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1.
Bioorg Med Chem Lett ; 89: 129311, 2023 06 01.
Artículo en Inglés | MEDLINE | ID: mdl-37149230

RESUMEN

Braylin (10b) is a 8,8-dimethyl chromenocoumarin present in the plants of the family Rutaceae and Meliaceae and possesses vasorelaxing and anti-inflammatory activities. In this study, six 6-alkoxy (10b, 15-19), and twelve 6-hydroxy-alkyl amine (20a-20l) derivatives of braylin (11 and 12) were synthesized to delineate its structural requirement for vasorelaxing activity. The synthesized compounds were evaluated for vasorelaxation response in preconstricted intact rat Main Mesenteric Artery (MMA). The compounds showed l-type VDCC channel blockade depended and endothelium-independent vasorelaxation within the range of Emax < 50.00-96.70 % at 30 µM. Amongst all, 6-alkoxy derivatives were more active than 6-hydroxy-alkyl amine derivatives. The structural refinements about braylin showed that deletion of its methoxy group or homologation beyond ethoxy group presented deleterious effect on vasorelaxation response of braylin. Interestingly, substituting the ethoxy group in 10b presented the best activity and selectivity towards l-type VDCC channel blockade, a specific target cardiovascular function.


Asunto(s)
Canales de Calcio Tipo L , Vasodilatación , Animales , Ratas , Alcoholes , Aminas/farmacología , Canales de Calcio Tipo L/farmacología
2.
Planta Med ; 89(1): 62-71, 2023 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-36167313

RESUMEN

This study aims to explore the possible pharmacological potential of Cleome viscosa Linn (Cleomaceae), an annual weed, into therapeutic value-added products. In the present study, we have explored the pharmacological and toxicological profile of coumarinolignoids isolated from Cleome viscose for the management of rheumatoid arthritis and related complications in a small animal model. To avoid the biasness during experiments on animals, we have coded the isolated coumarinolignoids as CLIV-92 to perform the experimental pharmacological study. CLIV-92 was orally administrated (30,100, 300 mg/kg) to animal models of collagen-induced arthritis (CIA), carrageenan-induced acute inflammation, thermal and chemical-induced pain, and Brewer's yeast-induced pyrexia. Oral administration of CLIV-92 significantly decreases the arthritis index, arthritis score, and increases the limb withdrawal threshold in the CIA model in experimental rats. The anti-arthritis studies revealed that the anti-inflammatory effect of CLIV-92 was associated with inhibition of the production of inflammatory mediators like TNF-α, IL-6, IL-17A, MMP-1, MMP-9, Nitric oxide, and C-RP in CIA rat's serum, and also reduced the NFкB-p65 expression as evidence of immunohistochemistry in knee joint tissue of CIA rats, in a dose-dependent manner. Further individual experiments related to arthritis-related complications in experimental animals demonstrated the analgesic, anti-inflammatory, and antipyretic potential of CLIV-92 in a dose-dependent manner. Further, an in-vivo acute oral toxicity study concluded that CLIV-92 is safe in experimental animals up to 2,000 mg/kg dose. The results of this study suggested that the oral administration of CLIV-92 may be a therapeutic candidate for further investigation in the management of rheumatoid arthritis and related complications.


Asunto(s)
Artritis Experimental , Artritis Reumatoide , Cleome , Ratas , Animales , Cleome/metabolismo , Artritis Reumatoide/inducido químicamente , Artritis Reumatoide/tratamiento farmacológico , Artritis Reumatoide/metabolismo , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Artritis Experimental/inducido químicamente , Artritis Experimental/tratamiento farmacológico , Artritis Experimental/metabolismo , Analgésicos/uso terapéutico , Citocinas/metabolismo
3.
Inflammopharmacology ; 31(1): 451-464, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-36595125

RESUMEN

The needle powder of Taxus wallichiana is in use for the management of diabetes and inflammation-related complications in the Indian and Chinese Systems of Traditional Medicine but the lack of proper pharmacological intervention has prompted us to investigate the pharmacological mechanism against inflammation-induced insulin resistance in high-fat diet-fed C57BL/6 mice. Hexane (Tw-H), chloroform (Tw-C), and ethyl acetate (Tw-EA) extracts were prepared from a needle of T. wallichiana and its effect on glucose uptake against TNF-α-induced insulin resistance in skeletal muscle cells was studied. Among all, Tw-EA extract has shown promising glucose uptake potential. Tw-EA treatment is also able to decrease the lipid accumulation in adipocytes. Chemical signature of Tw-EA using HPLC showed the presence of taxoids. Efficacy of taxoids-rich extract from T. wallichiana (Tw-EA) was further validated in in vivo system against high-fat diet (HFD)-induced insulin resistance in C57BL/6 mice. Oral treatment of Tw-EA showed significant reduction in blood glucose, pro-inflammatory cytokine production and body weight gain when compared with vehicle-treated HFD-induced insulin resistance in C57BL/6 mice. Histopathology and immunohistochemistry study in skeletal muscle and adipose tissue revealed that oral treatment of Tw-EA is able to reduce the infiltration of inflammatory cells in skeletal muscles, ameliorate the hypertrophy in adipose tissue and upregulate the GLUT4 protein expression. Treatment with Tw-EA significantly up-regulated mRNA expression of insulin signaling pathway (IRS-1, PI3K, AKT, GLUT 4). This study suggested the beneficial effect of taxoids-rich extract from Taxus wallichiana against the inflammation-associated insulin resistance condition.


Asunto(s)
Resistencia a la Insulina , Taxus , Ratones , Animales , Resistencia a la Insulina/fisiología , Dieta Alta en Grasa , Taxus/metabolismo , Taxoides/uso terapéutico , Ratones Endogámicos C57BL , Inflamación/tratamiento farmacológico , Insulina/metabolismo , Glucemia/metabolismo
4.
Inflammopharmacology ; 31(2): 983-996, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-36947299

RESUMEN

Liquiritigenin (LTG) and its bioprecursor isoliquiritigenin(ISL), the main bioactives from roots of Glycyrrhiza genus are progressively documented as a potential pharmacological agent for the management of chronic diseases. The aim of this study was to evaluate the pharmacological potential of liquiritigenin, isoliquiritigenin rich extract of Glycyrrhiza glabra roots (IVT-21) against the production of pro-inflammatory cytokines from activated macrophages as well as further validated the efficacy in collagen-induced arthritis model in rats. We also performed the safety profile of IVT-21 using standard in-vitro and in-vivo assays. Results of this study revealed that the treatment of IVT-21 and its major bioactives (LTG, ISL) was able to reduce the production of pro-inflammatory cytokines (TNF-α, IL-6) in LPS-activated primary peritoneal macrophages in a dose-dependent manner compared with vehicle-alone treated cells without any cytotoxic effect on macrophages. In-vivo efficacy profile against collagen-induced arthritis in Rats revealed that oral administration of IVT-21 significantly reduced the arthritis index, arthritis score, inflammatory mediators level in serum. IVT-21 oral treatment is also able to reduce the NFкB-p65 expression as evidence of immunohistochemistry in knee joint tissue and mRNA level of pro-inflammatory cytokines in paw tissue in a dose-dependent manner when compared with vehicle treated rats. Acute oral toxicity profile of IVT-21 demonstrated that it is safe up to 2000 mg/kg body weight in experimental mice. This result suggests the suitability of IVT-21 for further study in the management of arthritis and related complications.


Asunto(s)
Artritis Experimental , Glycyrrhiza , Ratas , Ratones , Animales , Artritis Experimental/tratamiento farmacológico , Artritis Experimental/metabolismo , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Extractos Vegetales/uso terapéutico , Glycyrrhiza/metabolismo , Citocinas/metabolismo , Macrófagos
5.
Microb Pathog ; 173(Pt A): 105884, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36379371

RESUMEN

Quorum sensing modulatory effect of linalool was tested for the first time against Pseudomonas syringae pv. tomato DC 3000, a bacterial plant pathogen responsible for causing huge losses worldwide. DC 3000 extensively regulates its virulence traits through quorum sensing mechanism involving expression of psyI, an acyl-homoserine lactone (AHL) synthase gene and psyR, a luxR-type regulator. In this study, exposure of DC 3000 to 80 ppm linalool concentration resulted in reduced biofilm formation, hampered motility, decreased AHL production, and reduced secretion of plant cell wall-degrading enzymes followed by negligible effect on the bacterial count and its metabolic activity. Extracellular polymeric substances (EPS), which play a crucial role in the development of biofilm and subsequent infection was significantly reduced which was further confirmed by Fourier Transform Infrared Spectroscopy. The qRT PCR analysis of the gene expression analysis of virulence genes (syringafactin production gene syfA, type III secretion system gene hrpA, flagellar genes fleQ and fliC, and coronatine production gene cfl unveiled significant downregulation of the same under Lin 80 ppm concentration. To further confirm the aforementioned possibilities, docking simulations run between PsyR and linalool suggested a strong interaction with the developed protein model. Overall, the treatment of DC 3000 with Lin 80 ppm affected the phenotypic and genotypic expressions associated with quorum sensing, thereby significantly reducing the infection rate as observed in in-vivo plant assay.


Asunto(s)
Pseudomonas syringae , Solanum lycopersicum , Pseudomonas syringae/genética , Percepción de Quorum/genética , Virulencia/genética , Proteínas Bacterianas/metabolismo , Acil-Butirolactonas/metabolismo
6.
Chem Biodivers ; 18(11): e2100531, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-34669255

RESUMEN

Artemisia pallens Wall. ex DC., popularly known as davana, has gained considerable attention because of its unique fragrance, high economic value, and pharmacological properties. The compositional complexity of davana essential oil (DO) has been a challenge for quality control. In this study, the chemical profile of DO was developed using polarity-based fractionation and a combination of gas chromatographic (GC-FID), hyphenated chromatographic (GC/MS), and spectroscopic (Fourier-Transform Infra-Red, 1D, 2D-Nuclear Magnetic Resonance) techniques. The analysis led to the identification of ninety-nine compounds. Major components of the DO were cis-davanone (D3, 53.0 %), bicyclogermacrene (6.9 %), trans-ethyl cinnamate (4.9 %), davana ether isomer (3.4 %), spathulenol (2.8 %), cis-hydroxy davanone (2.4 %), and trans-davanone (2.1 %). The study led to identifying several co-eluting novel minor components, which could help determine the authenticity of DO. The rigorous column-chromatography led to the isolation of five compounds. Among these, bicyclogermacrene, trans-ethyl cinnamate, and spathulenol were isolated and characterized by spectroscopic methods for the first time from DO. Pharmacological profile revealed that the treatment of DO and D3 inhibited the production of pro-inflammatory cytokines (TNF-α, IL-6) induced by lipopolysaccharide (LPS) in primary macrophages without any cytotoxic effect after administration of their effective concentrations. The result of this study indicates the suitability of DO and D3 for further investigation for the treatment of chronic skin inflammatory conditions.


Asunto(s)
Artemisia/química , Citocinas/antagonistas & inhibidores , Macrófagos/efectos de los fármacos , Aceites Volátiles/farmacología , Sesquiterpenos/farmacología , Animales , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Citocinas/metabolismo , Femenino , Lipopolisacáridos/antagonistas & inhibidores , Lipopolisacáridos/farmacología , Macrófagos/metabolismo , Ratones , Aceites Volátiles/química , Aceites Volátiles/aislamiento & purificación , Sesquiterpenos/química , Sesquiterpenos/aislamiento & purificación
7.
AAPS PharmSciTech ; 22(8): 259, 2021 Oct 26.
Artículo en Inglés | MEDLINE | ID: mdl-34704177

RESUMEN

Cliv-92 is a mixture of three structurally similar coumarinolignoids and a proven hepatoprotective agent. Low aqueous solubility and poor bioavailability are notable hindrances for its further use. Therefore, glycyrrhetinic acid-linked chitosan nanoparticles loaded with Cliv-92 were prepared for active targeting to the liver. The nanoparticles were prepared by the ionic gelation method to avoid the use of toxic solvents/rigorous agitation. The method of preparation was optimized using a central composite design with independent variables, namely polymer: drug ratio (3:1, w/w), crosslinker concentration (0.5%), and stirring speed (750 rpm). The optimized nanoparticles had a mean particle size of 185.17 nm, a polydispersity index of 0.41, a zeta potential of 30.93 mV, and a drug loading of 16.30%. The prepared formulation showed sustained release of approximately 63% of loaded Cliv-92 over 72 h. The nanoparticles were freeze-dried for long-term storage and further characterized. The formulation was found to be biocompatible for parenteral delivery. In vivo imaging study showed that optimized nanoparticles were preferentially accumulated in the liver and successfully targeting the liver. The present study successfully demonstrated the improved pharmacokinetic properties (≈12% relative bioavailability) and efficacy profile (evidenced by in vivo and histopathological studies) of fabricated Cliv-92 nanoparticles.


Asunto(s)
Quitosano , Ácido Glicirretínico , Nanopartículas , Portadores de Fármacos , Tamaño de la Partícula , Solubilidad
8.
Bioorg Med Chem Lett ; 30(1): 126759, 2020 01 01.
Artículo en Inglés | MEDLINE | ID: mdl-31711783

RESUMEN

A series of substituted 8,8-dimethyl-8H-pyrano[2,3-f]chromen-2-ones (chromeno-coumarin hybrids) was synthesized from scopoletin (11) as vasorelaxing agents. The synthesized compounds 21a-f, 22, 23a-e and scopoletin (11) were evaluated for vasorelaxation in endothelium intact rat main mesenteric artery (MMA). Compounds 11, 21a, 21c-f and 22 showed significant vasorelaxation in precontracted MMA within the range of EC50 value 1.58-5.02 µM. These derivatives presented 29.40-70.89 fold increased sensitivity for experimental tissue compared to scopoletin (11), the parent molecule. Among others, 22 was found to be the most active compound which had EC50 1.58 µM with 70.89 fold increased sensitivity. The mechanistic evaluation of 22 showed that it exerted vasorelaxation through Ca2+-activated K+ (BKca) channel and the effect was endothelium-independent.


Asunto(s)
Descubrimiento de Drogas/métodos , Vasodilatación/efectos de los fármacos , Humanos , Relación Estructura-Actividad
9.
Microb Pathog ; 115: 264-271, 2018 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-29273511

RESUMEN

The present investigation for the first time explains the anti biofilm and anti virulence potential of Kaffir lime oil (KLO) and its major constituent, Citronellal (3,7-dimethyloct-6-enal) against Xanthomonas oryzae pv. oryzae, causal organism of bacterial blight disease of rice. KLO at 500 ppm showed potential activity against X. oryzae pv. oryzae. Among the major components identified, citronellal (CIT) at 75 µM concentration was found to significantly inhibit biofilm along with the swimming and swarming potential of X. oryzae pv. oryzae. In contrary, CIT did not affect the metabolic status and growth kinetics of the bacterial cells. Gene expression analysis showed down regulation in motA, cheD, cheY, flgF, gumC, xylanase, endogluconase, cellulose, cellobiosidase, virulence and rpfF transcript levels by citronellal treatment. However, an insignificant effect of 75 µM CIT treatment was observed on motB, flgE, pilA, estY, pglA, protease and lytic genes expression. Finally, the observations recorded were in confirmity with the virulence leaf clip test as lesion length was significantly decreased (39%) in CIT treatment as compared to the control leaves inoculated with only X. oryzae pv. oryzae. Overall, the findings obtained advocate the use of CIT for promising anti biofilm and anti virulence activity which in turn can be used for managing the blight disease in rice.


Asunto(s)
Aldehídos/farmacología , Biopelículas/crecimiento & desarrollo , Citrus/química , Monoterpenos/farmacología , Aceites Volátiles/farmacología , Oryza/microbiología , Aceites de Plantas/farmacología , Xanthomonas/efectos de los fármacos , Monoterpenos Acíclicos , Regulación Bacteriana de la Expresión Génica/efectos de los fármacos , Movimiento/efectos de los fármacos , Enfermedades de las Plantas/microbiología , Hojas de la Planta/microbiología , Factores de Virulencia/genética , Xanthomonas/genética , Xanthomonas/patogenicidad
10.
Inflammopharmacology ; 26(5): 1245-1255, 2018 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-29429001

RESUMEN

BACKGROUND: Curcuma longa L. is an important industrial crop used by medicinal and cosmetic industries in the world. Its leaves are a waste material after harvesting rhizomes. The aim of the study was to evaluate the chemical and pharmacological profile of essential oil from waste leaves of Curcuma longa (EOCl) against skin inflammation. METHODS: EOCl was subjected to gas chromatography (GC) analysis for identification of essential oil constituents and its anti-inflammatory evaluation through in vitro and in vivo models. RESULTS: Chemical fingerprinting using GC and GC-MS analysis of EOCl revealed the presence of 11 compounds, representing 90.29% of the oil, in which terpinolene (52.88%) and α-phellandrene (21.13%) are the major components. In the in vitro testing EOCl inhibited the production of pro-inflammatory cytokines (TNF-α, IL-6, IL-1ß) in lipopolysaccharide (LPS) and 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in the human keratinocyte cell line (HaCaT). Topical application of EOCl produced anti-inflammatory effects by reducing ear thickness, ear weight and ameliorating the level of pro-inflammatory cytokines (TNF-α, IL-6, IL-1ß) at protein and mRNA levels as well as regulating the overproduction of oxidative markers and restoring the histopathological damage in a TPA-induced mouse model of inflammation. CONCLUSION: These findings of topical anti-inflammatory properties of EOCl provide a scientific basis for medicinal use of this plant material against inflammatory disorders.


Asunto(s)
Curcuma/química , Dermatitis/tratamiento farmacológico , Aceites Volátiles/uso terapéutico , Hojas de la Planta/química , Animales , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Femenino , Cromatografía de Gases y Espectrometría de Masas , Humanos , Ratones , Aceites Volátiles/farmacología , Conejos , Acetato de Tetradecanoilforbol
11.
BMC Genomics ; 18(1): 54, 2017 01 09.
Artículo en Inglés | MEDLINE | ID: mdl-28068903

RESUMEN

BACKGROUND: Pyrethrins are monoterpenoids and consist of either a chrysanthemic acid or pyrethric acid with a rethrolone moiety. Natural pyrethrins are safe and eco-friendly while possessing strong insecticidal properties. Despite such advantages of commercial value coming with the eco-friendly tag, most enzymes/genes involved in the pyrethrin biosynthesis pathway remain unidentified and uncharacterized. Since the flowers of Tanacetum cinerariifolium are rich in major pyrethrins, next generation transcriptome sequencing was undertaken to compare the flowers and the leaves of the plant de novo to identify differentially expressed transcripts and ascertain which among them might be involved in and responsible for the differential accumulation of pyrethrins in T. cinerariifolium flowers. RESULTS: In this first tissue specific transcriptome analysis of the non-model plant T. cinerariifolium, a total of 23,200,000 and 28,500,110 high quality Illumina next generation sequence reads, with a length of 101 bp, were generated for the flower and leaf tissue respectively. After functional enrichment analysis and GO based annotation using public protein databases such as UniRef, PFAM, SMART, KEGG and NR, 4443 and 8901 unigenes were identified in the flower and leaf tissue respectively. These could be assigned to 13344 KEGG pathways and the pyrethrin biosynthesis contextualized. The 2-C-methyl-D-erythritol 4-phosphate (MEP) pathway was involved in the biosynthesis of acid moiety of pyrethrin and this pathway predominated in the flowers as compared to the leaves. However, enzymes related to oxylipin biosynthesis were found predominantly in the leaf tissue, which suggested that major steps of pyrethrin biosynthesis occurred in the flowers. CONCLUSIONS: Transcriptome comparison between the flower and leaf tissue of T. cinerariifolium provided an elaborate list of tissue specific transcripts that was useful in elucidating the differences in the expression of the biosynthetic pathways leading to differential presence of pyrethrin in the flowers. The information generated on genes, pathways and markers related to pyrethrin biosynthesis in this study will be helpful in enhancing the production of these useful compounds for value added breeding programs. Related proteome comparison to overlay our transcriptome comparison can generate more relevant information to better understand flower specific accumulation of secondary metabolites in general and pyrethrin accumulation in particular.


Asunto(s)
Productos Biológicos/metabolismo , Chrysanthemum cinerariifolium/genética , Chrysanthemum cinerariifolium/metabolismo , Perfilación de la Expresión Génica , Genes de Plantas/genética , Insecticidas/metabolismo , Piretrinas/metabolismo , Ontología de Genes , Anotación de Secuencia Molecular , Proteómica , Análisis de Secuencia
12.
Bioorg Med Chem Lett ; 26(21): 5322-5327, 2016 11 01.
Artículo en Inglés | MEDLINE | ID: mdl-27671497

RESUMEN

Different alkyl amide (15a-l) and alkyl amine (16a-e) derivatives of 7,8-dimethoxy-3-hydroxy-2-(4-methoxyphenyl)benzopyran-4-one were synthesized and evaluated for their anticancer activity against five different cancer cell lines using SRB assay. Compounds 15e, 15i, 15j and 16a-e showed significant anticancer activity within the range of IC50 2.58-34.86µM. The most promising molecule, 16c, was further analyzed for its effect on cell cycle and apoptosis of estrogen receptor positive cancer cells (MCF-7 cells) which showed that 16c triggered apoptosis in MCF-7 cells and arrested cells population at sub-G0 (apoptotic) and G2M phase. In tubulin polymerization assay, 16c interfered with kinetics of tubulin polymerization.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Benzopiranos/síntesis química , Benzopiranos/farmacología , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Humanos , Concentración 50 Inhibidora , Relación Estructura-Actividad
13.
Curr Diabetes Rev ; 20(3): e290823220456, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-37644751

RESUMEN

BACKGROUND: The rising in diabetes incidents has clearly become one main worldwide health problem. Individuals suffering from diabetes are still more susceptible to many long-term and short-term side effects, which most often cause fatalities. Even though chemically synthesized anti-diabetic entities are capable of helping manage and treat, there has been significant risks related with their prolong and repetitive use. Hence, there is a requirement for safer and novel approaches that might be formed and utilized. OBJECTIVE: Aim of the present review is to explain the naturally occurring phytochemicals and novel approach as anti-diabetic agents in the treatment of diabetes and its related issues. METHOD: A survey of Google scholar, Research Gate, Pubmed, Science Direct, NCBI database was carried out conducted to determine a most hopeful phytochemicals and novel drug delivery systems in the management of diabetes. RESULT: The study stressed the significance of phytomolecules and some novel approaches researched or reported in the literature for the management and cure of diabetes. It is suggested that changes in lifestyle can help patients and like nutritional support, assessment and lifestyle guidance must be individualized based on physical and functional capacity. Further evaluations and improved preventative medicine were the result of improving patient outcomes. CONCLUSION: Conventional or synthetic drugs provide relief for short time but nanoformulations of phytomolecules offer an improved therapeutic with fewer negative side effects. Herbal medicines are rich in phytoconstituents and possess variety of health benefits. This review is compilation of phytoconstituents and novel drug delivery system of phytomolecules i.e. nanoparticles, niosomes, microsphere, microparticle and others.


Asunto(s)
Diabetes Mellitus , Plantas Medicinales , Humanos , Diabetes Mellitus/tratamiento farmacológico , Plantas Medicinales/química , Hipoglucemiantes/uso terapéutico , Hipoglucemiantes/química , Sistemas de Liberación de Medicamentos
14.
Curr Drug Targets ; 25(3): 201-219, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38231060

RESUMEN

Breast cancer is a widespread condition that kills more women from cancer-related causes than any other type of cancer globally. Women who have estrogen-dependent, initial metastatic breast cancer frequently receive treatment with surgery, radiation therapy, and chemotherapy. They may also get more specialized treatments like tamoxifen or aromatase inhibitors (anastrozole or letrozole). The World Health Organisation reported in 2012 that by 2030, breast cancer will be more common worldwide. There are several phytochemicals, such as isoflavones, coumestans, lignans, and prenylflavonoides. Isoflavones have been shown in studies to prevent the spread of breast cancer and to trigger apoptosis. Targeting BCs in metastatic breast cancer may be made possible by combining well-formulated phytochemicals in nanoparticles or other novel drug delivery agents with currently accepted endocrine and/or conventional chemotherapies. Cell signaling, regulation of cell cycles, oxidative stress action, and inflammation could be positively impacted by phytoconstituents. They have the ability to alter non-coding RNAs, to prevent the proliferation and regeneration of cancer cells. The availability of novel approaches helps in disease targeting, safety, effectiveness and efficacy. The current literature helps to know the available drugs i.e. phytoconstituents or novel drug delivery like nanoparticle, microsphere, micelles, liposomes and neosomes. The literature has been taken from PubMed, Google Scholar, SciFinder, or other internet sites.


Asunto(s)
Neoplasias de la Mama , Fitoquímicos , Humanos , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/patología , Femenino , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Fitoquímicos/química , Sistemas de Liberación de Medicamentos , Antineoplásicos Fitogénicos/uso terapéutico , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/administración & dosificación , Nanopartículas/química
15.
Curr Aging Sci ; 2024 Jun 06.
Artículo en Inglés | MEDLINE | ID: mdl-39005078

RESUMEN

BACKGROUND: Acute disseminated encephalomyelitis (ADEM), a neural and immune related state that occur when cerebrospinal system's damaged by extensive swelling. Although manifestation is possible no matter the age, adolescents have a greater probability that adults. The purpose of present manuscript is to provide recent advancement and enhance knowledge of the disease. METHOD: The literature search on etiology, pathophysiology, diagnosis and treatment was carried out using the online database of Scifinder, Medline, Pubmed and GoogleScholar, Scopus etc. Result: Although the cause of ADEM remains unclear, it is believed to be caused by the inflammation in those with genetic sensitivity to an environmental stimulation. When people have altered levels of awareness or multifocal neurological abnormalities, ADEM is a possibility as a diagnosis. The diagnosis of ADEM is dependent on a combination of clinical, radiologic symptoms and the exclusion of illnesses that mimic ADEM; there is no one test that can establish the diagnosis. The inflammation in a child's brain and spinal cord is treated with medication. Prednisone will occasionally be given to youngsters for a brief amount of time. CONCLUSION: Most children with ADEM improve with high doses of methylprednisolone. Cyclophosphamide and hypothermia was need to individual. Most investigations show that 50%-75% of individuals completely recover between the first and sixth month of their condition.

16.
Nat Prod Res ; : 1-13, 2024 Jun 03.
Artículo en Inglés | MEDLINE | ID: mdl-38828834

RESUMEN

Eugenol(1), a terpenoid found in Ocimum, has various biological activities. The present study aims at extraction, isolation of the plant secondary metabolite eugenol (1), it's derivatisation and structure identification as bioactive molecules. Synthesis and antiplasmodial activity (in-vitro and in-vivo), of a series of fourteen novel eugenol-based 1,2,3-triazole derivatives was done in the present study. Derivatives 5a-5n showed good antimalarial activity against the strain Plasmodium falciparum NF54. Derivative 5 m, IC50 at 2.85 µM was found to be several times better than its precursor 1 (106.82 µM) whereas the derivative 5n showed three fold better activity than compound 1, in vitro. The structure-activity relationship of the synthesised compounds indicated that the presence of triazole ring in eugenol analogues is responsible for their good activity. Compound 5m, was further evaluated for in-vivo antimalarial activity which showed about 79% parasitemia suppression. It is the first report on antimalarial activity of triazole eugenol derivatives.

17.
Nat Prod Res ; : 1-5, 2024 Jun 25.
Artículo en Inglés | MEDLINE | ID: mdl-38919044

RESUMEN

Cymbopogon distans (Nees ex Steud.) Will. Watson (Poaceae) is a promising aromatic plant distributed in the Himalayas. In this study, five acyclic monoterpenoids, namely geranyl acetate (RS1), neral (RS2), geranial (RS3), citral (RS4) and geraniol (RS5) were isolated from the essential oil of C. distans. The isolated compounds were tested for in-vitro neuroinflammation inhibitory potential in LPS-stimulated BV2 microglial cells. RS1-RS4 exhibited significant neuroinflammation inhibition without any cytotoxic effect at the dose of 10 µM. RS4, the most active anti-neuroinflammatory compound (TNF-α 31.48 ± 1.00%; IL-6 24.02 ± 0.63%; IL-1ß 42.15 ± 1.76%) was also able to inhibit acetylcholinesterase (AChE) in a dose-dependent manner. The results showed that RS4 (an isomeric mixture of neral and geranial) has the potential to inhibit neuroinflammation and AChE, which are the biomarkers of neurodegenerative disorders.

18.
Indian J Exp Biol ; 51(7): 515-21, 2013 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-23898550

RESUMEN

Since aging is the most important risk factor for variety of diseases, the discovery of a wide range of chemical modulators of aging in model organisms encourages new strategies for targeting age associated diseases. Simple genetic manipulation leads to long-lived and healthy animals, so any compound which could have similar effect would prove a boon to mankind. In the present study, effect of different pharmacological doses (1.0, 0.1, 0.01 and 0.001 mg/mL) of O. sanctum crude extract were used to determine their impact on life span, thermotolerance and ROS scavenging activities in C. elegans. The results revealed that 1 mg/mL of O. sanctum extract significantly extended the life span of C. elegans. The extract also proved to be a strong free radical scavenger and increased resistance against thermal stress. It is also suggested that the protective and life span extending action of the crude extract is not only due to its antioxidant capacity but may also be mediated by modulation of some signaling pathways. Thus, in addition to all the known medicinal property of Ocimum, it is capable of increasing stress tolerance and life span in C. elegans.


Asunto(s)
Envejecimiento/efectos de los fármacos , Antioxidantes/farmacología , Caenorhabditis elegans/efectos de los fármacos , Mezclas Complejas/farmacología , Depuradores de Radicales Libres/farmacología , Ocimum/química , Estrés Oxidativo/efectos de los fármacos , Animales , Caenorhabditis elegans/crecimiento & desarrollo , Caenorhabditis elegans/metabolismo , Proteínas de Caenorhabditis elegans/genética , Proteínas de Caenorhabditis elegans/metabolismo , Proliferación Celular , Quimiotaxis/efectos de los fármacos , Ambiente , Proteínas HSP70 de Choque Térmico/genética , Proteínas HSP70 de Choque Térmico/metabolismo , Calor , Peróxido de Hidrógeno/metabolismo , ARN Mensajero/genética , Reacción en Cadena en Tiempo Real de la Polimerasa , Reacción en Cadena de la Polimerasa de Transcriptasa Inversa , Transducción de Señal/efectos de los fármacos , Sirtuinas/genética , Sirtuinas/metabolismo
19.
Front Plant Sci ; 13: 960717, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36226284

RESUMEN

The global population is rising at an alarming rate, which is threatening food and nutritional security. Although chemical fertilizers and pesticides are important for achieving food security, their excessive usage critically affects soil health and adds up residues in the food chain. There is an increasing interest in identifying eco-friendly farm inputs that can improve crop productivity through sustainable agricultural practices. One of the most common approaches to reducing chemical inputs in agriculture is the use of plant growth regulators (PGRs). Here, we demonstrate the benefits of a natural and novel plant growth enhancer "calliterpenone," isolated from Callicarpa macrophylla, a medicinal plant, for increasing crop productivity in six crops, viz., rice, wheat, potato, tomato, chickpea, and onion. Results revealed that the application of calliterpenone (foliar spraying or seed soaking) enhanced the yield of rice (28.89%), onion (20.63%), potato (37.17%), tomato (28.36%), and chickpea (26.08%) at 0.001 mM and of wheat (27.23%) at 0.01 mM concentrations in comparison to control. This enhancement in yield was reflected through improvements in its growth attributes, viz., spike length, tillers plant-1, seeds spike-1, plant height, and biomass. Furthermore, the exogenous application of calliterpenone could increase the endogenous level of indole-3-acetic acid (IAA) in all tested crops and decrease the content of abscisic acid (ABA) in a few. Trials conducted at farmers' fields showed an overall ~12% increase in rice yield (mean of 11 farmers' fields ranging from 3.48 to 19.63%) and ~10% increase in wheat yield (ranging from 3.91 to 17.51%). The 0.001 mM of calliterpenone was the best effective dose for most crops except wheat, where a concentration of 0.01 mM was found to be the most optimal. This study indicates that calliterpenone is a natural plant growth promoter that can be used in boosting the yields of multiple crops and would be an important input component of organic farming.

20.
Nat Prod Res ; 36(17): 4439-4442, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34570617

RESUMEN

Ravenia spectabilis Engl. belongs to the family Rutaceae is known to possess several biologically active phytomolecules. This study was planned to investigate the chemical composition and antimicrobial activity of the leaf essential oil of R. spectabilis. The hydrodistillation of fresh leaves of R. spectabilis gave 0.19 ± 0.02% essential oil. The resulting essential oil was analysed by gas chromatography-flame ionization detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS). Altogether, thirty-one constituents forming 97.6 ± 1.72% of the total oil composition were identified. Major components of the oil were sabinene (60.8 ± 0.36%), α-pinene (5.4 ± 0.30%), myrcene (4.8 ± 0.25%), δ-3-carene (4.7 ± 0.62%) and ß-pinene (4.3 ± 0.17%). The in-vitro antimicrobial potential of the oil was examined against eight human pathogenic bacterial and fungal strains. The essential oil showed significant activity against Staphylococcus aureus, Staphylococcus epidermidis, methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Candida albicans, and Candida kefyr. This is the first report on R. spectabilis leaf essential oil composition and its antimicrobial activity. The essential oil could be a promising natural source of sabinene and antimicrobial for developing new phytotherapeutics.


Asunto(s)
Antiinfecciosos , Staphylococcus aureus Resistente a Meticilina , Aceites Volátiles , Rutaceae , Antibacterianos/química , Antiinfecciosos/química , Candida albicans , Cromatografía de Gases y Espectrometría de Masas , Humanos , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/química , Hojas de la Planta/química , Rutaceae/química
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