Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 17 de 17
Filtrar
Mais filtros











Base de dados
Intervalo de ano de publicação
1.
Plant Biotechnol J ; 2024 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-38776398

RESUMO

Sugarcane (Saccharum spp. hybrid) is a prime feedstock for commercial production of biofuel and table sugar. Optimizing canopy architecture for improved light capture has great potential for elevating biomass yield. LIGULELESS1 (LG1) is involved in leaf ligule and auricle development in grasses. Here, we report CRISPR/Cas9-mediated co-mutagenesis of up to 40 copies/alleles of the putative LG1 in highly polyploid sugarcane (2n = 100-120, x = 10-12). Next generation sequencing revealed co-editing frequencies of 7.4%-100% of the LG1 reads in 16 of the 78 transgenic lines. LG1 mutations resulted in a tuneable leaf angle phenotype that became more upright as co-editing frequency increased. Three lines with loss of function frequencies of ~12%, ~53% and ~95% of lg1 were selected following a randomized greenhouse trial and grown in replicated, multi-row field plots. The co-edited LG1 mutations were stably maintained in vegetative progenies and the extent of co-editing remained constant in field tested lines L26 and L35. Next generation sequencing confirmed the absence of potential off targets. The leaf inclination angle corresponded to light transmission into the canopy and tiller number. Line L35 displaying loss of function in ~12% of the lg1 NGS reads exhibited an 18% increase in dry biomass yield supported by a 56% decrease in leaf inclination angle, a 31% increase in tiller number, and a 25% increase in internode number. The scalable co-editing of LG1 in highly polyploid sugarcane allows fine-tuning of leaf inclination angle, enabling the selection of the ideotype for biomass yield.

2.
Chem Biodivers ; 21(2): e202301596, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38126959

RESUMO

Sorbus torminalis (L.) Crantz has a rich history of versatile applications spanning the fields of medicine and nutrition. It is noteworthy that the decoction obtained from S. torminalis leaves is a traditional treatment method against both diabetes and stomach disorders. Phytochemical profiling determined by HPLC/MS-MS. The effects of the extracts on cell viability were investigated using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) method against MDA-MB-231 cell line (human breast adenocarcinoma).The ethanol/water extract contained more concentration of total phenolic (91.41 mg gallic acid (GAE) equivalent /gr) and flavanoid (29.10 mg rutin (RE) equivalent/gr) in the tested extract (p<0.05). Resulting of HPLC analysis, the chemical constituents varied depending on the solvents and chlorogenic acid, hyperoside, isoquercetin, delphindin-3,5-diglucoside, procyanidin B2, epicatechin, neochlorogenic acid, 3,5-dicaffeoylquinic acid were identified in all extracts. Overall, ethanol, n-hexane and ethyl acetate extracts showed the highest inhibition for the tyrosinase enzyme. The effect of leaf extracts of S. torminalis on antimicrobial, biofilm inhibitory, and anticancer activities was examined. Based on outcomes of our study recognize this plant as a critical source of medically active chemicals for feasible phytopharmaceutical and nutraceutical applications, providing the first scientific insight into the detailed biological and chemical profiles of S. torminalis.


Assuntos
Sorbus , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/análise , Flavonoides/farmacologia , Antioxidantes/farmacologia , Etanol , Folhas de Planta/química , Compostos Fitoquímicos/farmacologia
3.
Chem Biodivers ; 19(7): e202101040, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35638152

RESUMO

As the safety and effectiveness of synthetic drugs remain in doubt, researchers are trying to develop natural medicines from medicinal plants. Herein, ethyl acetate, methanol and water extracts from the Heracleum humile plant were obtained by an ultrasonic-assisted extraction process and the aim was to evaluate some biological effects of the extracts due to the limited data on the pharmacological properties of Heracleum humile in the literature. Weak antibacterial activity was observed on tested bacterial species. The minimum inhibitory concentration and the minimum bactericidal concentration values ranged from 250 to 500 µg/mL. In addition, cytotoxic activity was determined using the MTT test. The strongest findings were determined for ethyl acetate extract on the MDA-MB-231 cell lines at the 48th  hour (IC50 :97.94 µg/mL), followed by the MCF-7 cell lines at the 24th  hour (IC50 :103.9 µg/mL). All extracts of Heracleum humile contained mainly flavonoids, phenolic acids and their derivatives, i. e., well-known compounds that possess numerous biological activities such as antioxidant, anti-inflammatory, anticancer, antimicrobial etc. The study results could provide important information that Heracleum humile could be a potential candidate as a natural enzyme inhibitor. It can be concluded that these extracts could be useful in the elementary step of improving novel plant-derived multifunctional pharmaceuticals.


Assuntos
Heracleum , Magnoliopsida , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Flavonoides/farmacologia , Testes de Sensibilidade Microbiana , Extratos Vegetais/farmacologia
4.
Indian J Dermatol ; 67(6): 705-714, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36998849

RESUMO

Vitiligo is a disease characterized by acquired depigmentation, white macules, and patches on the skin due to the dysfunction of epidermal melanocytes. In this study, we attempt to profile the microRNA (miRNA) expression patterns and predict the potential targets, assessing the biological functions of differentially expressed miRNAs in the blood of generalized vitiligo patients. Peripheral blood samples were taken from all participants, and the expression levels of 89 identified miRNAs were analyzed with real-time quantitative polymerase chain reaction (PCR). The results indicated significant upregulation of six miRNAs and downregulation of 19 miRNAs in the plasma of vitiligo patients. The top three upregulated miRNAs were hsa-miR-451a, hsa-miR-25-3p, and hsa-miR-19a-3p, and the top three downregulated miRNAs were hsa-miR-146a-5p, hsa-miR-940, and hsa-miR-142-3p. Moreover, the miRNA expression profiles of patients with Type 3 and Type 4 phototypes were substantially different in such a way that the patients with Type 3 phototype would be more prone to the emergence of melanoma and cancer. While significant variations in the expression patterns of miRNAs in male and female vitiligo patients were demonstrated, miR-let-7i-5p, miR-19a-3p, miR-25-3p, and miR-451a were commonly upregulated, and miR-142-3p and miR-146a-5p were commonly repressed in both sexes. This study may shed light on the roles of differentially expressed miRNAs in vitiligo patients by examining the miRNA expression patterns and the combined effects of miRNA and their predicted targets.

5.
Antioxidants (Basel) ; 10(12)2021 Dec 16.
Artigo em Inglês | MEDLINE | ID: mdl-34943106

RESUMO

Boerhavia diffusa is a great tropical plant and is widely used for various traditional purposes. In the present study, we examined the influence of solvents (dichloromethane, ethyl acetate, methanol and infusion (water)) on chemical composition and biological capabilities of B. diffusa. An UHPLC-HRMS method was used to determine the chemical characterization. The biological ability was examined for antioxidant, enzyme inhibitory and anti-cancer effects. To evaluate antioxidant effects, different chemical methods (ABTS, DPPH, CUPRAC, FRAP, metal chelating and phosphomolybdenum) were applied. With regard to enzyme inhibitory properties, cholinesterases, amylase, glucosidase and tyrosinase were used. The MDA-MB-231 breast cancer cell line was chosen to determine anticancer activity. Based on the UHPLC-HRMS analysis, 37 specialized metabolites were dereplicated and identified in the studied extracts. Results revealed the presence of 15 hydroxybenzoic, hydroxycinnamic, acylquinic acids, and their glycosides, one rotenoid, seven flavonoids, 12 fatty acids and two other glycosides. Among the tested extracts, the methanol extract showed a stronger antioxidant ability compared with other extracts. The methanol extract also showed the best inhibitory effects on tyrosinase and glucosidase. In the anti-cancer evaluation, the methanol extract showed stronger anticancer effects compared with water extract. In summary, our observations can contribute to the establishment of B. diffusa as a potential candidate for functional applications in the preparation.

6.
Int J Mol Sci ; 22(21)2021 Oct 29.
Artigo em Inglês | MEDLINE | ID: mdl-34769166

RESUMO

The short-chain dehydrogenase/reductase (SDR) gene family is widely distributed in all kingdoms of life. The SDR genes, 3ß-hydroxysteroid dehydrogenase (3ß-HSD) and progesterone 5-ß-reductases (P5ßR1, P5ßR2) play a crucial role in cardenolide biosynthesis pathway in the Digitalis species. However, their role in plant stress, especially in salinity stress management, remains unexplored. In the present study, transplastomic tobacco plants were developed by inserting the 3ß-HSD, P5ßR1 and P5ßR2 genes. The integration of transgenes in plastomes, copy number and transgene expression at transcript and protein level in transplastomic plants were confirmed by PCR, end-to-end PCR, qRT-PCR and Western blot analysis, respectively. Subcellular localization analysis showed that 3ß-HSD and P5ßR1 are cytoplasmic, and P5ßR2 is tonoplast-localized. Transplastomic lines showed enhanced growth in terms of biomass and chlorophyll content compared to wild type (WT) under 300 mM salt stress. Under salt stress, transplastomic lines remained greener without negative impact on shoot or root growth compared to the WT. The salt-tolerant transplastomic lines exhibited enhanced levels of a series of metabolites (sucrose, glutamate, glutamine and proline) under control and NaCl stress. Furthermore, a lower Na+/K+ ratio in transplastomic lines was also observed. The salt tolerance, mediated by plastidial expression of the 3ß-HSD, P5ßR1 and P5ßR2 genes, could be due to the involvement in the upregulation of nitrogen assimilation, osmolytes as well as lower Na+/K+ ratio. Taken together, the plastid-based expression of the SDR genes leading to enhanced salt tolerance, which opens a window for developing saline-tolerant plants via plastid genetic engineering.


Assuntos
3-Hidroxiesteroide Desidrogenases/genética , Digitalis/genética , Nicotiana/genética , Oxirredutases/genética , Proteínas de Plantas/genética , Plantas Geneticamente Modificadas/genética , Regulação da Expressão Gênica de Plantas , Plastídeos/genética , Tolerância ao Sal , Plantas Tolerantes a Sal/genética , Transgenes
7.
Comput Biol Chem ; 87: 107273, 2020 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-32516631

RESUMO

The scientific world tends to turn to natural products such as medicinal and aromatic plants because of the inadequacy of commercially available synthetic drugs as antibiotics or anticancer, and their adverse effects on healthy tissues. One of these plants is Daphne gnidioides Jaub. & Spach, which belongs to the Thymelaeaceae family, and there is no data in the literature on its biological activity. This study is aimed to elucidate the chemical profiles and in vitro anticancer, antibacterial and DNA protection and enzyme inhibitory properties of methanol extracts of root, stem, and leaf of D. gnidioides Jaub. & Spach. Polyphenolic components of the extracts were characterized by HPLC-MS/MS. The highest phenolic content was detected in the leaf extract (TIPC = 43.5 ± 0.5 mg/g DE), followed by stem (TIPC = 27.3 ± 0.7 mg/g DE) and root (TIPC = 18.3 ± 0.2 mg/g DE) extracts. Vicenin-2 and 3-O-p-coumaroyl-5-O-caffeoylquinic acid were the main identified compounds in leaf and both root and stem extracts, respectively. The extracts did not show any protective effect on DNA against experimental Fenton's reagent. The minimum inhibitory concentration and the minimum bactericidal concentration values for the root and leaf extracts against tested bacterial strains ranged from 31.25 to 500 µg/mL. After 48 h interaction of the cancer cell lines with the extracts, only the stem extract had significant cytotoxicity on HeLa cells (IC50 = 86.16 µg/mL). No remarkable activity of the extracts, which was tested against MDA-MB-231, was detected (IC50 > 1000 µg/mL). These data showed that D. gnidioides Jaub. & Spach stem extract inhibited the survival of HeLa cells in a time-dependent manner. After the treatment of IC50 concentration of stem extract with HeLa cells, an increase in LC3-II autophagic gene expression was detected. Also, the extracts exhibited significant tyrosinase inhibitory effects which were confirmed by molecular docking. To sum up, the tested extracts could be used as a starting point for the development of new multifunctional drugs.

8.
J Pharm Biomed Anal ; 179: 113012, 2020 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-31791838

RESUMO

This paper reports the anticarcinogenic and antimicrobial properties of silver nanoparticles (Ag NPs) obtained by green synthesis using the extract of Rheum ribes (R. ribes), a medicinal plant. For the synthesis of Ag NPs, the ethanolic extracts of R. ribes were used as a reducing as well as the stabilizing agent. For the characterization of Ag NPs, advanced analytical methods such as transmission electron microscopy (TEM), X-Ray photoelectron spectroscopy (XPS), X-ray diffraction (XRD), and UV-vis spectrophotometry were performed. The synthesized Ag NPs obtained from R. ribes were evaluated as a cytotoxic agent against MDA-MB-231 breast carcinoma cell line. The IC50 values of the nanoparticles were ranged from 165 to 99 µg/mL against MDA-MB 231 cell line for 24 h and 48 h, respectively. The results show that the use of Ag NPs at low concentrations show the toxic effect in the cancer cells. In addition, the results of experiments on gram-positive (Staphylococcus aureus (S. aureus), Methicillin-resistant Staphylococcus aureus (MRSA) and Bacillus subtilis (B. subtilis)) and gram-negative (Escherichia coli (E. coli)) bacteria showed that the Ag NPs had high antimicrobial activity. The results suggest that Ag NPs can be developed as potential anticancer and antibacterial agents.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Extratos Vegetais/administração & dosagem , Rheum/química , Antibacterianos/administração & dosagem , Antibacterianos/isolamento & purificação , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/isolamento & purificação , Bactérias/efeitos dos fármacos , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Feminino , Humanos , Concentração Inibidora 50 , Nanopartículas Metálicas , Extratos Vegetais/farmacologia , Prata/química
9.
J Pharm Biomed Anal ; 179: 112961, 2020 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-31732404

RESUMO

Herein, the biogenic platinum nanoparticles (Pt NPs) were synthesized by using black cumin seed (Nigella sativa L.) extract as a reducing agent. The biogenic platinum nanoparticles synthesized by black cumin seed extract was characterized in detail by Transmission Electron Microscopy (TEM), UV-vis spectrophotometer, X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS). According to TEM analysis, Pt nanoparticles have spherical shapes and sizes between 1-6 nm. Moreover, the biogenic Pt NPs was assessed for its cytotoxicity effect on MDA-MB-231 breast and HeLa cervical cancer lines and their antibacterial effect against selected strains of gram-positive and negative bacteria. The cytotoxicity and bacterial tests showed the effectiveness of biogenic Pt nanoparticles. Dose-dependent toxicity effects were shown in the MDA-MB-231 breast and HeLa cervical cancer lines (IC50: 36.86 µg/mL and 19.83 µg/mL, respectively). In addition, Pt NPs showed high zone diameters against gram-positive and gram-negative bacteria at concentrations of 100 and 500 µg/ml. These results contribute to the development of the pharmaceutical industry as a potential antibacterial and anticancer agent.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Nigella sativa/química , Extratos Vegetais/farmacologia , Antibacterianos/administração & dosagem , Antibacterianos/isolamento & purificação , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/isolamento & purificação , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Feminino , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Células HeLa , Humanos , Concentração Inibidora 50 , Nanopartículas Metálicas , Extratos Vegetais/administração & dosagem , Platina/química , Sementes , Neoplasias do Colo do Útero/tratamento farmacológico
10.
Comput Biol Chem ; 83: 107114, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31493741

RESUMO

Pittosporum senacia (PS) Putt. (Pittosporaceae), indigenous to the Mascarene Islands, is a common ingredient in traditional medicines. However, there is currently a dearth of studies to validate some of these traditional claims. Given the broad traditional uses of PS against several diseases, we aimed to provide a comprehensive insight into the biological and chemical profile of P. senacia. The antioxidant, enzyme inhibitory activity, anticancer, and phytochemical composition of the methanolic extract of P. senacia leaf extracts were studied. The possible interaction and binding mode of the most abundant phytochemicals were studied via in silico docking experiments on tyrosinase and α-glucosidase. The mechanism behind the cytotoxic property of P. senacia extract for MDA-MB-231 was also examined using different methods including 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cell viability test checking apoptosis-associated genes, and wound healing assays. Twenty-six compounds were identified, of which caffeoylquinic acid derivatives, ferulic acid derivative, cinnamoylquinic acid derivative and two other polyphenols (oleuropeine and isoramnetin glucoside) being abundant, have been tested using in silico studies, against α-glucosidase and tyrosinase. The extract (IC50 = 118.8 µg/ml) exhibited time and dose dependent anti-proliferative effect on human breast cancer cell line, MDA-MB-231. According to the expression profile of apoptosis inhibitors and apoptosis promoters genes, expression of Bax and Bak genes were significantly increased compared to Bcl-2 and Birc5 genes. Based on wound healing analysis, cell migration was inhibited after the application of the plant extract. The present findings suggested that PS might be a good candidate as sources of bioactive compounds for designing functional applications.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , DNA/efeitos dos fármacos , Inibidores Enzimáticos/farmacologia , Simulação de Acoplamento Molecular , Extratos Vegetais/farmacologia , Rosales/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Plasmídeos/efeitos dos fármacos , Espectrometria de Massas por Ionização por Electrospray , Células Tumorais Cultivadas , alfa-Glucosidases/metabolismo
11.
J Pharm Biomed Anal ; 174: 286-299, 2019 Sep 10.
Artigo em Inglês | MEDLINE | ID: mdl-31185340

RESUMO

This study aimed to reveal chemical profiles and biological activities of ethyl acetate (EA), methanol (MeOH), and water extracts of Lotus corniculatus. Ethnobotanical reports have indicated the importance of phytochemical properties of the genus Lotus. In this study, the effects of medicinal plant extracts on antioxidant (DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelating assays), enzyme inhibitory (on cholinesterase, tyrosinase, a-amylase and a-glucosidase), DNA protection and anticancer properties (including anti-proliferative, cell death and telomerase activity marker gene analysis, apoptotic DNA fragmentation analysis, cell migration test) were evaluated. According to chemical analysis, quercetin derivatives geraldol, isorhamnetin and kaempferol-O-coumaroylhexoside-O-deoxyhexoside isomers were dominant in the extracts. MeOH extracts showed the highest total flavonoids capacity with 21.13 mg RE/g. EA extract showed the strongest anti-amylase activity among the tested extracts. Water extract had the most protective activity against plasmid DNA. To indicate cell survival, MTT test was performed against human MCF-7 and MDA-MB-231 breast cancer cells. Half-maximal inhibitory concentration for cells were calculated and used for detection of mechanisms behind the cancer cell death. EA extract showed up-regulation of Bax proapoptotic gene and apoptotic DNA fragmentation activity on highly invasive MDA-MB-231 cells. Beclin-1 and LC3-II autophagy genes were higly expressed after treatment of MCF-7 cells with EA extracts. EA and MeOH extracts inhibited cell migration ability of both cancer cells. Linoleamide, was dominant component in EA extract and caused apoptosis on MDA-MB-231 breast cancer cells via increasing intranuclear Ca²+. The detailed mechanism behind the anticancer properties should be further investigated.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose , Autofagia , Neoplasias da Mama/tratamento farmacológico , Lotus/química , Extratos Vegetais/farmacologia , Acetatos/química , Amilases/antagonistas & inibidores , Animais , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Fragmentação do DNA , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Flavonoides/análise , Flavonoides/farmacologia , Humanos , Células MCF-7 , Melanoma Experimental , Metanol/química , Camundongos , Estresse Oxidativo , Água/química
12.
J Pharm Biomed Anal ; 171: 118-125, 2019 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-30986761

RESUMO

This study was geared towards assessing the possible antioxidant, enzyme inhibitory, and cytotoxic activities of ethyl acetate, methanol, and water extracts of Sideritis ozturkii Aytaç & Aksoy. The phytochemical profiles of the studied extracts were characterised by HPLC-MS/MS. The methanol extract, rich in phenolics (78.04 mg gallic acid equivalent/g), exhibited the strongest antioxidant activities. However, the ethyl acetate extract was the most active extract in the enzyme inhibitory assays. The water extract of S. ozturkii (1 mg/ml, 48 h incubation) slightly inhibited (22%) growth of human breast cancer cell line (MDA-MB-231 cells). On the other hand, the ethyl acetate and methanol extracts showed strong inhibition (98% and 97%, respectively) of MDA-MB-231 cells and caused apoptotic cell death. Scientific data generated from this study further appraises the multiple biological activities of plants belonging to the Sideritis genus. In addition, preliminary evidence gathered from the current investigation advocates for further studies geared towards the preparation of therapeutic formulations from S. ozturkii.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Inibidores Enzimáticos/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Sideritis/química , Acetatos/química , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Inibidores Enzimáticos/farmacologia , Humanos , Metanol/química , Extratos Vegetais/farmacologia , Sideritis/crescimento & desenvolvimento , Solventes/química , Turquia , Água/química
13.
Food Res Int ; 115: 425-438, 2019 01.
Artigo em Inglês | MEDLINE | ID: mdl-30599961

RESUMO

Phyllanthus phillyreifolius var. commersonii Müll. Arg is an endemic plant of Mauritius. To date, no study has been performed concerning its polyphenolic profile and pharmacological properties. In this study, a decoction (water), ethyl acetate and methanol extracts of the aerial parts of P. phillyreifolius, obtained from different extraction procedures (maceration and Soxhlet), were studied for antibacterial, antioxidant, anticancer, and enzyme inhibitory properties along with their polyphenolic profile. The ethyl acetate macerated extract showed high antibacterial activity against B. cereus (MIC = 0.293 mg/mL) and E. coli (MIC = 0.417 mg/mL) while S. epidermidis was most susceptible to the ethyl acetate-Soxhlet extract (MIC = 0.521 mg/mL). The methanol-Soxhlet extract displayed the most potent cupric and ferric reducing power, and metal chelating effect, while the macerated methanolic extract was the most effective DPPH and ABTS scavenger, and BChE inhibitor. Only the ethyl acetate-Soxhlet extract exhibited α-glucosidase inhibition. All extracts exhibited a strong anti-tyrosinase activity, which was further investigated by molecular docking and molecular dynamic. After 48 h exposure to the extracts for HeLa cell lines, the ethyl acetate-Soxhlet extract showed the highest inhibition (IC50 = 533.1 µg/mL) while the decoction extract was more cytotoxic to MDA-MB-231 cells (IC50 = 337.4 µg/mL). Treatment of cancer cell lines with all P. phillyreifolius extracts resulted in a time-dependent reduction of cell viability for HeLa and dose-and time-dependent reduction for MDA-MB-231. Gene expression ratio of Bcl-2 to Bax was higher for all Soxhlet-extracts. Total phenolics (TPC) and flavonoids (TFC) content were highest in the decoction and methanol-Soxhlet extract, respectively (122.43 mg GAE/g extract and 31.28 mg RE/g extract, respectively). The extracts were abundant in ellagitannins, although phenolic acids and flavonoids were also detected. Granatin B was detected for the first time in Phyllanthus species. Overall, the aerial parts of P. phillyreifolius exemplify a potent reservoir of bioactive phytochemicals for therapeutic applications.


Assuntos
Fenóis/análise , Fenóis/farmacologia , Phyllanthus/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Antibacterianos/análise , Antineoplásicos/análise , Antioxidantes/análise , Bactérias/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Inibidores Enzimáticos/análise , Flavonoides/análise , Células HeLa , Humanos , Taninos Hidrolisáveis/análise , Maurício , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Monofenol Mono-Oxigenase/efeitos dos fármacos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia
14.
Int J Biol Macromol ; 122: 1271-1278, 2019 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-30227206

RESUMO

Isatin, thiosemicarbazone and their derivatives have been widely used in biological applications such as antimicrobial, antiviral and anticancer therapies. Herein, eight isatin and thiosemicarbazone derivative compounds were re-synthesized and evaluated for DNA binding analysis including DNA protection studies using plasmid DNA (pUC19) and DNA interaction experiments using calf thymus DNA (CT-DNA). All compounds were also utilized in vitro assay to assess the antimicrobial activity of compounds against different pathogenic bacterial strains. All isatin and thiosemicarbazone derivative compounds exhibited DNA protection activity which ranged from 23.5 to 59.5%. Among them, I3-(N-2-MP)-TSC had the greatest DNA protective activity. For DNA binding analysis, all compounds had the same constant concentration (40 µM), which interacts with CT-DNA. It was also observed that DNA interactions gave a high intrinsic binding constant (Kb = 1.72 × 104 M-1-9.73 × 105 M-1). Besides, several derivatives of isatin thiosemicarbazone exhibited significant and selective antibacterial activity with low concentration. These compounds primarily affected Gram-positive bacteria, but were not effective against P. vulgaris and E. coli. The Gram-positive methicillin-resistant S. aureus ATCC 43300 (MRSA) was the most influenced strain by these compounds. It was found that methyphenyl group at isatin was essential for its antibacterial activity for MRSA.


Assuntos
Antibacterianos/metabolismo , Antibacterianos/farmacologia , DNA/metabolismo , Isatina/metabolismo , Isatina/farmacologia , Animais , Antibacterianos/química , Bactérias/efeitos dos fármacos , Bovinos , Isatina/química , Plasmídeos/genética
15.
Food Chem Toxicol ; 120: 172-182, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30008431

RESUMO

This study aims to establish the biological and chemical profile of Asphodeline liburnica (Scop.) Rchb. root. The antioxidant, antimicrobial, enzyme inhibitory, DNA protection, apoptotic DNA ladder fragmentation analysis, and anti-proliferative of A. liburnica were established using standard assays. In silico study was also performed to understand interactions between quantified anthraquinones and key enzymes of clinical relevance. Total phenolic and flavonoid contents were found to be 9.67 mgGAE/g and 1.48 mgRE/g extract, respectively. Chrysophanol was detected as a major anthraquinone. The extract exhibited radical scavenging ability against DPPH and ABTS with values of 13.23 and 66.99 mgTE/g extract, respectively. Good inhibitory activity against tyrosinase was recorded. In silico experiments showed that the anthraquinones were able to establish coordinative bonds with the copper atoms present in the enzymatic cavity of tyrosinase. MTT cell viability test on MDA-MB-231 cells showed that at 0.1 and 1 µg of extracts induced anti-proliferative effect. Apoptotic DNA fragmentation analysis indicated nuclear condensation resulting in DNA fragmentation, which exhibited apoptotic cell death in the presence of A. liburnica. This study has provided insights on the potential usage of A. liburnica which could open new avenues for research and stimulate future interest for the development of safe novel biopharmaceuticals.


Assuntos
Antraquinonas/toxicidade , Antraquinonas/uso terapêutico , Asphodelaceae/química , Extratos Vegetais/toxicidade , Extratos Vegetais/uso terapêutico , Raízes de Plantas/química , Antraquinonas/química , Anti-Infecciosos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Simulação por Computador , DNA/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/farmacologia , Humanos , Técnicas In Vitro , Testes de Sensibilidade Microbiana , Extratos Vegetais/química
16.
Food Chem Toxicol ; 111: 525-536, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29217268

RESUMO

Bidens tripartita L. is a traditional phyto-remedy used in several countries, yet there is still a paucity of data on its biological potential. We aimed to provide new insights on the pharmacological potential of extracts prepared from B. tripartita via highlighting its antioxidant, key enzymes inhibitory potency, and DNA protecting effects. Phytochemical profile was established using High-Performance Liquid Chromatography with Diode-Array Detection (HPLC-DAD) and bioactive compound(s) docked against target enzymes using in silico methods. Cytotoxicity against three cancer cell lines was assessed using the methylthiazolyldiphenyl-tetrazolium bromide (MTT) cell viability test. The main compounds were luteolin-7-glucoside (cynaroside), chlorogenic acid, and epicatechin in the extracts. The methanol extract exhibited the highest radical scavenging activity. Ethyl acetate extract showed strongest α-amylase inhibitory activity, while the best α-glucosidase inhibitory effect recorded for the methanol extract. Molecular docking showed that cynaroside strongly interact to α-glucosidase cavity by establishing six hydrogen bonds. B. tripartita extracts were found to protect supercoiled form of pUC19 plasmid (>70%) and also showed anti-proliferative properties. Results amassed in the present study add on to a growing body of literature on the multi-pharmacological potency of B. tripartita which can be applied to bio-products development geared towards management of common diseases.


Assuntos
Bidens/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Simulação por Computador , Simulação de Acoplamento Molecular , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo
17.
Physiol Mol Biol Plants ; 23(1): 5-21, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-28250580

RESUMO

Late embryogenesis abundant (LEA) proteins are large and diverse group of polypeptides which were first identified during seed dehydration and then in vegetative plant tissues during different stress responses. Now, gene family members of LEA proteins have been detected in various organisms. However, there is no report for this protein family in watermelon and melon until this study. A total of 73 LEA genes from watermelon (ClLEA) and 61 LEA genes from melon (CmLEA) were identified in this comprehensive study. They were classified into four and three distinct clusters in watermelon and melon, respectively. There was a correlation between gene structure and motif composition among each LEA groups. Segmental duplication played an important role for LEA gene expansion in watermelon. Maximum gene ontology of LEA genes was observed with poplar LEA genes. For evaluation of tissue specific expression patterns of ClLEA and CmLEA genes, publicly available RNA-seq data were analyzed. The expression analysis of selected LEA genes in root and leaf tissues of drought-stressed watermelon and melon were examined using qRT-PCR. Among them, ClLEA-12-17-46 genes were quickly induced after drought application. Therefore, they might be considered as early response genes for water limitation conditions in watermelon. In addition, CmLEA-42-43 genes were found to be up-regulated in both tissues of melon under drought stress. Our results can open up new frontiers about understanding of functions of these important family members under normal developmental stages and stress conditions by bioinformatics and transcriptomic approaches.

SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA