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1.
Drug Target Insights ; 18: 30-46, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38873988

RESUMEN

Aim: Researchers using herbs and natural products to find new drugs often prefer flavonoids because of their potential as antioxidants and anti-inflammatories. The planned review addressed baicalein research findings in detail. This manuscript provides a complete review of baicalein's potential pharmacological effects along with several molecular targets for better understanding of its therapeutic activities. Materials and methods: We targeted the review on in vitro and in vivo studies reported on baicalein. For this, the literature is gathered from the database available on search engines like PubMed, ScienceDirect, Scopus, and Google Scholar up to 21 December 2023. The keywords "Scutellaria baicalensis", "Oroxylum indicum", "Neuroprotective", "Cardioprotective", "Toxicity studies", and "Baicalein" were used to fetch the content. Results: Baicalein's molecular receptor binding approach has shown anticancer, antidiabetic, antimicrobial, antiaging, neuroprotective, cardioprotective, respiratory protective, gastroprotective, hepatic protective, and renal protective effects. The synergistic effects of this drug with other selective herbs are also contributed towards significant therapeutic potential. Conclusion: This systematic review article from a contemporary and scientific perspective offers fresh insight into S. baicalensis, O. indicum, and its bioactive component baicalein as a potential complementary medicine. Baicalein may be transformed into more efficacious and acceptable evidence-based medicine. However, we recommend more clinical and mechanistic approaches to confirm safety and efficacy of baicalein.

2.
Curr Pharm Des ; 30(1): 10-30, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38155468

RESUMEN

Metabolic syndrome (MetS) therapy with phytochemicals is an emerging field of study with therapeutic potential. Obesity, insulin resistance, high blood pressure, and abnormal lipid profiles are all components of metabolic syndrome, which is a major public health concern across the world. New research highlights the promise of phytochemicals found in foods, including fruits, vegetables, herbs, and spices, as a sustainable and innovative method of treating this illness. Anti-inflammatory, antioxidant, and insulin-sensitizing qualities are just a few of the many positive impacts shown by bioactive substances. Collectively, they alleviate the hallmark symptoms of metabolic syndrome by modulating critical metabolic pathways, boosting insulin sensitivity, decreasing oxidative stress, and calming chronic low-grade inflammation. In addition, phytochemicals provide a multimodal strategy by targeting not only adipose tissue but also the liver, skeletal muscle, and vascular endothelium, all of which have a role in the pathogenesis of MetS. Increasing evidence suggests that these natural chemicals may be useful in controlling metabolic syndrome as a complementary treatment to standard medication or lifestyle changes. This review article emphasizes the therapeutic potential of phytochemicals, illuminating their varied modes of action and their ability to alleviate the interconnected causes of metabolic syndrome. Phytochemical-based interventions show promise as a novel and sustainable approach to combating the rising global burden of metabolic syndrome, with the ultimate goal of bettering public health and quality of life.


Asunto(s)
Síndrome Metabólico , Plantas Medicinales , Humanos , Plantas Medicinales/química , Síndrome Metabólico/tratamiento farmacológico , Calidad de Vida , Antioxidantes , Verduras , Inflamación , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico
3.
Artículo en Inglés | MEDLINE | ID: mdl-36413908

RESUMEN

A novel Isoxazole (ISO) analog of curcumin is synthesized from curcumin and described as having a better pharmacological activity than curcumin, such as anti-cancer, anti-malarial, anti-mycobacterial, and many more. The present research aims to develop a bio-analytical method with a simple, rapid, selective, sensitive, accurate, and precise quantification of ISO by liquid chromatography coupled with tandem mass spectroscopy (LC-MS/MS) in rat plasma matrix. The simple plasma protein precipitation method was used for ISO extraction. The ISO was eluted in isocratic mode on a Water symmetry C18 column (75 × 4.6 mm2, 3.5 µm) at a 600 µL/min flow rate with a 0.1 % formic acid in water and methanol (20:80) as mobile phase. The MS/MS was used as a monitoring tool for the fragmentation of ISO as m/z = 366.1 → 145.1 and m/z = 237.1 → 194.07 for carbamazepine (CBZ; internal standard). The ISO showed good co-relation as (r2 = 0.999) linear and covered a wide range with a lower limit of quantification of 1.0 ng/mL. Finally, the developed method was successfully utilized for oral and intravenous pharmacokinetics of ISO in rats plasma. The absolute bioavailability of ISO was found at about 17.6 % after oral administration.


Asunto(s)
Curcumina , Ratas , Animales , Cromatografía Liquida , Espectrometría de Masas en Tándem , Isoxazoles , Carbamazepina , Agua
4.
J Food Biochem ; 45(3): e13290, 2021 03.
Artículo en Inglés | MEDLINE | ID: mdl-32632972

RESUMEN

Polyherbal Formulations (PHF) were developed by combining fruit juices of Momordica charantia, Cucumis sativus, and Solanum lycopersicum in different ratios and optimized through Oral Glucose Tolerance Test (OGTT) model. PHF-C pretreated rats showed the highest reduction of Serum Glucose Levels (SGL) after 60 min of glucose administration. PHF-C was incorporated into spheroids using fresh juice (FJS) and lyophilized powder (LPS) of selected plants. In OGTT study, LPS showed a significant reduction of SGL. LPS was characterized as almost spherical, having disintegration time 8 min, adequate friability, and good flow properties. In STZ-induced diabetic rats on 7th, 14th, and 21st days, LPS was reduced SGL by 9.01%, 20.9%, 38.9% (250 mg/kg dose); 20.5%, 33.9%, and 50.7% (500 mg/kg dose), respectively. LPS showed a significant improvement in abnormal body weight, biochemical, and oxidative parameters in comparison to PHF-C and metformin. Novel formulation LPS (500 mg/kg) was found more effective (p < .05) in reversing STZ-induced hyperglycemia as compared to PHF-C (1,000 mg/kg) and at par with metformin (500 mg/kg). PRACTICAL APPLICATIONS: Fresh vegetable juice contains large quantities of vitamins and minerals. Cooking and processing of fruits may destroy their nutritional value. However, FJS also has some limitations, including seasonal specificity, patient compliance, less stability, loss of vitamins and fibers, abnormal sugar level, weak immunity, and difficult to carry by patients. Lyophilization is a well-known method to improve the physical state, shelf life, and stability of phytoconstituents. Poor absorption and less bioavailability also impede the acceptance of PHF. To overcome these limitations, a suitable novel drug delivery system is required which has high therapeutic efficacy and enhanced bioavailability. The patented spheroids of herbal extracts which are in use for the treatment of the number of diseases encouraged the present work. Spheroid protects the constituents of herbal drugs from gastric destruction and gut bacteria. The outcome of present research supports the concept of enhanced stability and bioavailability of phytoconstituents present in FJS.


Asunto(s)
Diabetes Mellitus Experimental , Metformina , Momordica charantia , Animales , Diabetes Mellitus Experimental/tratamiento farmacológico , Jugos de Frutas y Vegetales , Humanos , Hipoglucemiantes , Ratas
5.
J Adv Pharm Technol Res ; 4(2): 108-17, 2013 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-23833751

RESUMEN

Multifactorial metabolic diseases, for instance diabetes develop several complications like hyperlipidemia, hepatic toxicity, immunodeficiency etc., Hence, instead of mono-drug therapy the management of the disease requires the combination of herbs. Marketed herbal drugs comprise of irrational combinations, which makes their quality control more difficult. Phytoconstituents, despite having excellent bioactivity in vitro demonstrate less or no in vivo actions due to their poor lipid solubility, resulting in high therapeutic dose regimen; phospholipids encapsulation can overcome this problem. Hence, present study was designed to develop a phospholipids encapsulated polyherbal anti-diabetic formulation. In the present study, polyherbal formulation comprises of lyophilized hydro-alcoholic (50% v/v) extracts of Momordica charantia, Trigonella foenum-graecum and Withania somnifera 2:2:1, respectively, named HA, optimized based on oral glucose tolerance test model in normal Wistar rats. The optimized formulation (HA) entrapped in the phosphatidylcholine and cholesterol (8:2) vesicle system is named HA lipids (HAL). The vesicles were characterized for shape, morphology, entrapment efficiency, polar-dispersity index and release profile in the gastric pH. The antidiabetic potential of HA, marketed polyherbal formulation (D-fit) and HAL was compared in streptozotocin-induced diabetic rat model of 21 days study. The parameters evaluated were behavioral changes, body weight, serum glucose level, lipid profile and oxidative stress. The antidiabetic potential of HA (1000 mg/kg) was at par with the D-fit (1000 mg/kg). However, the potential was enhanced by phospholipids encapsulation; as HAL (500 mg/kg) has shown more significant (P < 0.05) potential in comparison to HA (1000 mg/kg) and at par with metformin (500 mg/kg).

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