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1.
Molecules ; 27(23)2022 Nov 25.
Artigo em Inglês | MEDLINE | ID: mdl-36500313

RESUMO

Natural products are being targeted as alternative anticancer agents due to their non-toxic and safe nature. The present study was conducted to explore the in vitro anticancer potential of Justicia adhatoda (J. adhatoda) leaf extract. The methanolic leaf extract was prepared, and the phytochemicals and antioxidant potential were determined by LCMS analysis and DPPH radical scavenging assay, respectively. A docking study performed with five major alkaloidal phytoconstituents showed that they had a good binding affinity towards the active site of NF-κB. Cell viability assay was carried out in five different cell lines, and the extract exhibited the highest cytotoxicity in MCF-7, a breast cancer cell line. Extract-treated cells showed a significant increase in nitric oxide and reactive oxygen species production. Cell cycle analysis showed an arrest in cell growth at the Sub-G0 phase. The extract successfully inhibited cell migration and colony formation and altered mitochondrial membrane potential. The activities of superoxide dismutase and glutathione were also found to decrease in a dose-dependent manner. The percentage of apoptotic cells was found to increase in a dose-dependent manner in MCF-7 cells. The expressions of caspase-3, Bax, and cleaved-PARP were increased in extract-treated cells. An increase in the expression of NF-κB was found in the cytoplasm in extract-treated cells. J. adhatoda leaf extract showed a potential anticancer effect in MCF-7 cells.


Assuntos
Neoplasias da Mama , Justicia, Planta , Humanos , Feminino , Justicia, Planta/química , Metanol/química , NF-kappa B/farmacologia , Neoplasias da Mama/tratamento farmacológico , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Células MCF-7 , Folhas de Planta , Apoptose
2.
Mol Biol Rep ; 49(11): 10307-10314, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36097107

RESUMO

BACKGROUND: Justicia adhatoda is an important medicinal plant traditionally used in the Indian system of medicine and the absence of molecular-level studies in this plant hinders its wide use, hence the study was aimed to analyse the genes involved in its various pathways. METHODS AND RESULTS: The RNA isolated was subjected to Illumina sequencing. De novo assembly was performed using TRINITY software which produced 171,064 transcripts with 55,528 genes and N50 value of 2065 bp, followed by annotation of unigenes against NCBI, KEGG and Gene ontology databases resulted in 105,572 annotated unigenes and 40,288 non-annotated unigenes. A total of 5980 unigenes were mapped to 144 biochemical pathways, including the metabolism and biosynthesis pathways. The pathway analysis revealed the major transcripts involved in the tryptophan biosynthesis with TPM values of 6.0903, 33.6854, 11.527, 1.6959, and 8.1662 for Anthranilate synthase alpha, Anthranilate synthase beta, Arogenate/Prephenate dehydratase, Chorismate synthase and Chorismate mutase, respectively. The qRT-PCR validation of the key enzymes showed up-regulation in mid mature leaf when compared to root and young leaf tissue. A total of 16,154 SSRs were identified from the leaf transcriptome of J. Adhatoda ,which could be helpful in molecular breeding. CONCLUSIONS: The study aimed at identifying transcripts involved in the tryptophan biosynthesis pathway for its medicinal properties, as it acts as a precursor to the acridone alkaloid biosynthesis with major key enzymes and their validation. This is the first study that reports transcriptome assembly and annotation of J. adhatoda plant.


Assuntos
Justicia, Planta , Justicia, Planta/genética , Vias Biossintéticas/genética , Anotação de Sequência Molecular , Regulação da Expressão Gênica de Plantas/genética , Antranilato Sintase/genética , Triptofano/genética , Perfilação da Expressão Gênica , Transcriptoma/genética , Sequenciamento de Nucleotídeos em Larga Escala/métodos
3.
Chirality ; 34(11): 1453-1465, 2022 11.
Artigo em Inglês | MEDLINE | ID: mdl-36046957

RESUMO

Chiral compounds find importance as drugs and therapeutic targets. Enantiomers of chiral drugs have been found to show different biological properties like pharmacokinetics, toxicology, pharmacology, metabolism, and so forth. In this study, we have identified the chiral compounds present in the medicinal plant Adhatoda vasica Nees (Justicia adhatoda Linn). Phytochemical investigation on the leaves of Justicia adhatoda resulted in the identification of 27 chiral compounds. We report diverse compounds identified in the crude methanolic extract of Justicia adhatoda leaves by GC-MS analysis exhibiting diverse biological activities. Quantitative analysis of anticancer compound dihydroxycolchicine from the methanolic extract of J. adhatoda leaves was done by external standard method, and the amount of anticancer compound dihydroxycolchicine was found to be 87.823 mg/l indicative of moderate production in the leaves. Therefore, the extract of leaves of Justicia adhatoda can be used as a potential source of chiral bioactive molecules of pharmacological importance for drug synthesis.


Assuntos
Justicia, Planta , Cromatografia Gasosa-Espectrometria de Massas , Justicia, Planta/química , Metanol , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta , Estereoisomerismo
4.
Phytochemistry ; 203: 113410, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36030904

RESUMO

An infusion from the aerial parts of Justicia spicigera Schltdl., an herb commonly used to treat diabetes, inhibited the activity of protein tyrosine phosphatase 1B (PTP1B). Two undescribed compounds, 2-N-(p-coumaroyl)-3H-phenoxazin-3-one, and 3″-O-acetyl-kaempferitrin, along with kaempferitrin, kaempferol 7-O-α-L-rhamnopyranoside, perisbivalvine B and 2,5-dimethoxy-p-benzoquinone were isolated from the active extract. Their structures were elucidated by a combination of spectroscopic and spectrometric methods. The isolates were evaluated for their inhibitory activity against PTP1B; the most active compounds were 2-N-(p-coumaroyl)-3H-phenoxazin-3-one, and perisbivalvine B with IC50 values of 159.1 ± 0.02 µM and 106.6 ± 0.01 µM, respectively. However, perisbivalvine B was unstable. Kinetic analysis of 2-N-(p-coumaroyl)-3H-phenoxazin-3-one and 2,5-dimethoxy-p-benzoquinone (obtained in good amounts) indicated that both compounds behaved as parabolic competitive inhibitors and bind to the enzyme forming complexes with 1:1 and 1:2 stoichiometry. Docking of 2-N-(p-coumaroyl)-3H-phenoxazin-3-one and 2,5-dimethoxy-p-benzoquinone to PTP1B1-400 predicted a good affinity of these compounds for PTP1B catalytic site and demonstrated that the binding of a second ligand is sterically possible. The 1:2 complex was also supported by the second docking analysis, which predicted an important contribution of π-stacking interactions to the stability of these 1:2 complexes. Finally, an UHPLC-MS method was developed and validated to quantify the content of kaempferitrin in the infusion of the plant.


Assuntos
Acanthaceae , Justicia, Planta , Benzoquinonas , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Quempferóis/farmacologia , Cinética , Ligantes , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Proteína Tirosina Fosfatase não Receptora Tipo 1
5.
J Nat Prod ; 85(9): 2184-2191, 2022 09 23.
Artigo em Inglês | MEDLINE | ID: mdl-35998343

RESUMO

Herein, the isolation of secondary metabolites from the aerial parts of Justicia aequilabris guided by HPLC-MSn and molecular networking analyses is reported. Twenty-two known compounds were dereplicated. Three new lignans (aequilabrines A-C (1-3)) and three known compounds (lariciresinol-4'-O-ß-glucose (4), roseoside (5), and allantoin (6)) were obtained. The anti-inflammatory activity of compounds 1-3 was evaluated in vitro by inhibiting the nitric oxide production (NO) and pro-inflammatory activity on the cytokine IL-1ß. Compounds 2 and 3 showed significant inhibitory activity against NO production, with IC50 values of 9.1 and 7.3 µM, respectively. The maximum inhibition of IL-1ß production was 23.5% (1), 27.3% (2), and 32.5% (3).


Assuntos
Anti-Inflamatórios , Justicia, Planta , Lignanas , Alantoína/química , Alantoína/isolamento & purificação , Alantoína/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Furanos/química , Furanos/isolamento & purificação , Furanos/farmacologia , Lignanas/química , Lignanas/isolamento & purificação , Lignanas/farmacologia , Estrutura Molecular , Óxido Nítrico/antagonistas & inibidores , Extratos Vegetais/química
6.
Cell Mol Biol (Noisy-le-grand) ; 67(4): 248-263, 2022 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-35809281

RESUMO

Adhatoda vasica (L.), Nees belonging to the family Acanthaceae is a shrub with opposite ascending branches. The plant has been used in the indigenous system of medicine in India for near about 2500 years. It is a well-known plant as a drug in Ayurvedic and Unani medicines. Traditionally it was used for the treatment of various acute and chronic diseases and showed strong pharmacological activity particularly for bronchial infections, cough, bacterial infections, reproductive disorders, cardiac diseases and many more. Various phytochemicals like alkaloids, flavonoids, tannins, etc. were obtained from Adhatoda vasica (A. vasica). The active constituent of the plant is vasicine, l-vasicinone, deoxyvasicine, maiontone, vasicinolone and vasicinol etc. This review consists of updated information on the phyto-constituents isolated from A. vasica and their potential role in the treatment of various ailments traditionally and medically. Based on the critical review it was concluded that there is not sufficient scientifically strong evidence to explain that A. vasica extract, could be harmful to human beings especially in pregnant women. Major data on traditional uses as well as toxicological studies, evaluated various correctness, relevance, importance, and reliability for the overall evaluation of A. vasica safety. Numerous clinical trials are conducted around the globe on the herbal formulations of vasaka. This review includes strong data about phytochemical and ethnopharmacological studies that indicate that A. vasica is a versatile native plant of the Indian subcontinent having a commercial reputation and thus can be encouraged for diversified applications like medicinal and other potential uses.


Assuntos
Justicia, Planta , Etnobotânica , Feminino , Flavonoides , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Gravidez , Reprodutibilidade dos Testes
7.
J Biotechnol ; 353: 51-60, 2022 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-35691257

RESUMO

Adhatoda vasica is used in the treatment of cold, cough, chronic bronchitis, asthma, diarrhea, and dysentery. The biological activities of this species are attributed with the presence of alkaloids, triterpenoids, and flavonoids. Agrobacterium rhizogenes-mediated transformation of A. vasica, produces pyrroloquinazoline alkaloids, was achieved by infecting leaf discs with strain ATCC15834. The bacterial strain infected 82.7% leaf discs and 5-7 hairy root initials were developed from the cut edges of leaf discs. In this study, seven strains of Azotobacter chroococcum and five strains of Pseudomonas putida were used for the biotization of hairy roots. Plant growth-promoting rhizobacteria (PGPR) develops symbiotic association with roots of plants and increases the growth parameters of plants. PGPR (A. chroococcum and P. putida) increased the profiles of nitrogenase and acid phosphatase enzymes, biomass, dry matter contents, anthranilate synthase activity and accumulation of pyrroloquizoline alkaloids in the biotized hairy roots. Both enzymes (nitrogenase and acid phosphatase) maintain sufficient supply of nitrogen and dissolved phosphorus to the cells of hairy roots therefore, the levels of anthranilate synthase activity and pyrroloquinazoline alkaloids are increased. Total seven pyrroloquinazoline alkaloids (vasicine, vasicinone, vasicine acetate, 2-acetyl benzyl amine, vasicinolone, deoxyvasicine and vasicol) were identified from the biotized hairy roots of A. vasica. In our study, biotization increased the profiles of pyrroloquinazoline alkaloids therefore, this strategy may be used in increasing the production of medicinally important secondary metabolites in other plant species also. Our hypothetical model demonstrates that P. putida cell surface receptors receive root exudates by attaching on hairy roots. After attachment, the bacterial strain penetrates in the biotized hairy roots. This endophytic interaction stimulates acid phosphatase activity in the cells of biotized hairy roots. The P. putida plasmid gene (ppp1) expression led to the synthesis of acid phosphatase in cytosol. The enzyme enhances phosphorus availability as well as induces the formation of phosphoribosyl diphosphate. Later, phosphoribosyl diphosphate metabolizes to tryptophan and finally tryptophan converts to anthranilic acid. The synthesized anthranilic acid used in the synthesis of alkaloids in A. vasica.


Assuntos
Alcaloides , Justicia, Planta , Pseudomonas putida , Fosfatase Ácida/metabolismo , Alcaloides/metabolismo , Alcaloides/farmacologia , Antranilato Sintase/genética , Antranilato Sintase/metabolismo , Azotobacter , Difosfatos/metabolismo , Nitrogenase/metabolismo , Fósforo/metabolismo , Raízes de Plantas/metabolismo , Pseudomonas putida/genética , Triptofano/metabolismo
8.
Biomed Pharmacother ; 153: 113322, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35763968

RESUMO

Plants are regarded as a valuable and inexpensive source of new drug development, and a variety of plant compounds are now being used in clinical trials to treat a variety of ailments. The goal of this work was to characterize and evaluate the anti-inflammatory and antioxidant effects of Justicia adhatoda L. leaf extract (Acanthaceae). The presence of alkaloids, saponins, tannins, phytosterols, phenols, and proteins in the leaf extract of J. adhatoda was determined using phytochemical screening. While the identification of different compounds in the leaf extract was carried out by HPLC analysis. Similarly, the anti-inflammatory potential of the leaf extract was assessed in Carrageenan and Formalin-induced inflammatory mice models. The phytochemical analysis of the leaf extract indicated a positive test for alkaloids, saponins, tannins, phytosterols, phenols, proteins, and amino acids, while the negative test for carbohydrates, and glycosides, flavonoids, and diterpenes. Moreover, among the detected compounds, gallic acid was found in the highest concentration with a 45.42% composition. The leaf extract showed the highest antibacterial activity against E. coli, while the lowest activity against Listeria was observed. The leaf extract of J. adhatoda revealed promising anti-inflammatory, analgesic, and antioxidants activities both in vitro and in vivo. Similarly, the detected compounds portrayed variable pharmacokinetic as well as binding affinities with the target proteins. In conclusion, the leaf extract exhibited significant antioxidants and antibacterial activities using in vitro assays. Similarly, the extract also revealed promising anti-inflammatory activities in vivo while exhibiting variable Pharmacokinetics and binding affinities towards protein target using computational tools.


Assuntos
Acanthaceae , Alcaloides , Justicia, Planta , Fitosteróis , Saponinas , Analgésicos/uso terapêutico , Animais , Antibacterianos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Antioxidantes/farmacologia , Carragenina , Escherichia coli , Formaldeído , Justicia, Planta/química , Camundongos , Estresse Oxidativo , Fenóis , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/uso terapêutico , Folhas de Planta , Saponinas/farmacologia , Taninos/farmacologia
9.
J Ethnopharmacol ; 294: 115392, 2022 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-35589019

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Justicia procumbens L. is a traditional Chinese medicine, first recorded in "Shen Nong's Herbal Classic", for the treatment of lumbar pain and fever. As a widely distributed herb, it has also been documented in India, Nepal, and Malaysia. In "Tang Materia Medica", a famous medicinal book of Tang Dynasty in ancient China, it was first used to treat diseases associated with blood stasis. Blood stasis syndrome is closely related to thrombus formation and platelet aggregation. Although some compounds isolated from this plant have anti-platelet aggregation effects, the main chemical components and mechanism of J. procumbens in terms of these effects are little known. AIMS OF THE STUDY: Through in vivo and in vitro experiments, this studsy revealed the characteristic components and action mechanism of anti-platelet aggregation by J. procumbens from an overall perspective. MATERIALS AND METHODS: The effective crude extracts of the whole plant were screened via an in vitro anti-platelet aggregation test. After incubating these extracts with apheresis platelets, high affinity compounds were detected by HPLC-MS and regulatory genes were detected using gene chips. The effective components and potential target proteins were analyzed using computational docking technology. Furthermore, the compound with the strongest predicted activity was evaluated in vivo via an anti-thrombotic test. RESULTS: Integrin aⅡbß3, PKCα, PI3Kγ, and mitogen-activated protein kinase 14 were found to be potential targets. Justicidin B, tuberculatin, chinensinaphthol methyl ether, and neojusticin B were effective compounds that inhibited human platelet aggregation by suppressing Gq-PLC-PKC and Gi-PI3K-MAPK signaling pathways. Among the compounds that bind to platelets, justicidin B showed the strongest virtual binding force. The test of carotid artery thrombosis induced by ferric chloride in SD rats confirmed that justicidin B inhibited thrombus formation. CONCLUSION: Experimental investigation showed that arylnaphthalene lignan aglycones with one methylenedioxy group and two methoxy groups are effective components for anti-platelet aggregation by J. procumbens. These compounds inhibit Gq-PLC-PKC and Gi-PI3K-MAPK signaling pathways by suppressing the expression of genes such as ITGB3, PRKCA, PIK3CG, and MAPK14. These results reflected the characteristics of multi-component and multi-target synergistic treatment of Chinese medicine.


Assuntos
Justicia, Planta , Animais , Cromatografia Líquida de Alta Pressão/métodos , Justicia, Planta/química , Fosfatidilinositol 3-Quinases , Agregação Plaquetária , Inibidores da Agregação Plaquetária/química , Inibidores da Agregação Plaquetária/farmacologia , Ratos , Ratos Sprague-Dawley
10.
Nutrients ; 14(9)2022 May 06.
Artigo em Inglês | MEDLINE | ID: mdl-35565913

RESUMO

Oxidative stress is a factor that contributes to the development of complications in diabetes; however, its effects can be counteracted using exogenous antioxidants that are found in some plants, which is why people turn to traditional medicines in the search for therapeutic treatment. Justicia spicigera has been demonstrated to have the capacity to reduce glycemic levels; however, its effects on non-insulin-dependent organs such as the liver have not been reported. During 30 days of administration of Justicia spicigera ethanol extract, the blood glucose and weight of rats were measured every 5 days. Once the treatment was concluded, the rats were sacrificed. Corporal weight, blood glucose, cholesterol, very-low-density lipoprotein (VLDL), triglycerides, total lipids, and liver profile were reduced in the diabetic condition and normalized with the application of ethanol extract from J. spicigera (EJS). Additionally, there was a significant increase in catalase and superoxide dismutase activity in the control diabetic rats, a decrease in their activity with the extract administration, and no effect on normoglycemic rats. In conclusion, EJS is considered to be capable of reducing oxidative stress by maintaining diminished lipid and liver function profiles in male Wistar rats with streptozotocin-induced diabetes.


Assuntos
Diabetes Mellitus Experimental , Justicia, Planta , Animais , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Glicemia , Diabetes Mellitus Experimental/tratamento farmacológico , Etanol/farmacologia , Humanos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Masculino , Estresse Oxidativo , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar , Estreptozocina
11.
Rev. bioét. derecho ; (54): 23-46, Mar. 2022.
Artigo em Espanhol | IBECS | ID: ibc-210213

RESUMO

The effects of COVID-19 pandemic depend on socio-cultural determinants that shield some individuals or groups from the most severe effects or make others more vulnerable to suffering harms to their health, social position, or economic stability. The case of vaccination is symptomatic of how specific groups suffer a higher degree of vulnerability due to socioeconomic inequalities and cultural determinants. Consequently, vaccine hesitancy among these groups might deepen the vulnerabilities, which is why it is necessary to design strategies that, while confronting vaccine hesitancy, do not ignore those structural inequalities which could continue feeding skepticism and resistance to vaccination, if unattended. In this work we claim that public health policies focused on promoting vaccination may benefit from a syndemic approach that considers the synergies between diseases and socioeconomic and cultural determinants. This implies introducing social justice issues into the planning of public health strategies. By critically analyzing the work of bioethicist Norman Daniels —who goes over the moral importance of public health from an interpretation of John Rawls’ theory of justice—we explore the criticism to justice as fairness made by the communitarian and the politics of difference standpoints (specifically, I. M. Young), to show that a syndemic approach to public health is essential to achieve complete vaccination: the design of strategies will have to consider the specific contexts of vaccine hesitant groups, to achieve efficiency vaccinating in the short, medium and long term.(AU)


Las afectaciones por la pandemia de COVID-19 dependen de determinantes socio-culturales que blindan a algunos individuos o grupos de los efectos más severos o vuelven a otros más susceptibles de sufrir daños a su salud, posición social o estabilidad económica. El caso de la vacunación es sintomático de cómo grupos específicos sufren mayor vulnerabilidad por inequidades socioeconómicas y determinantes culturales. Consecuentemente, la resistencia a la vacunación entre estos grupos puede profundizar la vulnerabilidad, por lo que es necesario diseñar estrategias que, al confrontar la resistencia a la vacunación, no dejen de lado aquellas inequidades estructurales que, de no atenderse, seguirán alimentando la suspicacia y renuencia a vacunarse. En este trabajo sostenemos que las políticas de salud pública enfocadas a promover la vacunación pueden beneficiarse de un enfoque sindémico que considere las sinergias entre enfermedades y determinantes socioeconómicas y culturales. Esto implica introducir problemas de justicia social en la planificación de estrategias de salud pública. Haciendo un análisis crítico del trabajo del bioeticista Norman Daniels —quien aborda la importancia moral de la salud pública desde una interpretación de la teoría de la justicia de John Rawls—retomamos las críticas a la justicia como imparcialidad de las posturas comunitarista y delas políticas de la diferencia (específicamente I. M. Young), para mostrar que un enfoque sindémico de la salud pública es indispensable para lograr una vacunación completa: el diseño de estrategias tendrá que considerar los contextos específicos de grupos renuentes a vacunarse para lograr eficiencia a corto, mediano y largo plazo.(AU)


Les afectacions per la pandèmia de COVID-19 depenen de determinants socioculturals que blinden a alguns individus o grups dels efectes més severs o tornen a uns altres més susceptibles de sofrir danys a la seva salut, posició social o estabilitat econòmica. El cas de la vacunació és simptomàtic de com grups específics sofreixen major vulnerabilitat per inequitats socioeconòmiques i determinants culturals. Conseqüentment, la resistència a la vacunació entre aquests grups pot aprofundir la vulnerabilitat, per la qual cosa és necessari dissenyar estratègies que, en confrontar la resistència a la vacunació, no deixin de costat aquelles inequitats estructurals que, de no atendre's, continuaran alimentant la suspicàcia i renuència a vacunar-se. En aquest treball sostenim que les polítiques de salut pública enfocades a promoure la vacunació poden beneficiar-se d'un enfocament sindèmic que consideri les sinergies entre malalties i determinants socioeconòmiques i culturals. Això implica introduir problemes de justícia social en la planificació d'estratègies de salut pública. Fent una anàlisi crítica del treball del bioeticista Norman Daniels —qui aborda la importància moral de la salut pública des d'una interpretació de la teoria de la justícia de John Rawls—reprenem les crítiques a la justícia com a imparcialitat de les postures comunitarista i de les polítiques de la diferència (específicament I. M. Young), per a mostrar que un enfocament sindèmic de la salut pública és indispensable per a aconseguir una vacunació completa: el disseny d'estratègies haurà de considerar els contextos específics de grups renuents a vacunar-se per a aconseguir eficiència a curt, mitjà i llarg termini.(AU)


Assuntos
Humanos , Justiça Social , Vacinação , Pandemias , Betacoronavirus , Infecções por Coronavirus , Vírus da SARS , Recusa de Vacinação , 50207 , Sindemia , Vulnerabilidade a Desastres , Bioética , Direitos Humanos , Ética , Princípios Morais , Justicia, Planta , Fatores Socioeconômicos
12.
J Biomol Struct Dyn ; 40(6): 2785-2796, 2022 04.
Artigo em Inglês | MEDLINE | ID: mdl-33222622

RESUMO

Inflammation plays a major role in the onset and progression of many diseases related to the respiratory system. Cysteinyl leukotrienes, the products of 5-LOX are a potent bronchoconstrictor. Vasicine, vasicinone and deoxyvasicine are the pyrroquinazoline alkaloids of Adhatoda vasica that are well known for their bronchodilatory activity. The current investigation evaluates the 5-LOX inhibitory potential of these alkaloids. Molecular docking results indicated that these alkaloids have similar binding energy as that of Zileuton, a commercial drug. Analysis of the molecular dynamics simulations, the binding free energy derived from MM-PBSA and interaction entropy indicated that vasicinone (-8.33 kcal/mol) exhibited a binding free energy comparable to that of Zileuton (-8.52 kcal/mol). The in-vitro results indicate the potential of vasicinone as a competitive inhibitor, while the in-silico results highlighted the potential of vasicine and deoxyvasicine as allosteric inhibitors. A possible mechanism behind the activity exhibited by the plant was also determined, which emphasized the potential of these alkaloids as leads for the design of novel 5-LOX inhibitors.


Assuntos
Alcaloides , Justicia, Planta , Alcaloides/química , Justicia, Planta/química , Justicia, Planta/metabolismo , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia
13.
J Biomol Struct Dyn ; 40(16): 7245-7255, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-33715610

RESUMO

Eicosanoid pathways play a crucial role in the progression and resolution of inflammation. NSAIDs act as anti-inflammatory agents by inhibiting both the isoforms of cyclooxygenases (COXs) whereas, COXIBs act as specific COX-2 inhibitors. Excessive usage of the same is linked with gastrointestinal bleeding and increased cardiovascular risk, respectively. The current in-silico study was aimed at evaluating the potential of major alkaloids of A. vasica (vasicine (VAS), vasicinone (VAE), and Deoxyvasicine (DOV)) as inhibitors of COXs. The results of the computed binding energy (ΔG) indicate that Celecoxib (CEL), DOV, and VAS have a higher affinity to COX-2, while VAE has a higher affinity to COX-1, and Mefenamic acid (MEF) was not selective. Among the alkaloids, VAE exhibited the best ΔG (of -8.2 kcal/mol) with COX-1, while VAS exhibited the best ΔG (of -8.2 kcal/mol) with COX-2. This was comparable to the ΔG exhibited by Mefenamic acid (-8.7 kcal/mol with both the COXs). With their potential to remain gastroprotective while having the ability to inhibit enzymes of both the prostaglandin and leukotriene pathways, the alkaloids of A. vasica could be promising leads for the design of Eicosanoid pathway modulators/inhibitors.Communicated by Ramaswamy H. Sarma.


Assuntos
Alcaloides , Justicia, Planta , Alcaloides/metabolismo , Anti-Inflamatórios/farmacologia , Ciclo-Oxigenase 2 , Inibidores de Ciclo-Oxigenase 2/farmacologia , Justicia, Planta/metabolismo , Ácido Mefenâmico
14.
J AOAC Int ; 105(1): 267-271, 2022 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-34459903

RESUMO

BACKGROUND: Adhatoda vasica L. is a medicinal plant, known as Malabar nut in English, belonging to the family Acanthaceae. It has been used traditionally to treat respiratory disorders like severe coughs, colds, chronic bronchitis, asthma, tuberculosis, and other illnesses. The multifunctional range of bioactives found in it has piqued the interest of pharmaceutical companies, who are looking for more evidence-based ways to develop new formulations. OBJECTIVE: To analyse the A. vasica leaves by GC-MS technique and evaluation of its antioxidant activity. METHOD: Methanolic extract of A. vasica L. (MEAV) leaves was analyzed by GC-MS for identification and characterization of its bioactives and traditional therapeutic claims. A widely anticipated 2,2-diphenyl-1-picrylhydrazyl (DPPH) method was used to determine the antioxidant activity of MEAV. RESULTS: The major compounds revealed in MEAV leaves are: 1,3,5-triazine-2,4,6-triamine (3.06%); 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one (5.35%); 5-hydroxymethylfurfural (16.82%); 2-butylphenol (6.85%); 3,4-dihydroxy-5-methyl-dihydro-furan-2-on (2.5%); 2(OR 3)-(1,1-dimethylethyl)-4-methoxyphenol (3.52%); megastigmatrienone 3 (1.02%); tetradecanoic acid (1.52%); vomifoliol (0.58%); oxalic acid, cyclobutylhexyl ester (6.03%); hexadecanoic acid (6.06%); 4-ethyl-2-oxo-2,5,6,7-tetrahydro-1H-cyclopenta[B]pyridine-3-carbonitrile (10.08%); phytol (2.01%); and vitamin E (3.18%). A significant reduction in free radicals against DPPH was observed, which revealed the antioxidant potential of MEAV. CONCLUSION: MEAV consists of both polar and nonpolar components. GC-MS analysis was used to identify these compounds. The current work validates that the antioxidant activity of MEAV is attributed to the presence of compounds such as vitamin E and terpenes. HIGHLIGHTS: This work validates the antioxidant activity of methanolic extract of A. vasica attributed to the presence of compounds like vitamin E and terpenes.


Assuntos
Justicia, Planta , Antioxidantes/análise , Cromatografia Gasosa-Espectrometria de Massas , Metanol , Extratos Vegetais , Folhas de Planta/química
15.
Microsc Res Tech ; 85(5): 1757-1767, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-34953112

RESUMO

This article reports the three principal groups of compounds for the first time from Adhatoda vasica and Calotropis procera plants species using nuclear magnetic resonance methods in which aliphatic, oxy heterocyclic, and tannins compounds were detected from these plants. The leaves of both species were subjected to testing tyrosinase inhibition and antioxidant activities. ATP bioluminescence use for indirect measurement of the amount of organic residue on the surface of the leaves that provide support to microbial growth. The distinguishing characteristics and intraoperative findings of bacterial diseases involved in treatments were conducted against the positive and negative microbial strains using a scanning electron microscope (SEM). The methanolic extracts of leaves of both species were applied to bacterial strains through broth microdilution method to determine the minimum inhabitation concentrations (MICs) for both species. It was concluded that both plants are a rich resource of bioactive compounds. Their extract may also be used to treat various bacterial diseases and in drug manufacturing. HIGHLIGHTS: New chemical compounds of oxy-heterocyclic, aliphatic, and tannins derivatives are isolated from herbal plants as a source of various drugs. 1 H NMR spectrum and 13 C NMR spectrum of each new derivate were calculated. NMR-spectral analysis of new compound of chemistry class was studied and further applied in various bacterial strains. Tyrosinase inhibition property of bacteria strains by application of active compounds on these strains. Agar overlay bioassays were used to evaluate intercellular morphological features of strains applied on extracts by electron microscope (SEM). a-Glucosidase inhibition assay determined with antioxidants activity through FRAP assay methods.


Assuntos
Calotropis , Justicia, Planta , Antioxidantes/farmacologia , Bioensaio , Calotropis/química , Justicia, Planta/química , Monofenol Mono-Oxigenase , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Taninos/farmacologia
16.
J Ethnopharmacol ; 287: 114942, 2022 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-34968664

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Justicia vahlii Roth. (Acanthaceae), also called as kodasoori and bhekkar is an annual therophyte erect or decumbent herb used traditionally in toothache, skin diseases (itching, topical inflammation) and for the treatment of various respiratory disorders. AIM OF THE STUDY: The current study aimed at exploring pain cessation potential of J. vahlii Roth. via murine model of neuropathic pain and its phytochemical, toxicological and antioxidant profiles. MATERIALS AND METHODS: The hydro-alcoholic extract of J. vahlii (HAEJv) prepared by maceration technique was subjected to preliminary phytochemical screening, total bioactive content determination, UPLC-QTOF-MS and GC-MS analysis. Toxicity assessment was carried out by using brine shrimp lethality assay and acute oral toxicity test. Murine model of neuropathic pain was applied to assess the antineuropathic potential of the species. Furthermore effect of the extract on catalase, superoxide oxide dismutase (SOD), Glutathione (GSH), interleukin-1beta (IL-1ß) and total necrosis factor-alpha (TNF-α) was also studied. In vitro antioxidant profile was explored by using four methods; 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azinobis(3-ethylbenothiazoline)-6-sulfonic acid (ABTS), CUPric reducing antioxidant capacity (CUPRAC) and Ferric reducing antioxidant power (FRAP) assay. RESULTS: The phytochemical screening revealed the presence of phenols, flavonoids, coumarins, alkaloids and lignans as the major classes of secondary metabolites. The extract was found rich in total phenolics content (TPC) and total flavonoids content (TFC) with identification of total 59 bioactives in UPLC-QTOF-MS and 40 compounds in GC-MS analysis. The extract was found nontoxic up to 4000 mg/kg (p.o.) in mice and no mortality observed in brine shrimp lethality assay. The HAEJv significantly reduced number of acetic acid induced abdominal constrictions at 100 mg/kg (p < 0.01) and 200 mg/kg (p < 0.001) and increased paw withdrawal threshold p < 0.05 at 100 mg/kg and p < 0.001 at 200 mg/kg, and an increase in tail withdrawal latency time p < 0.001 at 200 mg/kg was observed. The extract significantly increased levels of catalase, SOD and GSH while decreased IL-1ß and TNF-α levels in sciatic nerve tissue of mice. HAEJv showed highest antioxidant activity through CUPRAC method 121.32 ± 1.22 mg trolox equivalent per gram of dry extract (mg TE/g DE) followed by DPPH 81.334 ± 4.35 mg TE/g DE, FRAP 69.89 ± 3.05 mg TE/g DE and ABTS 38.17 ± 2.12 mg TE/g DE. CONCLUSION: The current study back the traditional use of J. vahlii in pain cessation through antioxidant based antineuropathic pain activity and revealed the extract non-toxic with number of functional phytoconstituents and warrants further research on isolation of the compounds and sub-acute toxicity studies.


Assuntos
Antioxidantes/farmacologia , Justicia, Planta/química , Neuralgia/tratamento farmacológico , Extratos Vegetais/farmacologia , Analgésicos/administração & dosagem , Analgésicos/isolamento & purificação , Analgésicos/farmacologia , Animais , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Artemia , Cromatografia Líquida de Alta Pressão , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Cromatografia Gasosa-Espectrometria de Massas , Espectrometria de Massas , Camundongos , Camundongos Endogâmicos BALB C , Extratos Vegetais/toxicidade , Testes de Toxicidade Aguda
17.
Cult. cuid ; 26(63): 1-13, 2do cuatrimestre, 2022.
Artigo em Espanhol | IBECS | ID: ibc-206680

RESUMO

Background: Was there bioethics before Potter? Certainly yes, and a clear example is the Nursingof San Juan de Dios, father of modern Nursing of the s. XVI. After performing various trades, it will bein Granada where he will reform the socio-health care by observing the great inequalities between peopledue to a social and individual conscience numbed by the sense of honor; developing a high sense ofotherness, being his being, the other, framed within a community. And since the poor were his focus ofaction, the sick were his priority, since they were the most disadvantaged dying on the streets of Granada.Aim: Therefore, in this study we propose to describe the principle of Justice and Equality in San Juan deDios through his care, influenced by his Master San Juan de Ávila. Methodology: For this we resort tothe historiographic-hermeneutic method, being the documentary sources the texts of the same closest totheir time. Results-Conclusion: In them we have been able to observe how their spirituality led them totake care of all kinds of people, being the poor, sick, women and children, the center of their actions.However, he took care of the entire population, awakening solidarity among the entire population,making them co-responsible for all their hospital reform through material and human resources. (AU)


Introducción: ¿Existía bioética antes de Potter? Ciertamente sí, y un claro ejemplo es laEnfermería de San Juan de Dios, padre de la Enfermería moderna del s. XVI. Tras desempeñar diversosoficios, será en Granada donde reformará la atención socio-sanitaria al observar las grandesdesigualdades entre personas por una conciencia social e individual adormecida por el sentido del honor;desarrollando un alto sentido de la alteridad, siendo su ser, el otro, enmarcado dentro de una comunidad.Y siendo los pobres su foco de actuación, los enfermos fueron su prioridad, pues eran los másdesfavorecidos muriendo por las calles de Granada. Objetivo: En este estudio nos proponemos describirel principio de Justicia e Igualdad en San Juan de Dios a través de sus cuidados, influido por su MaestroSan Juan de Ávila. Metodología: Para ello recurrimos al método historiográfico-hermenéutico, siendo lasfuentes documentales los textos de los mismos más cercanos a su tiempo. Resultados-Conclusión: Enellos hemos podido observar cómo su espiritualidad les llevó a atender a todo género de personas, siendolos pobres, enfermos, mujeres y niños, el centro de su actuación. Sin embargo, cuidó a toda la poblacióndespertando la solidaridad en toda persona haciéndoles co-responsables de toda su reforma hospitalariamediante recursos materiales y humanos. (AU)


Introdução: Havia bioética antes de Potter? Certamente sim, e um exemplo claro é a Enfermagemde San Juan de Dios, pai da Enfermagem moderna do s. XVI. Depois de realizar vários ofícios, será emGranada onde irá reformar o sistema sócio-sanitário observando as grandes desigualdades entre aspessoas devido a uma consciência social e individual entorpecida pelo sentido da honra; desenvolver umalto senso de alteridade, sendo seu ser, o outro, enquadrado em uma comunidade. E como os pobres eramo seu foco de ação, os doentes eram a sua prioridade, pois eram os mais desfavorecidos morrendo nasruas de Granada. Objetivo: Portanto, neste estudo, propomos descrever o princípio da Justiça e daIgualdade em San Juan de Dios com seus cuidados, influenciados por seu Mestre San Juan de Ávila.Metodologia: Para isso, recorremos ao método historiográfico-hermenêutico, sendo as fontesdocumentais os textos mais próximos do seu tempo. Resultados-Conclusão: Neles, conseguimos observarcomo sua espiritualidade os levou a cuidar de todos os tipos de pessoas, sendo pobres, doentes, mulherese crianças, o centro de suas ações. No entanto, ele cuidou de toda a população, despertando asolidariedade entre toda a população, tornando-os co-responsáveis por toda a reforma hospitalar atravésde recursos materiais e humanos. (AU)


Assuntos
Humanos , História da Enfermagem , Bioética/história , Justicia, Planta , 17627/história
18.
Molecules ; 26(22)2021 Nov 18.
Artigo em Inglês | MEDLINE | ID: mdl-34834066

RESUMO

Angiotensin converting enzyme (ACE) plays a crucial role in regulating blood pressure in the human body. Identification of potential ACE inhibitors from medicinal plants supported the idea of repurposing these medicinal plants against hypertension. A method based on ultra-performance liquid chromatography (UPLC) coupled with a diode array detector (DAD) was used for the rapid screening of plant extracts and purified compounds to determine their ACE inhibitory activity. Hippuryl-histidiyl-leucine (HHL) was used as a substrate, which is converted into hippuric acid (HA) by the action of ACE. A calibration curve of the substrate HHL was developed with the linear regression 0.999. The limits of detection and quantification of this method were found to be 0.134 and 0.4061 mM, respectively. Different parameters of ACE inhibitory assay were optimized, including concentration, incubation time and temperature. The ACE inhibition potential of Adhatoda vasica (methanolic-aqueous extract) and its isolated pyrroquinazoline alkaloids, vasicinol (1), vasicine (2) and vasicinone (3) was evaluated. Compounds 1-3 were characterized by various spectroscopic techniques. The IC50 values of vasicinol (1), vasicine (2) and vasicinone (3) were found to be 6.45, 2.60 and 13.49 mM, respectively. Molecular docking studies of compounds 1-3 were also performed. Among these compounds, vasicinol (1) binds as effectively as captopril, a standard drug of ACE inhibition.


Assuntos
Alcaloides/farmacologia , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Justicia, Planta/química , Extratos Vegetais/farmacologia , Quinazolinas/farmacologia , Alcaloides/química , Inibidores da Enzima Conversora de Angiotensina/química , Cromatografia Líquida de Alta Pressão , Descoberta de Drogas , Avaliação Pré-Clínica de Medicamentos , Humanos , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Quinazolinas/química
19.
Pak J Biol Sci ; 24(11): 1162-1168, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34842388

RESUMO

<b>Background and Objective:</b> <i>Justicia gendarussa </i>(family <i>Acanthaceae</i>) is regarded as a medicinal plant valued for its beneficial pharmacological activities. A polybag experiment has been conducted at Bogor (Indonesia) to determine the effects on growth, photosynthetic and yield of various NPK ratios and manure fertilizer application in <i>J. gendarussa</i>. <b>Materials and Methods:</b> Six treatments (control: 50 g/plant manure, NPK (1.1 g/plant N:0.7 g/plant P<sub>2</sub>O<sub>5</sub> and 0.6 g/plant K), 50+50%/plant (manure+NPK), 10+50%/plant (manure+NPK) and 50+10%/plant (manure+NPK) were performed in a randomized complete block design. Data of individual plants were extracted from various treatments: plant height, number of leaves, number of branches, chlorophyll content, photosynthetic parameters, yield and sugar content were collected. <b>Results:</b> The plant treated with 10+50%/plant (manure+NPK) demonstrated a statistically significant increase in plant height, number of leaves and number of branches with the value of 59.00 cm, 85.00 per plant and 9.50 per plant, respectively. Chlorophyll a (0.538 mg g<sup>1</sup> FW), chlorophyll b (0.192 mg g<sup>1</sup> FW) and total chlorophyll (0.730 mg g<sup>1</sup> FW) were significantly improved by the treatment of NPK fertilizer. The application of manure and NPK at (50+50%) and (50+10%) was significantly increased stomatal conductance and transpiration rate, respectively. Leaves yield (9 g/plant DW) was improved by the application of 10+50%/plant (manure+NPK) fertilizer. The highest sugar content was obtained from <i>J. gendarussa</i> growth with 50+50%/plant (manure+NPK) followed by 10+50% plant (manure+NPK) fertilizer. <b>Conclusion:</b> The <i>J. gendarussa</i> plants could benefit from combined manure and NPK fertilizer application in growth, stomatal conductance, intercellular CO<sub>2</sub> concentration, transpiration rate, leaves yield and sugar content.


Assuntos
Justicia, Planta/efeitos dos fármacos , Justicia, Planta/crescimento & desenvolvimento , Esterco , Fotossíntese/fisiologia , Indonésia , Justicia, Planta/fisiologia
20.
IET Nanobiotechnol ; 15(4): 391-401, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-34694712

RESUMO

Biogenic silica synthesised from rice husk was used as a controlled release system of an eco-friendly biocide consisting of a Justicia adhatoda extract. Fourier-transform infrared spectroscopy (FTIR) indicated the presence of ester bonds between the silica support and the conjugated Justicia adhatoda extract. Surface area analysis and microscopy confirmed a high level of Justicia adhatoda extract loading in the silica support. The phytochemical investigation of Justicia adhatoda was done by Gas chromatography-mass spectrometry (GC-MS) spectroscopy. Moreover, compared with the naked biogenic silica nanoparticles, a better thermal stability was determined for the conjugated system of the extracted compounds. Trial of kinetic release of silica: Justicia adhatoda ∼29% of loaded Justicia adhatoda was released within 1 h and then the rate of release became slow. Net release of Justicia adhatoda was observed up to 50% within 7 h. The Justicia adhatoda compounds released from silica also showed the improved mortality rate against stored product pest rice weevil (Sitophilus oryzae).


Assuntos
Desinfetantes , Justicia, Planta , Nanopartículas , Extratos Vegetais , Folhas de Planta , Dióxido de Silício
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