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1.
RSC Adv ; 14(19): 13100-13128, 2024 Apr 22.
Artigo em Inglês | MEDLINE | ID: mdl-38655462

RESUMO

Epoxides are oxygen containing heterocycles which are significantly employed as crucial intermediates in various organic transformations. They are considered highly reactive three-membered heterocycles due to ring strain and they undergo epoxide ring opening reactions with diverse range of nucleophiles. Epoxide ring-opening reactions have gained prominence as flexible and effective means to obtain various functionalized molecules. These reactions have garnered substantial attention in organic synthesis, driven by the need to comprehend the synthesis of biologically and structurally important organic compounds. They have also found applications in the synthesis of complex natural products. In this review article, we have summarized the implementation of epoxide ring opening reactions in the synthesis of alkaloids and terpenoids based natural products reported within the last decade (2014-2023).

2.
Heliyon ; 10(3): e25414, 2024 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-38352784

RESUMO

In this study, chitosan nanoparticles (CSNPs) encapsulating Foeniculum vulgare (FV) seed extract (SE) were prepared for the controlled delivery of bioactive phytoconstituents. The prepared CSNPs encapsulating FVSE as sustain-releasing nanoconjugate (CSNPs-FVSE) was used as a potent source of functional metabolites including kaempferol and quercetin for accelerated reclamation of sensory and motor functions following peripheral nerve injury (PNI). The nanoconjugate exhibited in vitro a biphasic diffusion-controlled sustained release of quercetin and kaempferol ensuring prolonged therapeutic effects. The CSNPs-FVSE was administered through gavaging to albino mice daily at a dose rate of 25 mg/kg body weight from the day of induced PNI till the end of the experiment. The conjugate-treatment induced a significant acceleration in the regain of motor functioning, evaluated from the sciatic function index (SFI) and muscle grip strength studies. Further, the hotplate test confirmed a significantly faster recuperation of sensory functions in conjugate-treated group compared to control. An array of underlying biochemical pathways regulates the regeneration under well-optimized glucose and oxidant levels. Therefore, oxidant status (TOS), blood glycemic level and total antioxidant capacity (TAC) were evaluated in the conjugate-treated group and compared with the controls. The treated subjects exhibited controlled oxidative stress and regulated blood sugars compared to the non-treated control. Thus, the nanoconjugate enriched with polyphenolics significantly accelerated the regeneration and recovery of functions after nerve lesions. The biocompatible nanocarriers encapsulating the nontoxic natural bioactive constitutents have great medicinal and economic value.

3.
Epilepsy Res ; 200: 107302, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38280331

RESUMO

BACKGROUND: Antiseizure medications (ASMs) are known to potentially impact bone health, but existing literature presents conflicting results regarding their specific effects on bone mineralization, metabolism, and quality. OBJECTIVE: This systematic review aims to establish a consensus regarding the influence of ASMs on bone health based on existing preclinical studies. METHODS: Following SYRCLE and PRISMA guidelines, we conducted a systematic search in PubMed, Science Direct, and Google Scholar to identify relevant studies. Ultimately, 21 articles were selected for inclusion in this review. RESULTS: Among the chosen studies, approximately half involved Wistar rats as experimental subjects. Levetiracetam and sodium valproate were the most frequently investigated drugs, with a typical treatment duration of 10-12 weeks. These studies exhibited a low risk of bias in aspects like sequence generation, random housing, random outcome assessment, and reporting bias. However, blinding in performance, allocation concealment, and detection were often rated as having a high risk of bias. The collective findings suggest that prolonged ASM use leads to reduced bone mineral density, altered bone turnover marker levels (including hypovitaminosis D, hypocalcemia, and secondary hyperparathyroidism), deterioration of bone microarchitecture, and decreased mechanical strength. CONCLUSION: The adverse effects on bone associated with ASMs are not limited to enzyme-inducing drugs, as newer generation ASMs may also contribute to these effects. Hypovitaminosis D alone may not be solely responsible for ASM-induced bone issues, suggesting the involvement of other mechanisms. Furthermore, substantial variations were observed in the results of different preclinical studies on individual ASMs, highlighting the need to standardize animal study methodologies to enhance reproducibility and reduce variation.

4.
Heliyon ; 10(1): e23416, 2024 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-38170008

RESUMO

The exploitation of natural products and their analogues in the field of pharmacology has been regarded as of great importance. It can be attributed to the fact that these scaffolds exhibit diverse chemical properties, distinct biological activities and zenith specificity in their biochemical processes, enabling them to act as favorable structures for lead compounds. The synthesis of natural products has been a crafty and hard-to-achieve task. Steglich esterification reaction has played a significant role in that area. It is a mild and efficient technique for constructing ester linkages. This technique involves the establishment of ester moiety via a carbodiimide-based condensation of a carboxylic acid with an alcohol, thiol or an amine catalyzed by dimethyl aminopyridine (DMAP). Specifically, labile reagents with multiple reactive sites are esterified efficiently with the classical and modified Steglich esterification conditions, which accounts for their synthetic utility. This review encloses the performance of the Steglich esterification reaction in forging the ester linkage for executing the total synthesis of natural products and their derivatives since 2018.

5.
Curr Drug Metab ; 24(9): 622-634, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37779408

RESUMO

Artificial Intelligence (AI) has emerged as a powerful tool in various domains, and the field of drug formulation and development is no exception. This review article aims to provide an overview of the applications of AI in drug formulation and development and explore its future prospects. The article begins by introducing the fundamental concepts of AI, including machine learning, deep learning, and artificial neural networks and their relevance in the pharmaceutical industry. Furthermore, the article discusses the network and tools of AI and its applications in the pharmaceutical development process, including various areas, such as drug discovery, manufacturing, quality control, clinical trial management, and drug delivery. The utilization of AI in various conventional as well as modified dosage forms has been compiled. It also highlights the challenges and limitations associated with the implementation of AI in this field, including data availability, model interpretability, and regulatory considerations. Finally, the article presents the future prospects of AI in drug formulation and development, emphasizing the potential for personalized medicine, precision drug targeting, and rapid formulation optimization. It also discusses the ethical implications of AI in this context, including issues of privacy, bias, and accountability.


Assuntos
Inteligência Artificial , Aprendizado de Máquina , Humanos , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Desenvolvimento de Medicamentos
6.
ACS Omega ; 8(33): 30306-30314, 2023 Aug 22.
Artigo em Inglês | MEDLINE | ID: mdl-37636953

RESUMO

In this study, we reported the synthesis of 1-(4-bromobenzoyl)-1,3-dicyclohexylurea by the reaction of DCC (N,N'-dicyclohexylcarbodiimide) with 4-bromobenzoic acid. Subsequently, we further synthesized a new series of 1-(4-arylbenzoyl)-1,3-dicyclohexylurea (5a-g) derivatives using a Suzuki cross-coupling reaction between 1-(4-bromobenzoyl)-1,3-dicyclohexylurea (3) and various aryl/heteroaryl boronic acids (4). Thus, density functional theory (DFT) calculations have been performed to examine the electronic structure of the synthesized compounds (3, 5a-g) and to calculate their spectroscopic data. Moreover, optimized geometries and thermodynamic properties, such as frontier molecular orbitals (HOMO, LUMO), molecular electrostatic potential surfaces, and reactivity descriptors, were also calculated at the PBE0-D3BJ/def2-TZVP/SMD1,4-dioxane level of theory to validate the structures of the synthesized compounds.

7.
Molecules ; 28(15)2023 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-37570621

RESUMO

Simmons-Smith cyclopropanation is a widely used reaction in organic synthesis for stereospecific conversion of alkenes into cyclopropane. The utility of this reaction can be realized by the fact that the cyclopropane motif is a privileged synthetic intermediate and a core structural unit of many biologically active natural compounds such as terpenoids, alkaloids, nucleosides, amino acids, fatty acids, polyketides and drugs. The modified form of Simmons-Smith cyclopropanation involves the employment of Et2Zn and CH2I2 (Furukawa reagent) toward the total synthesis of a variety of structurally complex natural products that possess broad range of biological activities including anticancer, antimicrobial and antiviral activities. This review aims to provide an intriguing glimpse of the Furukawa-modified Simmons-Smith cyclopropanation, within the year range of 2005 to 2022.


Assuntos
Alcaloides , Produtos Biológicos , Produtos Biológicos/química , Alcaloides/química , Ciclização , Nucleosídeos , Ciclopropanos/química
8.
Pharmaceuticals (Basel) ; 16(3)2023 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-36986444

RESUMO

Human tyrosinase (hTYR) is a key and rate-limiting enzyme along with human tyrosinase-related protein-1 (hTYRP1), which are among the most prominent targets of inhibiting hyper pigmentation and melanoma skin cancer. In the current in-silico computer-aided drug design (CADD) study, the structure-based screening of sixteen furan-1,3,4-oxadiazole tethered N-phenylacetamide structural motifs BF1-BF16 was carried out to assess their potential as hTYR and hTYRP1 inhibitors. The results revealed that the structural motifs BF1-BF16 showed higher binding affinities towards hTYR and hTYRP1 than the standard inhibitor kojic acid. The most bioactive lead furan-1,3,4-oxadiazoles BF4 and BF5 displayed stronger binding in affinities (-11.50 kcal/mol and -13.30 kcal/mol) than the standard drug kojic acid against hTYRP1 and hTYR enzymes, respectively. These were further confirmed by MM-GBSA and MM-PBSA binding energy computations. The stability studies involving the molecular dynamics simulations also provided stability insights into the binding of these compounds with the target enzymes, wherein it was found that they remain stable in the active sites during the 100 ns virtual simulation time. Moreover, the ADMET, as well as the medicinal properties of these novel furan-1,3,4-oxadiazole tethered N-phenylacetamide structural hybrids, also showed a good prospect. The excellent in-silico profiling of furan-1,3,4--oxadiazole structural motifs BF4 and BF5 provide a hypothetical gateway to use these compounds as potential hTYRP1 and hTYR inhibitors against melanogenesis.

9.
Clin Exp Med ; 23(6): 2267-2273, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36802308

RESUMO

To determine the antibody levels at 6 months in SARS-CoV-2 vaccinated individuals in COVID-recovered versus non-infected groups to determine the need to administer booster COVID vaccine in each group. Prospective longitudinal study. Pathology Department, Combined Military Hospital, Lahore for a period of eight months from July 2021 to February 2022. Two hundred and thirty three study participants in both COVID recovered and non-infected groups (105 participants in infected group, 128 participants in non-infected group) were subjected to blood sampling at 6 months post-vaccination. Anti-SARS-CoV-2 IgG antibody test was done using Chemiluminescence method. Comparison of antibody levels between COVID-recovered and non-infected groups was made. Results were compiled and statistically analyzed using SPSS version 21. Out of 233 study participants, males were 183 (78%) while females were 50 (22%), mean age being 35.93 years ± 8.298. Mean Anti-SARS-CoV-2 S IgG levels among COVID-recovered group was 1342 U/ml and among non-infected group was 828 U/ml at 6 months post-vaccination. Mean antibody titers in COVID-19 recovered group are higher than in non-infected group at 6 months post-vaccination in both groups.


Assuntos
Vacinas contra COVID-19 , COVID-19 , Feminino , Masculino , Humanos , Adulto , COVID-19/prevenção & controle , Estudos Longitudinais , Estudos Prospectivos , SARS-CoV-2 , Imunoglobulina G , Anticorpos Antivirais , Imunidade , Vacinação
10.
Pak J Pharm Sci ; 35(3(Special)): 885-889, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35791583

RESUMO

Hydrazones of theophylline-7-acetic acid 5a-g have been synthesized using ultrasonic irradiation as well as conventional heating system and analyzed for their anticancer characteristics against human lung cancer cell line (A549). Compound 5g with cell viability 33.19±0.49% (100 µg/µL) compared to the starting reference drug acefylline having cell viability 86.32±11.75% (100 µg/µL) was found to be the most active anticancer agent among all. The synthesized derivatives were also exposed to hemolytic and thrombolytic studies to determine their cytotoxic profile and results revealed their low toxicity and moderate clot lysis activity.


Assuntos
Antineoplásicos , Neoplasias Pulmonares , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Linhagem Celular Tumoral , Hemólise , Humanos , Hidrazonas/farmacologia , Neoplasias Pulmonares/tratamento farmacológico , Relação Estrutura-Atividade , Teofilina/análogos & derivados
11.
Pak J Pharm Sci ; 35(1(Supplementary)): 177-182, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-35228175

RESUMO

A green ultrasound assisted convenient approach has been reported for the ring opening of epoxides. As a result, a series of N-phenyl piperazine and morpholine based ß-amino alcohols has been synthesized under ultrasound irradiation in DMSO for 60 minutes at 70°C. This methodology showed excellent tolerance with various epoxides and provided excellent yields upto 96%. All the synthetic derivatives (4a-e) (5c-d) significantly influence the catalytic activity of protease while 5d exhibited maximum (100%) inhibitory effect with a half-life of 40.76 minutes. Among the target derivatives, compound 4c exhibited significant antibacterial activity against Bacillus subtilis and Escherichia coli bacterial strains with zone of inhibition values 45 mm and 32 mm, respectively.


Assuntos
Aminoácidos/farmacologia , Antibacterianos/farmacologia , Compostos de Epóxi/química , Inibidores de Proteases/farmacologia , Aminoácidos/síntese química , Relação Estrutura-Atividade
12.
Microsc Res Tech ; 85(4): 1410-1420, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-34850481

RESUMO

Pollen micromorphology is not only used to check the functional and structural evolution in plants but also to solve the taxonomic problem related to the classification of plants. Therefore, keeping in view the significance of pollen traits, selected taxa of the subfamily Caesalpiniaceae was collected from different geographical regions of Pakistan. The species were then analyzed under both light microscopy and scanning electron microscopy techniques to investigate the importance of micromorphological characters of pollen in the identification and classification of species. Great variation was recorded in equatorial shape, surface ornamentation, tectum, polar diameter, equatorial diameter, and exine thickness. However, little variation was observed in pollen type, polar shape, and fertility of pollen. The equatorial shape of five types was observed: prolate, prolate-spheroidal, spheroidal-subprolate, subspheroidal-prolate, and subspheroidal. Four types of surface ornamentation, psilate, granulate, clavate, and perforate, were recorded. Tectum of five types, intactate, reticulate regulate, medium reticulate, tactate, and striate, was observed. Sexine was thicker than nexine in all studied species. The largest polar diameter was observed in Caesalpinia pulcherrima 64.1 µm while the smallest in Parkinsonia aculeata 26.1 µm. The largest equatorial diameter was found in C. pulcherrima of 70.25 µm whereas the smallest in P. aculeata 27.57 µm. All the pollens analyzed were tricolporate. All studied species have a fertility ratio of more than 90%. A taxonomic key was developed to show the variation in pollen features and delimit species for the correct identification. In conclusion, the pollen traits were found useful to define species boundaries at various taxonomic ranks and will strengthen the taxonomy of this subfamily. Besides, this study also explored the palynological traits and their implication in the taxonomy of the subfamily Caesalpiniaceae.


Assuntos
Caesalpinia , Pólen , Microscopia Eletrônica de Varredura , Paquistão , Pólen/anatomia & histologia
13.
Mol Divers ; 26(1): 589-628, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33575984

RESUMO

Fukuyama reaction for the synthesis of multifunctional aldehydes, secondary amines and ketones has gained considerable importance in synthetic organic chemistry because of mild reaction conditions. The use of thioesters in both Fukuyama aldehydes and ketones synthesis is highly attractive for organic chemists as they are easily accessible from corresponding carboxylic acids. Fukuyama-Mitsunobu reaction utilizes 2-nitrobenzenesulfonyl (Ns) for the protection/activation/deprotection of primary amines to afford secondary amines in good yields and high enantioselectivities. This review presents recent synthetic developments and applications of Fukuyama reaction for the synthesis of aldehydes, secondary amines and ketones.


Assuntos
Aldeídos , Aminas , Alquilação , Ácidos Carboxílicos , Catálise , Cetonas
14.
J Ethnopharmacol ; 283: 114743, 2022 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-34655670

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Kidney disease (KD) is one of the serious health issues, which causes worrisome morbidity and economic burden. Therapeutic strategies are available however majority of them are associated with severe adverse effects and poor patient compliance and adherence. This explorative article was undertaken to provide a holistic review of known nephroprotective (NP) phytoconstituents along with their research-based evidences on mechanism, sources, and clinical trials that may play essential role in prevention and cure of KD. AIM OF THE STUDY: The present systematic review aimed to provide in-depth and better evidences of the global burden of KD, phytoconstituents as NP with emphasis on mechanism of action both in vitro and in vivo, their wide biological sources as well as their clinical efficacy in management of kidney disease and its related disorders. MATERIAL AND METHODS: Comprehensive information was searched systematically from electronic databases, namely, PubMed, Sciencedirect, Wiley, Scopus, Google scholar and Springer until February 2021 to find relevant data for publication on phytoconstituents with nephroprotective potential. RESULTS: In total, 24,327 articles were screened in first search for "phytoconstituents and medicinal plants for nephroprotection and kidney disorder". On the basis of exclusion and inclusion criteria, 24,091 were excluded. Only 236 papers were spotted to have superlative quality data, which is appropriate under titles and sub-titles of the present review. The phytoconstituents having multiple research evidence along with wide number of medicinal plants sources and mechanism reported for nephroprotection have been selected and reviewed. CONCLUSION: This review, based on pre-clinical and clinical data of NP phytoconstituents, provides scientific-basis for the rational discovery, development and utilization of these upcoming treatment practices. Further,-more clinical studies are warranted to improve the pharmacodynamic and pharmacokinetic understanding of phytoconstituents. Also, more specific evaluation for natural sources is needed.


Assuntos
Nefropatias/prevenção & controle , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Animais , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Fitoterapia/métodos
15.
J Food Biochem ; 46(4): e13852, 2022 04.
Artigo em Inglês | MEDLINE | ID: mdl-34250628

RESUMO

The biomedical survey reports edible plant Aegle marmelos has been utilized for centuries by tribal communities in India as a dietary supplement for the management of diabetes. Herein, we have investigated cytotoxicity, cytoprotective and antidiabetic activity of characterized alkaloid-free hydroalcoholic extract of A. marmelos (AFEAM; 200 and 400 mg/kg). Identification of polyphenols and quantification of major compounds were done using UPLC-MS and HPTLC, respectively. AFEAM showed good cytocompatibility and cytoprotective potential against oxidative stress induced by hyperglycemia in HepG2 cells. The AFEAM intake had significantly ameliorated the serum blood glucose level, state of dyslipidemia, level of pro-inflammatory markers (tumor necrosis factor-α, interleukin-6, and interleukin-1ß), and antioxidant (superoxide dismutase, catalase, glutathione peroxidase, and malondialdehyde) status in diabetic mice. Histological examination of the treated groups showed amelioration of damaged pancreas, liver, and kidney tissues. Conclusively, AFEAM intake might be promising dietary supplements for prediabetics as well as an adjuvant to modern treatment in diabetics. PRACTICAL APPLICATIONS: Different reports have been published on Aegle marmelos but as per our understanding till date, no study has been reported on the amelioration of diabetes due to alkaloid free hydroalcoholic extract of A. marmelos /polyphenolic content in the animal model. The result of this study indicated that A. marmelos supplementation effectively ameliorates diabetes through the restoration of antioxidant and anti-inflammatory status. This study has collated sufficient scientific evidence for the dietary application of A. marmelos in society especially for prediabetics, however, it can also be used as an adjuvant to modern treatments in diabetics.


Assuntos
Aegle , Diabetes Mellitus Experimental , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Cromatografia Líquida , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Camundongos , Extratos Vegetais/farmacologia , Folhas de Planta , Polifenóis/farmacologia , Polifenóis/uso terapêutico , Espectrometria de Massas em Tandem
16.
Saudi J Biol Sci ; 28(11): 6441-6453, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34764761

RESUMO

Chronic Kidney Disease (CKD) is a major health problem characterized by kidney dysfunction with progressive segmental glomerulosclerosis to end-stage renal disease (ESRD). Due to lack of scientific data and comprehensive reports, the current systematic review provides an inclusive understanding and prospective associated with phytopharmacology of NEERI-KFT in CKD. The data was collected from more than five databases such as Science Direct, Google Scholar, Elsevier, PubMed, Springer, ACS publication etc using keywords like CKD/Kidney disease, epidemiology/prevalence, modern therapies for CKD management, NEERI-KFT and its role in kidney disease. The study was performed based on scientific reports screened by experts according to inclusion and exclusion criteria. The pre-clinical and clinical findings suggested that NEERI-KFT has promising effects as nephroprotective and considered safe and well effective in primary care of kidney against disease. Phytopharmacological evaluation of NEERI-KFT suggest that it exhibit substantial potential against oxidative and inflammatory stress induced apoptosis by exerting antioxidants, nephroprotective and immunomodulatory effects. Hence, it can be enlighten that NEERI-KFT have potential herbs which exerts significant antioxidants, nephroprotective and immunomodulatory effects in the patients associated with renal dysfunction or CKD thus improving altered renal architecture and renal physiology. Clinically, it is concluded that NEERI-KFT works kidney malfunction and cease ESRD progression or even reduce the number of dialysis.

17.
J Ethnopharmacol ; 272: 113936, 2021 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-33610710

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Synthetic drugs used for cancer treatment have side effects that may be immunosupressive, can cause liver, kidney and cardiac toxicity, and infertility and ovarian failure, among others. Thus, herbal drugs could be used in the cancer treatment as an adjuvant therapy. Andrographis paniculata (Burm.f.) Nees (AP) is one of the traditional herbs used in different alternative medicinal systems such as Ayurveda, Unani, Chinese, Malayi, Siddha, etc. for the treatment of various disorders and diseases including cancer. AIM OF THE STUDY: The aim of writing this review is to highlight the medicinal importance of AP and its main phytoconstituent andrographolide (AG). The main emphasis was given on the anticancer activity of AG, its proposed mechanisms of action, novel approaches used to improve its biopharmaceutical properties with the perspective of evidence-based research, and its development as an adjuvant therapy for cancer treatment in future. MATERIALS AND METHODS: Literature survey was conducted and research papers were retrieved from different databases such as Pubmed, Google Scholar, ACS, Wiley online library, ScienceDirect, Springer, and Scopus during 1970-2020. Research articles, review articles, and short communications, etc. were used for this purpose. The papers were selected on the basis of exclusion and inclusion criteria. RESULTS: Different anticancer mechanisms of AG have been reportedly proven such as cell cycle arrest, apoptosis, NF-κß inhibition, antiangiogenesis, cytokine inhibition, etc. whereas its pharmacokinetic properties showed its highly protein bound nature, Cyt P400 (CYP) inhibition, low aqueous solubility, poor oral bioavailability, etc. Different novel formulations of AG have been investigated to increase its bioavailability for better efficacy. CONCLUSION: This review can provide knowledge about the potential applicability of AP or AG as an adjuvant therapy in cancer treatment. Further research is needed before making any conclusion about the efficacy in humans as an adjuvant therapy in cancer.


Assuntos
Andrographis/química , Antineoplásicos/farmacologia , Diterpenos/farmacologia , Animais , Antineoplásicos/uso terapêutico , Diterpenos/uso terapêutico , Composição de Medicamentos , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia
18.
ACS Omega ; 5(46): 29688-29697, 2020 Nov 24.
Artigo em Inglês | MEDLINE | ID: mdl-33251404

RESUMO

BGR-34 is a polyherbal formulation frequently used to combat diabetes around the globe especially in Asian countries. It provides an attractive treatment option to prediabetics, diabetics, and in metabolic disorders by controlling the altered blood glucose level. The lack of phytopharmacological studies on BGR-34 prompted as to reveal the compounds responsible for the antidiabetic and free-radical scavenging activity of BGR-34. An attempt was made to assess in vitro α-amylase and α-glucosidase enzyme inhibition of BGR-34 along with its free-radical scavenging potential via DPPH scavenging activity. Further, HPTLC profiling and quantitative analysis of berberine and palmatine in BGR-34 were carried out. Thereafter, the TLC-bioautographic-MS analysis was performed to identify the compounds responsible for antidiabetic and antioxidant activities in BGR-34. The results had shown a significant and dose-dependent inhibition potential of BGR-34 against in vitro α-amylase and α-glucosidase enzymatic reactions along with significant inhibition in DPPH free-radical scavenging activity. The HPTLC profiling and quantitative validation studies showed the presence of berberine and palmatine 44.926 ± 0.2907 and 10.507 ± 0.154 µg/g, respectively. The TLC-MS bioautography revealed a total of four DPPH-active, two α-amylase-active, and nine α-glucosidase-active compounds in BGR-34. It was observed from the study that BGR-34 possesses verities of bioactive compounds, which are reasonable not only for its antidiabetic effect but also for its antioxidant activity.

19.
Front Pharmacol ; 11: 578970, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33737875

RESUMO

The cases of COVID-19 are still increasing day-by-day worldwide, even after a year of its first occurrence in Wuhan city of China. The spreading of SARS-CoV-2 infection is very fast and different from other SARS-CoV infections possibly due to structural differences in S proteins. The patients with severe diseases may die due to acute respiratory distress syndrome (ARDS) caused by systemic inflammatory reactions due to the excessive release of pro-inflammatory cytokines and chemokines by the immune effector cells. In India too, it is spreading very rapidly, although the case fatality rate is below 1.50% (https://www.statista.com), which is markedly less than in other countries, despite the dense population and minimal health infrastructure in rural areas. This may be due to the routine use of many immunomodulator medicinal plants and traditional AYUSH formulations by the Indian people. This communication reviews the AYUSH recommended formulations and their ingredients, routinely used medicinal plants and formulations by Indian population as well as other promising Indian medicinal plants, which can be tested against COVID-19. Special emphasis is placed on Indian medicinal plants reported for antiviral, immunomodulatory and anti-allergic/anti-inflammatory activities and they are categorized for prioritization in research on the basis of earlier reports. The traditional AYUSH medicines currently under clinical trials against COVID-19 are also discussed as well as furtherance of pre-clinical and clinical testing of the potential traditional medicines against COVID-19 and SARS-CoV-2. The results of the clinical studies on AYUSH drugs will guide the policymakers from the AYUSH systems of medicines to maneuver their policies for public health, provide information to the global scientific community and could form a platform for collaborative studies at national and global levels. It is thereby suggested that promising AYUSH formulations and Indian medicinal plants must be investigated on a priority basis to solve the current crisis.

20.
J AOAC Int ; 103(3): 609-633, 2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-31547901

RESUMO

Unani medicine, based largely on herbs, is practiced as a traditional system of medicine in the Indian subcontinent. It owes its origination to the Greek philosopher Hippocrates (460-377 BC) and his associates. However, it progressed and got established under the patronage of Persian and Arab empires and later came to the Indian sub-continent around the middle of the 14th century. Unani scholars have been of the view that every person has their own distinct temperament constituted from four basic humoral combinations. Temperament of an individual is supposed to be influenced by various intrinsic and extrinsic factors such as age and mental status of individual, local climate, and environmental conditions, etc. Treatment is applied through dietotherapy and/or pharmacotherapy consonant with the patient's temperament. Unani medicine believes in health promotion and manages the disease through various modes of treatment such as regimental therapy, dietotherapy, and pharmacotherapy. A variety of clinical studies have shown that Unani medicines are effective with minimal side effects. Standardization, quality control, and toxicity profiling of many herbal drugs and the validation of formulations mentioned in the Unani Pharmacopeia of India have been accomplished in the recent past. Despite the mounting benefits of this system in the management of human health, it remains under-utilized. This article elucidates the basic concepts and a brief history of Unani medicine and summarizes information about its quality control, as well as its contribution to the health sector in India.


Assuntos
Medicina Unani , Grécia , Humanos , Índia
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