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1.
Sci Total Environ ; 722: 137907, 2020 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-32208265

RESUMO

Natural products (NPs) will continue to serve humans as matchless source of novel drug leads and an inspiration for the synthesis of non-natural drugs. As our scientific understanding of 'nature' is rapidly expanding, it would be worthwhile to illuminate the pharmacological distinctions of NPs to the scientific community and the public. Flavonoids have long fascinated scientists with their remarkable structural diversity as well as biological functions. Consequently, this review aims to shed light on the sources and pharmacological significance of a dietary isoflavone, biochanin A, which has been recently emerged as a multitargeted and multifunctional guardian of human health. Biochanin A possesses anti-inflammatory, anticancer, neuroprotective, antioxidant, anti-microbial, and hepatoprotective properties. It combats cancer development by inducing apoptosis, inhibition of metastasis and arresting cell cycle via targeting several deregulated signaling pathways of cancer. It fights inflammation by blocking the expression and activity of pro-inflammatory cytokines via modulation of NF-κB and MAPKs. Biochanin A acts as a neuroprotective agent by inhibiting microglial activation and apoptosis of neurons. As biochanin A has potential to modulate several biological networks, thus, it can be anticipated that this therapeutically potent compound might serve as a novel lead for drug development in the near future.

2.
Biofactors ; 2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-32039535

RESUMO

Reprogrammed metabolism is key biochemical characteristic of malignant cells, which represents one of the emerging hallmarks of cancer. Currently, there is rising contemplation on oxidative pentose phosphate pathway (PPP) enzymes as potential therapeutic hits due to their affiliation with tumor metabolism. 6-Phosphogluconate dehydrogenase (6PGD), third oxidative decarboxylase of PPP, has received a great deal of attention during recent years due to its critical role in tumorigenesis and redox homeostasis. 6PGD has been reported to overexpress in number of cancer types and its hyperactivation is mediated through post-transcriptional and post-translational modifications by YTH domain family 2 (YTHDF2), Nrf2 (nuclear factor erythroid 2-related factor 2), EGFR (epidermal growth factor receptor) and via direct structural interactions with ME1 (malic enzyme 1). Upregulated expression of 6PGD provides metabolic as well as defensive advantage to cancer cells, thus, promoting their proliferative and metastatic potential. Moreover, enhanced 6PGD expression also performs key role in development of chemoresistance as well as radiation resistance in cancer. This review aims to discuss the historical timeline and cancer-specific role of 6PGD, pharmacological and genetic inhibitors of 6PGD and 6PGD as prognostic biomarker in order to explore its potential for therapeutic interventions. We anticipate that targeting this imperative supplier of NADPH might serve as tempting avenue to combat the deadly disease like cancer.

3.
J Pharm Biomed Anal ; 181: 113122, 2020 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-31991320

RESUMO

The headspace gas chromatographic method has been widely used to detect volatile metabolites to reflect the growth state of microorganisms, however, it has never been used for the determination of the minimum inhibitory concentration in antibacterial drugs. This paper reports a new method for evaluating the antimicrobial activity of drugs by measuring the amount of CO2 produced by bacterial metabolism after treatment with drugs. According to the amount of CO2 produced by bacterial metabolism, a proper amount of bacterial liquid is selected and added to a drug-containing culture medium as compared with bacteria without drugs in parallel. The amount of CO2 produced by bacteria is measured by using a headspace gas chromatograph coupled with a thermal conductivity detector to measure the bacteriostasis rate and the minimum bacteriostasis concentration of the tested drug, so as to evaluate its antibacterial activity. The accuracy of this method was verified by comparison with the standard method (the OD method), which indicated that the precision was less than 3 % (expressed by relative standard deviation), the inhibition rate (R2 = 0.968) was consistent with the reference method above. This method is simple in operation and can avoid the error caused by the properties of the sample such as volatility, solubility and color in the determination of the minimum inhibitory concentration. It is suitable for the determination of antibacterial activity of drugs, especially natural drugs.

4.
Phytochem Anal ; 31(2): 135-146, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31469459

RESUMO

INTRODUCTION: Cannabinoids are organic compounds, natural or synthetic, that bind to the cannabinoid receptors and have similar pharmacological properties as produced by the cannabis plant, Cannabis sativa. Gas chromatography (GC), e.g. gas chromatography mass spectrometry (GC-MS), is a popular analytical tool that has been used extensively to analyse cannabinoids in various matrices. OBJECTIVE: To review published literature on the use of various GC-based analytical methods for the analysis of naturally occurring cannabinoids published during the past decade. METHODOLOGY: A comprehensive literature search was performed utilising several databases, like Web of Knowledge, PubMed and Google Scholar, and other relevant published materials including published books. The keywords used, in various combinations, with cannabinoids being present in all combinations, in the search were cannabinoids, Cannabis sativa, marijuana, analysis, GC, quantitative, qualitative and quality control. RESULTS: During the past decade, several GC-based methods for the analysis of cannabinoids have been reported. While simple one-dimensional (1D) GC-MS and GC-FID (flame ionisation detector) methods were found to be quite common in cannabinoids analysis, two-dimensional (2D) GC-MS as well as GC-MS/MS also were popular because of their ability to provide more useful data for identification and quantification of cannabinoids in various matrices. Some degree of automation in sample preparation, and applications of mathematical and computational models for optimisation of different protocols were observed, and pre-analyses included various derivatisation techniques, and environmentally friendly extraction protocols. CONCLUSIONS: GC-based analysis of naturally occurring cannabinoids, especially using GC-MS, has dominated the cannabinoids analysis in the last decade; new derivatisation methods, new ionisation methods, and mathematical models for method optimisation have been introduced.


Assuntos
Canabinoides , Cannabis , Cromatografia Gasosa-Espectrometria de Massas , Espectrometria de Massas em Tandem
5.
Phytochem Anal ; 31(1): 5-14, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31370102

RESUMO

INTRODUCTION: Artemisinin (1), a well-known natural antimalarial drug, is a sesquiterpene lactone that contains a unique peroxide bridge. Since its discovery, the amount of research into the analysis of artemisinin has increased considerably, and it has been further intensified since the Noble Prize win by Tu Youyou in the year 2015 for the discovery of artemisinin. OBJECTIVE: To review literature on the extraction and analysis of artemisinin, published during 2017-present, and to present an appraisal of those methods. METHODOLOGY: Extensive literature search was carried out which involved, but not limited to, the use of, various databases, like Web of Knowledge, PubMed and Google Scholar, and relevant published materials including published books. The keywords used, in various combinations, with artemisinin being present in all combinations, in the search were artemisinin, Artemisia annua, analysis, extraction, quantitative, qualitative and quality control. RESULTS: During the period covered in this review, several methods of analysis of artemisinin have been reported, the most of which were liquid chromatography (LC)-based methods. However, the use of new methods like near-infrared analysis, fluorometirc analysis and molecular imprinting, and a significant increase in the use of computational tools have been observed. Mainly several methods involving supercritical fluid extraction and ultrasound-assisted extraction of artemisinin have dominated the extraction area. CONCLUSIONS: Newer analytical tools, as well as improved protocols for the known analytical tools, for qualitative and quantitative determination of artemisinin (1), have been made available by various researchers during the period covered by this review. Supercritical fluid extraction and ultrasound-assisted extraction are still the methods of choice for extraction of artemisinin.


Assuntos
Antimaláricos , Artemisia annua , Artemisininas , Cromatografia Líquida , Extratos Vegetais
6.
Phytochem Anal ; 2019 Dec 17.
Artigo em Inglês | MEDLINE | ID: mdl-31849137

RESUMO

INTRODUCTION: Organic molecules that bind to cannabinoid receptors are called cannabinoids, and they have similar pharmacological properties like the plant, Cannabis sativa L. Hyphenated liquid chromatography (LC), incorporating high-performance liquid chromatography (HPLC) and ultra-performance liquid chromatography (UPLC, also known as ultrahigh-performance liquid chromatography, UHPLC), usually coupled to an ultraviolet (UV), UV-photodiode array (PDA) or mass spectrometry (MS) detector, has become a popular analytical tool for the analysis of naturally occurring cannabinoids in various matrices. OBJECTIVE: To review literature on the use of various LC-based analytical methods for the analysis of naturally occurring cannabinoids published since 2010. METHODOLOGY: A comprehensive literature search was performed utilising several databases, like Web of Knowledge, PubMed and Google Scholar, and other relevant published materials including published books. The keywords used, in various combinations, with cannabinoids being present in all combinations, in the search were Cannabis, hemp, cannabinoids, Cannabis sativa, marijuana, analysis, HPLC, UHPLC, UPLC, quantitative, qualitative and quality control. RESULTS: Since 2010, several LC methods for the analysis of naturally occurring cannabinoids have been reported. While simple HPLC-UV or HPLC-UV-PDA-based methods were common in cannabinoids analysis, HPLC-MS, HPLC-MS/MS, UPLC (or UHPLC)-UV-PDA, UPLC (or UHPLC)-MS and UPLC (or UHPLC)-MS/MS, were also used frequently. Applications of mathematical and computational models for optimisation of different protocols were observed, and pre-analyses included various environmentally friendly extraction protocols. CONCLUSIONS: LC-based analysis of naturally occurring cannabinoids has dominated the cannabinoids analysis during the last 10 years, and UPLC and UHPLC methods have been shown to be superior to conventional HPLC methods.

7.
Heliyon ; 5(11): e02768, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31768435

RESUMO

Southern coastal people of Bangladesh are highly vulnerable to food insecurity and malnutrition due to coastal flooding, deforestation and increased soil salinity. A number of green leafy vegetables are found in the southern coastal belt being traditionally eaten as daily basis by local people. But they are unaware of nutritional and medicinal use of these vegetables. To contribute to their wider utilization, five common vegetables namely Hibiscus sabdariffa, Trianthema portulacastrum, Diplazium esculentum, Heliotropium indicum L. and Hygrophila auriculata were selected for analysis of nutritional proximate, micronutrients and antioxidant potential. Nutritional properties were analyzed in terms of moisture, pH, protein, lipid, ash, fibre, minerals and carbohydrate. Total flavonoid, tannin and antioxidant capacity were evaluated using established protocols. The results demonstrated that collected plants are rich in carbohydrate, fibre, proteins, moisture and ash content but low in lipid content. The mineral elements were high with remarkable amount of Na (19.9-21.5 mg/gm), K (7.9-13.5 mg/gm) and P (1.0-1.8 mg/gm). All the samples were found to have considerable amount of flavonoid (90.6-144.5 mg QE/gm) and tannin content (26.8-57.2 mg GAE/gm). The IC50 value of DPPH and superoxide radical scavenging was the lowest for H. indicum (37.1 and 83.4 µg/ml, respectively) whereas T. portulacastrum possessed high reducing power (IC50 53.7 µg/ml). Among the five investigated species, T. portulacastrum and H. indicum were found to have good nutritional and antioxidant properties, thus can be promoted as a significant source of nutritional and antioxidant food supplements.

8.
Front Pharmacol ; 10: 977, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31551782

RESUMO

Obesity has been implicated as a risk factor for insulin resistance and cardiovascular diseases (CVDs). Although the association between obesity and CVD is a well-established phenomenon, the precise mechanisms remain incompletely understood. This has led to a relative paucity of therapeutic measures for the prevention and treatment of CVD and associated metabolic disorders. Recent studies have shed light on the pivotal role of prolonged endoplasmic reticulum stress (ERS)-initiated activation of the unfolded protein response (UPR), the ensuing chronic low-grade inflammation, and altered insulin signaling in promoting obesity-compromised cardiovascular system (CVS). In this aspect, potential ways of attenuating ERS-initiated UPR signaling seem a promising avenue for therapeutic interventions. We review intersecting role of obesity-induced ERS, chronic inflammation, insulin resistance, and oxidative stress in the discovery of targeted therapy. Moreover, this review highlights the current progress and strategies on therapeutics being explored in preclinical and clinical research to modulate ERS and UPR signaling.

9.
Phytother Res ; 33(10): 2585-2608, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31373097

RESUMO

Traditionally, sesame oil (SO) has been used as a popular food and medicine. The review aims to summarize the antioxidant and antiinflammatory effects of SO and its identified compounds as well as further fatty acid profiling and molecular docking study to correlate the interaction of its identified constituents with cyclooxygenase-2 (COX-2). For this, a literature study was made using Google Scholar, Pubmed, and SciFinder databases. Literature study demonstrated that SO has potential antioxidant and antiinflammatory effects in various test systems, including humans, animals, and cultured cells through various pathways such as inhibition of COX, nonenzymatic defense mechanism, inhibition of proinflammatory cytokines, NF-kB or mitogen-activated protein kinase signaling, and prostaglandin synthesis pathway. Fatty acid analysis of SO using gas chromatography identified known nine fatty acids. In silico study revealed that sesamin, sesaminol, sesamolin, stigmasterol, Δ5-avenasterol, and Δ7-avenasterol (-9.6 to -10.7 kcal/mol) were the most efficient ligand for interaction and binding with COX-2. The known fatty acid also showed binding efficiency with COX-2 to some extent (-6.0 to -8.4 kcal/mol). In summary, it is evident that SO may be one of promising traditional medicines that we could use in the prevention and management of diseases associated with oxidative stress and inflammation.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Simulação de Acoplamento Molecular , Óleo de Gergelim/farmacologia , Animais , Humanos , Estresse Oxidativo/efeitos dos fármacos , Óleo de Gergelim/análise , Óleo de Gergelim/química
10.
Phytochem Anal ; 30(6): 727-734, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31317605

RESUMO

INTRODUCTION: Quaternary alkaloids (QAs) are the major alkaloids in several traditional Chinese medicines, especially in Zanthoxylum simulans. However, few studies on enrichment of QAs from Z. simulans were conducted due to their high polarity and low content. OBJECTIVE: To develop a weak cation exchange (WCX) solid-phase extraction (SPE) coupled with liquid chromatography mass spectrometry (LC-MS) method to enrich and identify QAs from Z. simulans. Meanwhile, the qualitative and quantitative analyses of QAs were carried out based on the optimum conditions of the method. METHODS: Fresh stem bark of Z. simulans was extracted with 70% aqueous methanol and enriched by WCX-SPE. A high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS) with an electrospray ionisation (ESI) source was used for the qualitative and quantitative analyses of QAs. RESULTS: Significant improvements were observed in resolution and abundance of the peaks with WCX-SPE. The linearity, limit of detection (LOD) and limit of quantification (LOQ) were determined for this analytical method. The linear relationship (A = 338.85C - 187.72, R2  = 0.99) was explored in the range of 0.5 to 312.5 µg/mL for chelerythrine. The LOD and LOQ for chelerythrine standard solutions were 0.0539 µg/mL and 0.1798 µg/mL, respectively. In addition, 22 peaks were detected successfully with WCX-SPE and nine of them are undetectable without the processing of WCX-SPE. CONCLUSION: A highly selective and efficient method for simultaneous enrichment and identification of QAs from crude extract of Z. simulans was developed for the first time by combining WCX-SPE with LC-MS.


Assuntos
Alcaloides/análise , Resinas de Troca de Cátion/química , Cromatografia por Troca Iônica/métodos , Extração em Fase Sólida/métodos , Zanthoxylum/química , Cromatografia Líquida de Alta Pressão/métodos , Limite de Detecção , Reprodutibilidade dos Testes
11.
Phytother Res ; 33(8): 2075-2082, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31157484

RESUMO

Three biflavonoids [cupressuflavone (1), amentoflavone (2), and sumaflavone (3)], four diterpenoids [13-epi-cupressic acid (4), imbricatholic acid (5), 3-hydroxy-sandaracopimaric acid (6), and dehydroabietic acid (7)], and one lignan [ß-peltatin methyl ether (8)] were isolated from the cytotoxic fractions of the extracts of the leaves of the Libyan Juniperus phoenicea L. The structures of these compounds were elucidated by spectroscopic means. Cytotoxicity of compounds 1-6 were assessed against the human lung cancer cell line A549 using the MTT assay. Compounds 1 and 3 showed cytotoxicity against the A549 cells (IC50  = 65 and 77 µM, respectively), whereas compound 2 did not show any activity. Diterpenes 4-6 exhibited weak cytotoxicity against the A549 cells with the IC50 values of 159, 263, and 223 µM, respectively. The cytotoxicity of each compound was compared with the anticancer drug, etoposide (IC50  = 61 µM). Cupressuflavone (1) was evaluated also for cytotoxicity against both the human PC3 cancer cell line and the normal prostate cell line (PNT2), and this compound revealed a high degree of cytotoxic selectivity towards the prostate cancer cells (PC3), with IC50 value of 19.9 µM, without any evidence of cytotoxicity towards the normal prostate cell line (PNT2).


Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/uso terapêutico , Biflavonoides/química , Diterpenos/química , Juniperus/química , Neoplasias/tratamento farmacológico , Folhas de Planta/química , Humanos
12.
Front Pharmacol ; 10: 509, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31178720

RESUMO

The liver is not only involved in metabolism and detoxification, but also participate in innate immune function and thus exposed to frequent target Thus, they are the frequent target of physical injury. Interestingly, liver has the unique ability to regenerate and completely recoup from most acute, non-iterative situation. However, multiple conditions, including viral hepatitis, non-alcoholic fatty liver disease, long term alcohol abuse and chronic use of medications can cause persistent injury in which regenerative capacity eventually becomes dysfunctional resulting in hepatic scaring and cirrhosis. Despite the recent therapeutic advances and significant development of modern medicine, hepatic diseases remain a health problem worldwide. Thus, the search for the new therapeutic agents to treat liver disease is still in demand. Many synthetic drugs have been demonstrated to be strong radical scavengers, but they are also carcinogenic and cause liver damage. Present day various hepatic problems are encountered with number of synthetic and plant based drugs. Nexavar (sorafenib) is a chemotherapeutic medication used to treat advanced renal cell carcinoma associated with several side effects. There are a few effective varieties of herbal preparation like Liv-52, silymarin and Stronger neomin phages (SNMC) against hepatic complications. Plants are the huge repository of bioactive secondary metabolites viz; phenol, flavonoid, alkaloid etc. In this review we will try to present exclusive study on phenolics with its mode of action mitigating liver associated complications. And also its future prospects as new drug lead.

13.
Daru ; 27(1): 433-449, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31115871

RESUMO

The application of natural products to treat various diseases, such as cancer, has been an important area of research for many years. Several phytochemicals have demonstrated anticarcinogenic activity to prevent or reduce the progression of cancer by modulating various cellular mechanisms. However, poor bioavailability has hindered clinical success and the incorporation of these drugs into efficient drug delivery systems would be beneficial. For lung cancer, local delivery via the pulmonary route would also be more effective. In this article, recent in vitro scientific literature on phenolic compounds with anticancer activity towards lung cancer cell lines is reviewed and nanoparticulate delivery is mentioned as a possible solution to the problem of bioavailability. The first part of the review will explore the different classes of natural phenolic compounds and discuss recent reports on their activity on lung cancer cells. Then, the problem of the poor bioavailability of phenolic compounds will be explored, followed by a summary of recent advances in improving the efficacy of these phenolic compounds using nanoparticulate drug delivery systems. Graphical abstract The rationale for direct delivery of phenolic compounds loaded in microparticles to the lungs.


Assuntos
Neoplasias Pulmonares/tratamento farmacológico , Fenóis/farmacocinética , Compostos Fitoquímicos/farmacocinética , Disponibilidade Biológica , Linhagem Celular Tumoral , Sistemas de Liberação de Medicamentos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Fenóis/química , Compostos Fitoquímicos/química
14.
Nat Prod Res ; : 1-8, 2019 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-30931627

RESUMO

Phytochemical study was conducted on the leaves of Globimetula braunii which is a hemi parasitic plant belonging to the family Loranthaceae. Extraction was carried out using cold extraction method with increasing polarity of solvents i.e n-hexane, CH2Cl2 and MeOH. The components were separated by chromatographic technique and the structures of the compounds were elucidated by extensive spectroscopic analyses including MS, FTIR, 1D and 2D NMR, HRMS and chemical methods. Six new pentacyclic triterpenoid esters named as globrauneine A (1), globrauneine B (2), globrauneine C (3), globrauneine D (4), globrauneine E (5), and globrauneine F (6), together with six known compounds (7 - 12) were successfully isolated from the leaves of G. braunii growing on Piliostigma thonningii. These results depict a substantial support to the chemotaxonomy of the genus Globimetula.

15.
Fitoterapia ; 134: 151-157, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30825571

RESUMO

Bioassay-guided fractionation of the leaves of Macaranga barteri collected from Nigeria led to the isolation of three previously undescribed cytotoxic stilbenes, macabartebenes A-C (1-3), together with six known compounds including prenylated stilbenes: vedelianin (4), schweinfurthin G (5), and mappain (7), prenylated flavonols: 8-prenylkaempferol (6), and broussoflavonol F (8), and the geranylated flavonol, isomacarangin (9). The cytotoxicity of the compounds was evaluated against four human cancer cell lines, with vinblastine as the positive control and DMSO vehicle as the negative control. Vedelianin (IC50 = 0.32-0.54 µM) displayed the greatest antiproliferative activity across the panel of cancer cell lines amongst the compounds, while macabartebene A (IC50 = 0.60-0.79 µM) was the most potent of the previously unreported compounds. The compounds displayed varying selectivity towards the cancer cell lines compared to the normal human prostate cell line. The findings of this study revealed that M. barteri leaves contain several cytotoxic compounds.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Euphorbiaceae/química , Flavonóis/farmacologia , Estilbenos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Bioensaio , Linhagem Celular Tumoral , Fracionamento Químico , Ensaios de Seleção de Medicamentos Antitumorais , Flavonóis/isolamento & purificação , Humanos , Estrutura Molecular , Nigéria , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Estilbenos/isolamento & purificação
16.
Nat Prod Res ; : 1-5, 2019 Mar 24.
Artigo em Inglês | MEDLINE | ID: mdl-30905175

RESUMO

Trillium govanianum Wall. ex D. Don (Melanthiaceae alt. Trilliaceae), is native to the Himalayas. The present study, for the first time, was undertaken to explore the antimicrobial potential, to determine the minimum inhibitory concentration (MIC) values of the methanol extract of the roots of Trillium govanianum and its solid phase extraction (SPE) fractions by using resazurin microtiter assay (REMA) against Gram positive and Gram negative bacterial registered strains and to carry out phytochemical analysis. The remarkable amount of gallic acid equivalent phenolic and quercetin equivalent flavonoid content was manifested by MeOH extract (20.27 ± 3.03 mg GAE/g DW and 9.25 ± 0.50 mg QE/g DW respectively). The GC/MS analysis revealed the presence saturated and unsaturated components. Considerable level of antibacterial potential against Gram-positive bacteria (MIC: 2.5-0.009 mg/mL) than against Gram-negative bacteria (MIC: 2.5-0.165 mg/mL) were observed. The use of microtiter plates has the advantage of lower cost, fast and quantitative results.

17.
Food Chem Toxicol ; 126: 56-66, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30753858

RESUMO

Scandenolone, an isoflavone, has shown anti-cancer potential. In this study, we extracted scandenolone from Cudrania tricuspidata fruit and evaluated its anti-breast cancer effects as well as toxicity in cell and animal models. In cell model, scandenolone suppressed the breast cancer MCF-7 cells viability, ceased mitotic cell cycle, decreased mitochondrial membrane potential, up-regulated cleaved caspase-3 and promoted the phosphorylation of p53. Additionally, this isoflavone promoted cell apoptosis and induced a sustained activation of the phosphorylation of p38 and ERK, but not JNK and Akt. The effects were further verified in a human MCF-7 breast cancer xenograft model, where scandenolone efficiently suppressed the cancer growth and increased apoptotic cells in tumor tissue. However scandenolone has also shown certain toxicity to normal hepatocytes and breast epithelial cells. It could be concluded that scandenolone suppressed the growth of breast cancer cells, but its toxicity towards normal cells might limit its potential clinical use.


Assuntos
Antineoplásicos Fitogênicos/administração & dosagem , Neoplasias da Mama/fisiopatologia , Sobrevivência Celular/efeitos dos fármacos , Isoflavonas/administração & dosagem , Moraceae/química , Extratos Vegetais/administração & dosagem , Animais , Antineoplásicos Fitogênicos/efeitos adversos , Antineoplásicos Fitogênicos/química , Apoptose/efeitos dos fármacos , Proteínas Reguladoras de Apoptose/genética , Proteínas Reguladoras de Apoptose/metabolismo , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/genética , Neoplasias da Mama/metabolismo , Caspase 3/genética , Caspase 3/metabolismo , Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Feminino , Frutas/química , Humanos , Isoflavonas/efeitos adversos , Células MCF-7 , Camundongos Nus , Fosforilação , Extratos Vegetais/efeitos adversos , Extratos Vegetais/química , Transdução de Sinais
18.
Phytother Res ; 33(1): 159-166, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30346066

RESUMO

Commiphora africana (A. Rich.) Endl. (Burseraceae) is a medicinal plant widely used in Nigerian ethnomedicine. The in vitro cytotoxicity of the stem bark extract of C. africana and isolated cytotoxic compounds was investigated. Three resveratrol derivatives: (E)-resveratrol 3-O-rutinoside (1), 5-methoxy-(E)-resveratrol 3-O-rutinoside (2), and pinostilbene (3), together with 3-hydroxy-5-methoxybenzoic acid (4) were isolated from the methanol fraction of C. africana. Their structures were determined by extensive analysis of their HREIMS and NMR spectra. The cytotoxicity of the isolated compounds against four human carcinoma cells was determined using the MTT assay. Compound 1 displayed the highest antiproliferative effect on the cell lines, with IC50 values of 16.80, 21.74, 17.89, and 17.44 µM, against MCF7, A549, PC3, and HepG2 human cancer cell lines, respectively. In addition, compounds 1-3 showed low toxicity against normal human prostate cell line, with selectivity indices greater than five across the carcinoma cells, indicating that the compounds possess potential in the development of low-toxicity chemotherapeutic agents. These results support the traditional use of this plant in the treatment of cancer.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Antineoplásicos Fitogênicos/uso terapêutico , Produtos Biológicos/uso terapêutico , Commiphora/química , Neoplasias/tratamento farmacológico , Plantas Medicinais/química , Resveratrol/uso terapêutico , Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Produtos Biológicos/farmacologia , Linhagem Celular Tumoral , Humanos , Resveratrol/farmacologia
19.
Phytochem Anal ; 30(1): 101-109, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30288828

RESUMO

INTRODUCTION: Cassia singueana Del. (Fabaceae) is a rare medicinal plant used in the traditional medicine preparations to treat various ailments. The root of C. singueana is a rich source of anthraquinones that possess anticancer, antibacterial and antifungal properties. OBJECTIVE: The objective of this study was to develop an ultrasound-assisted extraction (UAE) method for achieving a high extraction yield of anthraquinones using the response surface methodology (RSM), Box-Behnken design (BBD), and a recycling preparative high-performance liquid chromatography (HPLC) protocol for isolation of anthraquinones from C. singueana. METHODOLOGY: Optimisation of UAE was performed using the Box-Behnken experimental design. Recycling preparative HPLC was employed to isolate anthraquinones from the root extract of C. singueana. RESULTS: The BBD was well-described by a quadratic polynomial model (R2  = 0.9751). The predicted optimal UAE conditions for a high extraction yield were obtained at: extraction time 25.00 min, temperature 50°C and solvent-sample ratio of 10 mL/g. Under the predicted conditions, the experimental value (1.65 ± 0.07%) closely agreed to the predicted yield (1.64%). The obtained crude extract of C. singueana root was subsequently purified to afford eight anthraquinones. CONCLUSION: The extraction protocol described here is suitable for large-scale extraction of anthraquinones from plant extracts.


Assuntos
Antraquinonas/isolamento & purificação , Cassia/química , Cromatografia Líquida de Alta Pressão/métodos , Raízes de Plantas/química , Projetos de Pesquisa , Ultrassom/métodos , Fracionamento Químico/métodos , Modelos Estatísticos , Extratos Vegetais/química , Espectroscopia de Prótons por Ressonância Magnética , Reprodutibilidade dos Testes
20.
J Pharm Biomed Anal ; 164: 653-658, 2019 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-30472583

RESUMO

Green tea is a popular beverage consumed worldwide. Its quality should be controlled adequately as the quality is influenced by several factors in addition to adulterations. This study aimed to develop a simple method for assessing the quality of green tea samples obtained from the South and the East Asian regions. The UV-vis, FTIR and HPLC data from 38 samples were subjected to multivariate analyses using the unsupervised recognition techniques comprising Hierarchical Cluster Analysis (HCA) and Principal Component Analysis (PCA). The model for their authentication was constructed and validated by applying the supervised recognition techniques as Soft Independent Modeling of Class Analogy (SIMCA) and Partial Least Square Discriminant Analysis (PLS-DA). The percentages of caffeine in the identified samples were determined using a validated HPLC assay in addition to in vitro determination of their antioxidant activity using DPPH radical-scavenging capacity assay. HCA and PCA based on UV data successfully distributed the tested samples into informative clusters. However, that obtained from visible data could only differentiate samples with respect to their powdered condition. On the contrary, PCA from FTIR and HPLC data could hardly discriminate any of the samples. The models constructed using SIMCA and PLS-DA showed a good class separation between the South and the East Asian samples. The percentages of caffeine in the identified samples and the IC50 in DPPH assay are greatly diverse among all the tested samples. Thus, UV spectroscopy and chemometrics have provided a simple and quick tool for the quality control of commercial green tea samples.


Assuntos
Antioxidantes/análise , Cafeína/análise , Análise de Componente Principal/métodos , Controle de Qualidade , Chá/química , Compostos de Bifenilo/química , Cromatografia Líquida de Alta Pressão/métodos , Análise por Conglomerados , Análise Discriminante , Depuradores de Radicais Livres/química , Análise Multivariada , Picratos/química , Espectrofotometria Ultravioleta/métodos , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Chá/normas
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