV) for idiopathic epiretinal membranes (ERM). Methods: We performed a retrospective analysis of 72 patients who underwent PPV for idiopathic ERM in a tertiary hospital over 5 consecutive years. The main outcome measurement was change in visual acuity and macular thickness as recorded with optical coherence tomography (OCT). Results: Medical records of 239 patients with a diagnosis of ERM who underwent PPV with or without internal limiting membrane (ILM) peeling were reviewed; of these, 72 patients with idiopathic ERM were included in the final analysis. All patients completed at least one year of follow-up, and 23 patients (30%) had 5 or more years of follow-up. The mean preoperative best corrected visual acuity (BCVA) was 20/65, and mean preoperative central macular thickness (CMT) on OCT was 434 microns (µm). Mean postoperative BCVA and CMT at one year were 20/40 and 303 µm, respectively (p<0.0001). A total of 42 patients (58%) improved by 2 or more lines; BCVA and CMT continued to improve postoperatively for up to 5 years of the follow-up period. There was no significant difference in BCVA or CMT between phakic and pseudophakic patients, and ILM peeling was performed in 67% of patients. Improved BCVA at 1 year was associated with younger age (p<0.0001) and ILM peeling (p=0.020). Conclusion: PPV is an effective treatment for idiopathic ERM, and ILM peel may be of benefit. BCVA continues to improve up to 2 years and beyond after surgery regardless of the duration of symptoms.

11.
J Basic Clin Physiol Pharmacol ; 34(3): 291-310, 2023 May 01.
Article in English | MEDLINE | ID: mdl-36989026

ABSTRACT

Uterine fibroids (UFs), leiomyomas or myomas, are a type of malignancy that affects the smooth muscle of the uterus, and it is most commonly detected in women of reproductive age. Uterine fibroids are benign monoclonal growths that emerge from uterine smooth muscle cells (myometrium) as well as fibroblasts. Uterine fibroid symptoms include abnormal menstrual bleeding leading to anaemia, tiredness, chronic vaginal discharge, and pain during periods. Other symptoms include protrusion of the abdomen, pain during intercourse, dysfunctions of bladder/bowel leading to urinary incontinence/retention, pain, and constipation. It is also associated with reproductive issues like impaired fertility, conceiving complications, and adverse obstetric outcomes. It is the leading cause of gynaecological hospitalisation in the American subcontinent and a common reason for the hysterectomy. Twenty-five percent of the reproductive women experience the symptoms of uterine fibroids, and among them, around 25% require hospitalization due to the severity of the disease. The frequency of the disease remains underestimated as many women stay asymptomatic and symptoms appear gradually; therefore, the condition remains undiagnosed. The exact frequency of uterine fibroids varies depending on the diagnosis, and the population investigated; nonetheless, the incidence of uterine fibroids in reproductive women ranges from 5.4 percent to 77 percent. The uterine fibroid treatment included painkillers, supplementation with iron, vitamin D3, birth control, hormone therapy, gonadotropin-releasing hormone (GnRH) agonists, drugs modulating the estrogen receptors, and surgical removal of the fibroids. However, more research needed at the level of gene to get a keen insight and treat the disease efficiently.


Subject(s)
Leiomyoma , Uterine Neoplasms , Pregnancy , Female , Humans , Uterine Neoplasms/therapy , Uterine Neoplasms/drug therapy , Leiomyoma/therapy , Leiomyoma/drug therapy , Uterus , Hysterectomy , Pain
12.
Curr Drug Res Rev ; 15(3): 199-206, 2023.
Article in English | MEDLINE | ID: mdl-36824005

ABSTRACT

Oral disintegrating tablets (ODT) offer an attractive choice for Gastroesophageal Reflux Disease (GERD) patients suffering from dysphagia. In chronic condition, GERD patient suffers from severe erosive esophagitis. Thus patients feel difficulty and pain during swallowing, which results in patient in-compliance toward medication of tablets or capsules- especially in geriatrics and pediatric patients. These symptoms of GERD patients have attracted the formulation scientists in improving the formulation methodology for such patients. Orally disintegrating tablets could increase the therapeutic impact and drug compliance in these patients. The aim of this compilation is to provide a more convenient way to develop an oral disintegrating drug delivery system of proton pump inhibitors in patients suffering from odynophagia, associated with chronic Gastroesophageal Reflux Disease (GERD). Oral disintegrating tablets (ODT), when placed on the tongue, can quickly disintegrate and release the medicament. It later dissolves or disperses in saliva without any additional water. The saliva containing drug can easily be swallowed and descends into the stomach leading to maximum absorption from the mouth, throat, and upper esophagus. The patient compliance and bio-availability of Oral disintegrating tablets (ODT) are high compared to other conventional tablets.


Subject(s)
Deglutition Disorders , Gastroesophageal Reflux , Humans , Child , Proton Pump Inhibitors/therapeutic use , Gastroesophageal Reflux/drug therapy , Tablets/therapeutic use , Medication Adherence
13.
Sci Rep ; 13(1): 1795, 2023 Jan 31.
Article in English | MEDLINE | ID: mdl-36720948

ABSTRACT

Coil tubing (CT) is widely regarded as one of the most effective servicing tools for dealing with a variety of oil and gas production issues, and it is also commonly used for oil well workover operations in India's upper Assam basin. The current work considers QT 800 to be the CT material used for actual oil well operations. With reference to actual operations carried out in some of the oil wells in the upper Assam basin, the current research analyses the limitations of CTs (QT 800, QT 900, and QT 1000) based on developing limit curves that can depict the operating limit and infer CT failure probability. This study also includes fatigue analysis to determine the likelihood of damage from hot oil circulation, water injection, and nitrogen shot operations while performing them using the CTs (QT 700, QT 800, QT 900, and QT 1000). The current work adopts the methodology of CT assessment based on a computational model built in MATLAB with respect to different oil well parameters in the upper Assam basin. This study takes an innovative approach by taking downhole temperature into account when determining the CT limit for QT 800, which signifies novelty in the current work. According to the computational analysis used in the study on CT limits, mechanical strain, thermal strain, and the combined strain of the CT material all affect CT elongation. This observation was often found to be a research gap in different research works as this aspect in previous studies was not considered while analysing CT operations. The findings of the present study highlight and draw the conclusion that temperature variations in the well and the CTU's circulating fluid contribute linearly to CT strain. CT's working limit diminishes with increasing internal and external pressure and diametrical growth, which eventually causes fatigue damage.

15.
Drug Res (Stuttg) ; 73(1): 23-29, 2023 Jan.
Article in English | MEDLINE | ID: mdl-36138544

ABSTRACT

Cardiac dysfunction such as cirrhotic cardiomyopathy is more common in liver cirrhosis related disorders including primary biliary cholangitis or biliary cirrhosis and primary sclerosing cholangitis. Bile duct ligation (BDL) is an effective model of biliary cholestasis, producing oxidative damage and fibrosis. This research was designed to evaluate the effect of Lupeol and Naringin and its combination on bile duct ligation induced cardiac injury in rats. For pharmacological evaluation, rats were randomly divided into seven groups; intrahepatic cholestasis induced by ligation of the bile duct might lead to cirrhotic cardiomyopathy. The results were analyzed by physical, biochemical and histological examination. The Lupeol (100 mg/kg, p.o.), Naringin (100 mg/kg, p.o.) and its combination (100 mg/kg each) treated group significantly improved physical infarct size, biochemical (Nitrite, SOD, CAT, and GSH) and histological (heart tissue- mitochondrial function/integrity and fibrosis) alterations occurs due to BDL-ligation. This study was concluded that oral administration of Lupeol, Naringin, and its combination has a curative potential against BDL-induced cardiac injury in rats by reducing oxidative stress and inflammatory reactions, resulting in reduced heart necrosis/myocardial infarction and increased myocardial activity. It also inhibits cardiac damage in the rat heart, these effects may be linked to the NO level (eNOS) is increased and the inactivation of the NF-kB-p65 expression pathways.This study also provides new insights into the development of lupeol and Naringin combination that can be used as supportive therapy for cardiovascular diseases.


Subject(s)
Liver Diseases , NF-kappa B , Animals , Rats , Bile Ducts/surgery , Bile Ducts/metabolism , Bile Ducts/pathology , Fibrosis , Ligation , Liver/metabolism , Liver Cirrhosis/metabolism , NF-kappa B/metabolism , NF-kappa B/pharmacology , Nitrites , Oxidative Stress
16.
Environ Sci Pollut Res Int ; 30(1): 884-898, 2023 Jan.
Article in English | MEDLINE | ID: mdl-35907074

ABSTRACT

Arsenic (As) traces have been reported worldwide in vegetables and crops cultivated in As-polluted soils. Being carcinogenic, the presence of As in edibles is of great concern as it ultimately reaches humans and animals through the food chain. Besides, As toxicity adversely affects the growth, physiology, metabolism, and productivity of crops. In the present study, Trigonella foenum-graecum (Fenugreek) was exposed to the As stress (0, 50, 100, and 150 µM sodium arsenate) for a week. Further, evaluation of As accumulation in roots and shoots, magnitude and visualization of oxyradicals, and thiol-based defence offered by Fenugreek was assessed. The root and leaf accumulated 258-453 µg g-1 dry wt (DW) and 81.4-102.1 µg g-1 DW of As, respectively. An arsenic-mediated decline in the growth index and increase in oxidative stress was noted. Arsenic stress modulated the content of thiol compounds; especially cysteine content increased from 0.36 to 0.43 µmole g-1 FW protein was noted. Random Amplified Polymorphic DNA (RAPD)-based analysis showed DNA damage in As-treated plants. Health risk assessment parameters showed that As concentration in the consumable plant shoot was below the critical hazard level (hazard quotient < 1). Moreover, T. foenum-graecum showed varied responses to As-induced oxidative stress with applied concentrations (150 µM being more toxic than lower concentrations). In addition, the RAPD profile and level of thiol compounds were proved significant biomarkers to assess the As toxicity in plants. The conclusion of this study will help users of fenugreek to have a clue and create awareness regarding the consumption.


Subject(s)
Arsenic , Trigonella , Humans , Animals , Arsenic/toxicity , Arsenic/metabolism , Random Amplified Polymorphic DNA Technique , Plant Extracts/pharmacology , DNA Damage , Sulfhydryl Compounds/metabolism
17.
ACS Omega ; 7(50): 46156-46173, 2022 Dec 20.
Article in English | MEDLINE | ID: mdl-36570189

ABSTRACT

Type 2 diabetes mellitus leads to metabolic impairment caused by insulin resistance and hyperglycemia, giving rise to chronic diabetic complications and poor disease prognosis. The heartwood of Pterocarpus marsupium has been used in Ayurveda for a long time, and we sought to find the actual mechanism(s) driving its antidiabetic potential. Methanol was used to prepare the extract using a Soxhlet extraction, and the identification of metabolites was performed by thin-layer chromatography (TLC) and ultraperformance-liquid chromatography and mass spectroscopy (UP-LCMS). The antioxidant potential of methanolic heartwood extract of Pterocarpus marsupium MHPM was determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and a reducing power assay. The α-amylase and α-glucosidase enzyme inhibitory potential of MHPM were investigated for their antidiabetic activity against acarbose. TLC-MS-bioautography was performed to identify the compounds responsible for possible antioxidant and antidiabetic activities. Moreover, targeting protein tyrosine phosphatase 1B (PTP1B), a key regulator of insulin resistance, by identified metabolites from MHPM through molecular docking and all-atom molecular dynamics (MD) simulations was also undertaken, suggesting its potential as an antidiabetic herb. The IC50 of free-radical scavenging activity of MHPM against DPPH was 156.342 ± 10.70 µg/mL. Further, the IC50 values of MHPM in α-amylase and α-glucosidase enzymatic inhibitions were 158.663 ± 10.986 µg/mL and 180.21 ± 11.35 µg/mL, respectively. TLC-MS-bioautography identified four free radical scavenging metabolites, and vanillic acid identified by MS analysis showed both free radical scavenging activity and α-amylase inhibitory activity. Among the identified metabolites from MHPM, epicatechin showed significant PTP1B docking interactions, and its MD simulations revealed that PTP1B forms a stable protein-ligand complex with epicatechin throughout the progression, which indicates that epicatechin may be used as a promising scaffold in the development of the antidiabetic drug after isolation from Pterocarpus marsupium. Overall, these findings imply that Pterocarpus marsupium is a source of valuable metabolites that are accountable for its antioxidant and antidiabetic properties.

18.
Metabolites ; 12(10)2022 Oct 05.
Article in English | MEDLINE | ID: mdl-36295849

ABSTRACT

Diabetes mellitus leads to cellular damage and causes apoptosis by oxidative stress. Heartwood extract of Pterocarpus marsupium has been used in Ayurveda to treat various diseases such as leprosy, diabetes, asthma, and bronchitis. In this study, we worked out the mechanism of the antidiabetic potential of methanolic heartwood extract of Pterocarpus marsupium (MPME). First, metabolic profiling of MPME was done using gas chromatography-mass spectrometry (GCMS), ultra-performance liquid chromatography-mass spectroscopy (UPLC-MS), and high-performance thin-layer chromatography (HPTLC) to identify phenols, flavonoids, and terpenoids in MPME. Biological studies were carried out in vitro using the HepG2 cell line. Many antidiabetic compounds were identified including Quercetin. Methanolic extract of MPME (23.43 µg/mL-93.75 µg/mL) was found to be safe and effective in reducing oxyradicals in HepG2 cells. A concentration of 93.75 µg/mL improved glucose uptake efficiently. A significant decrease in oxidative stress, cell damage, and apoptosis was found in MPME-treated HepG2 cells. The study suggests that the heartwood of Pterocarpus marsupium offers good defense in HepG2 cells against oxidative stress and improves glucose uptake. The results show the significant antidiabetic potential of MPME using a HepG2 cell model. The effect seems to occur by reducing oxidative stress and sensitizing the cells towards glucose uptake, hence lowering systemic glucose levels, as well as rescuing ROS generation.

19.
Plants (Basel) ; 11(12)2022 Jun 13.
Article in English | MEDLINE | ID: mdl-35736711

ABSTRACT

Forty-day-old Brassica juncea (var. Pusa Jai Kisan) plants were exposed to arsenic (As, 250 µM Na2HAsO4·7H2O) stress. The ameliorative role of ferrous sulfate (2 mM, FeSO4·7H2O, herein FeSO4) was evaluated at 7 days after treatment (7 DAT) and 14 DAT. Whereas, As induced high magnitude oxidative stress, FeSO4 limited it. In general, As decreased the growth and photosynthetic parameters less when in the presence of FeSO4. Furthermore, components of the antioxidant system operated in better coordination with FeSO4. Contents of non-protein thiols and phytochelatins were higher with the supply of FeSO4. Blue-Native polyacrylamide gel electrophoresis revealed an As-induced decrease in almost every multi-protein-pigment complex (MPC), and an increase in PSII subcomplex, LHCII monomers and free proteins. FeSO4 supplication helped in the retention of a better stoichiometry of light-harvesting complexes and stabilized every MPC, including supra-molecular complexes, PSI/PSII core dimer/ATP Synthase, Cytochrome b6/f dimer and LHCII dimer. FeSO4 strengthened the plant defence, perhaps by channelizing iron (Fe) and sulfur (S) to biosynthetic and anabolic pathways. Such metabolism could improve levels of antioxidant enzymes, and the contents of glutathione, and phytochelatins. Important key support might be extended to the chloroplast through better supply of Fe-S clusters. Therefore, our results suggest the importance of both iron and sulfur to combat As-induced stress in the Indian mustard plant at biochemical and molecular levels through enhanced antioxidant potential and proteomic adjustments in the photosynthetic apparatus.

20.
Article in English | MEDLINE | ID: mdl-35562190

ABSTRACT

A wearable textile that is engineered to reflect incoming sunlight and allow the transmission of mid-infrared radiation simultaneously would have a great impact on the human body's thermal regulation in an outdoor environment. However, developing such a textile is a tough challenge. Using nanoparticle-doped polymer (zinc oxide and polyethylene) materials and electrospinning technology, we have developed a nanofabric with the desired optical properties and good applicability. The nanofabric offers a cool fibrous structure with outstanding solar reflectivity (91%) and mid-infrared transmissivity (81%). In an outdoor field test under exposure of direct sunlight, the nanofabric was demonstrated to reduce the simulated skin temperature by 9 °C when compared to skin covered by a cotton textile. A heat-transfer model is also established to numerically assess the cooling performance of the nanofabric as a function of various climate factors, including solar intensity, ambient air temperature, atmospheric emission, wind speed, and parasitic heat loss rate. The results indicate that the nanofabric can completely release the human body from unwanted heat stress in most conditions, providing an additional cooling effect as well as demonstrating worldwide feasibility. Even in some extreme conditions, the nanofabric can also reduce the human body's cooling demand compared with traditional cotton textile, proving this material as a feasible solution for better thermoregulation of the human body. The facile fabrication of such textiles paves the way for the mass adoption of energy-free personal cooling technology in daily life, which meets the growing demand for healthcare, climate change, and sustainability.

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