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1.
Med Oncol ; 41(4): 81, 2024 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-38400892

RESUMO

Plectranthus amboinicus leaves were subjected to hydrodistillation to obtain essential oil (EO). Phytochemical analysis using gas chromatography-mass spectrometry revealed a diverse range of compounds in the EO, with p-cymen-4-ol (18.57%) emerging as the most predominant, followed by isocaryophyllene (12.18%). The in vitro antiproliferative activity of EO against breast cancer was assessed in MCF-7 and MDA-MB-231 cell lines. The MTT assay results revealed that EO showed IC50 values of 42.25 µg/mL and 13.44 µg/mL in MCF-7 cells and 63.67 µg/mL and 26.58 µg/mL in MDA-MB-231 cells after 24 and 48 h, respectively. The in silico physicochemical and pharmacokinetic profiles of the EO constituents were within acceptable limits. Molecular docking was conducted to investigate the interactions between the constituents of the EO and protein Aromatase (PDB ID:3S79). Among the EO constituents, 4-tert-butyl-2-(5-tert-butyl-2-hydroxyphenyl)phenol (4BHP) exhibited the highest dock score of -6.580 kcal/mol when compared to the reference drug, Letrozole (-5.694 kcal/mol), but was slightly lesser than Anastrozole (-7.08 kcal/mol). Molecular dynamics simulation studies (100 ns) of the 4BHP complex were performed to study its stability patterns. The RMSD and RMSF values of the 4BHP protein complex were found to be 2.03 Å and 4.46 Å, respectively. The binding free energy calculations revealed that 4BHP displayed the highest negative binding energy of -43 kcal/mol with aromatase protein, compared to Anastrozole (-40.59 kcal/mol) and Letrozole (-44.54 kcal/mol). However, further research is required to determine the safety, efficacy, and mechanism of action of the volatile oil. Taking into consideration the key findings of the present work, the development of a formulation of essential oil remains a challenging task and novel drug delivery systems may lead to site-specific and targeted delivery for the effective treatment of breast cancer.


Assuntos
Neoplasias da Mama , Óleos Voláteis , Plectranthus , Humanos , Feminino , Óleos Voláteis/farmacologia , Óleos Voláteis/análise , Óleos Voláteis/química , Plectranthus/química , Plectranthus/metabolismo , Aromatase/metabolismo , Neoplasias da Mama/tratamento farmacológico , Anastrozol/metabolismo , Letrozol/metabolismo , Simulação de Acoplamento Molecular
2.
Cells ; 11(20)2022 10 15.
Artigo em Inglês | MEDLINE | ID: mdl-36291112

RESUMO

Plectranthus ornatus Codd, the genus Plectranthus of the Lamiaceae family, has been used as traditional medicine in Africa, India and Australia. Pharmacological studies show the use of this plant to treat digestive problems. In turn, leaves were used for their antibiotic properties in some regions of Brazil to treat skin infections. The present study examines the anti-inflammatory, antioxidant and cytotoxic effects of the halimane and labdane diterpenes (11R*,13E)-11-acetoxyhalima-5,13-dien-15-oic acid (HAL) and 1α,6ß-diacetoxy-8α,13R*-epoxy-14-labden-11-one (PLEC) and the forskolin-like 1:1 mixture of 1,6-di-O-acetylforskolin and 1,6-di-O-acetyl-9-deoxyforskolin (MRC) isolated from P. ornatus on lung (A549) and leukemia (CCRF-CEM) cancer cell lines, and on normal human retinal pigment epithelial (ARPE-19) cell line in vitro. Additionally, molecular docking and computational approaches were used. ADMET properties were analysed through SwissADME and proTox-II-Prediction. The results indicate that all tested compounds significantly reduced the viability of the cancer cells and demonstrated no cytotoxic effects against the non-neoplastic cell line. The apoptosis indicators showed increased ROS levels for both the tested A549 and CCRF-CEM cancer cell lines after treatment. Furthermore, computational studies found HAL to exhibit moderate antioxidant activity. In addition, selected compounds changed mitochondrial membrane potential (MMP), and increased DNA damage and mitochondrial copy number for the CCRF-CEM cancer cell line; they also demonstrated anti-inflammatory effects on the ARPE-19 normal cell line upon lipopolysaccharide (LPS) treatment, which was associated with the modulation of IL-6, IL-8, TNF-α and GM-CSF genes expression. Docking studies gave indication about the lowest binding energy for 1,6-di-O-acetylforskolin docked into IL-6, TNF-α and GM-CSF, and 1,6-di-O-acetyl-9-deoxyforskolin docked into IL-8. The ADMET studies showed drug-likeness properties for the studied compounds. Thus, halimane and labdane diterpenes isolated from P. ornatus appear to offer biological potential; however, further research is necessary to understand their interactions and beneficial properties.


Assuntos
Diterpenos , Plectranthus , Humanos , Antibacterianos/farmacologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/metabolismo , Antioxidantes/metabolismo , Colforsina , Diterpenos/química , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Fator Estimulador de Colônias de Granulócitos e Macrófagos/metabolismo , Interleucina-6/metabolismo , Interleucina-8/metabolismo , Lipopolissacarídeos/metabolismo , Simulação de Acoplamento Molecular , Plectranthus/química , Plectranthus/metabolismo , Protoporfirinogênio Oxidase/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Pigmentos da Retina/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
3.
J Chromatogr A ; 1676: 463198, 2022 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-35704959

RESUMO

A new multianalytical methodology based on gas chromatography (GC) and liquid chromatography (LC) coupled to mass spectrometry (MS) has been proposed to evaluate frauds affecting the composition of Coleus forskohlii root supplements (FKS). After optimization and validation of chromatographic methods, 24 FKS were analyzed. Forskolin, their main bioactive component, was only found in 50% of the FKS evaluated (in the 0.032-17.1% range), with 27% of these supplements showing concentrations of this bioactive lower than those declared in their labels. Application of this methodology also proved to be successful for the detection of frauds regarding the replacement of C. forskohlii by other vegetable sources (green tea, soy leaves and a plant of the Berberidaceae family) in 17% of supplements analyzed. A study on stability of forskolin under accelerated conditions allowed to rule out its degradation as responsible for the lack of this bioactive or other natural constituents in 25% of FKS evaluated. It can be concluded that the multianalytical methodology here developed is an advantageous alternative to address the wide diversity of frauds affecting these supplements.


Assuntos
Coleus , Plectranthus , Coleus/química , Coleus/metabolismo , Colforsina/análise , Colforsina/metabolismo , Cromatografia Gasosa-Espectrometria de Massas , Raízes de Plantas/química , Plectranthus/metabolismo
4.
Bioprocess Biosyst Eng ; 44(8): 1593-1616, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34075470

RESUMO

Titanium dioxide nanoparticles exhibit good anticancer and antibacterial activities. They are known to be environmentally friendly, stable, less toxic, and have excellent biocompatibility nature. Due to these properties, they are well suited for biological applications particularly in biomedical applications such as drug delivery and cancer therapy. In this research article, three medicinal herbs namely, Plectranthus amboinicus (Karpooravalli), Phyllanthus niruri (Keezhanelli), and Euphorbia hirta (Amman Pacharisi), were used to modify the surface of the TiO2 nanoparticles. The synthesized nanoparticles were subjected to various characterization techniques. The samples are then subjected to MTT assay to determine cell viability. KB oral cancer cells are used for the determination of the anticancer nature of the pure and bio modified nanoparticles. It is observed that Plectranthus amboinicus-Phyllanthus niruri modified TiO2 nanoparticles exhibit excellent anticancer activities among other bio modified and pure samples. The samples are then examined for antibacterial activities against three Gram-negative bacterial strains namely, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and two Gram-positive bacterial strains namely, Staphylococcus aureus and Streptococcus mutans, respectively. Among the modified and pure samples, Plectranthus amboinicus showed good antibacterial activity against Gram-positive and Gram-negative bacteria. In the Flow cytometry analysis, the generation of p53 protein expression from Plectranthus amboinicus-Phyllanthus niruri modified TiO2 nano herbal particles shows the anti-cancerous nature of the sample. Then to determine the toxic nature of the Plectranthus amboinicus-Phyllanthus niruri modified TiO2 nano herbal particles against normal cells, the NPs were subjected to MTT assay against normal L929 cells, and it was found to be safer and less toxic towards the normal cells.


Assuntos
Euphorbia/metabolismo , Phyllanthus/metabolismo , Plectranthus/metabolismo , Titânio/química , Ágar/química , Animais , Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Linhagem Celular , Sobrevivência Celular , Células HEK293 , Humanos , Concentração de Íons de Hidrogênio , Nanopartículas Metálicas/química , Camundongos , Testes de Sensibilidade Microbiana , Modelos Químicos , Nanotecnologia/métodos , Extratos Vegetais , Folhas de Planta , Preparações de Plantas/farmacologia , Pós , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Sais de Tetrazólio/farmacologia , Tiazóis/farmacologia , Difração de Raios X
5.
Probiotics Antimicrob Proteins ; 12(2): 481-493, 2020 06.
Artigo em Inglês | MEDLINE | ID: mdl-31407234

RESUMO

Coleus forskohlii is an herb, well-known for its medicinal compound forskolin present in its roots, with wide range of pharmaceutical applications. Here, we report, for the first time, the role of plant-probiotic bacterial endophytes of C. forskohlii, CFLB1 and CFRB1, isolated from leaf and root, which regulate plant growth and in plant forskolin content. Native bacterial endophyte, CFRB1 (Alcaligenes faecalis), significantly modulates primary plant productivity and forskolin content under pot and field conditions. Under field conditions, CFRB1 endophyte application significantly enhanced photosynthetic pigments and reduced the severity of root-knot and root rot diseases. Expression analyses of functional genes involved in the forskolin biosynthesis in C. forskohlii plants treated with CFRB1 endophyte under field conditions revealed differential upregulation of four C. forskohlii diterpene synthases (CfTPSs), CfTPS1, CfTPS2, CfTPS3 and CfTPS4, along with cytochrome P450 (CfCYP76AH15) and acyltransferase (CfACT1-8) genes. CFRB1 treatment reduced the severity of nematode infection and root rot in C. forskohlii plants by 81 and 78%, respectively. Overall, we demonstrate that cross-talk of plant-endophyte interaction in C. forskohlii is beneficial, leading to enhanced forskolin content through modulation of forskolin biosynthetic pathway genes along with increased plant yield and reduced disease incidence. Thus, endophytic isolate, A. faecalis (CFRB1), could be deployed as a novel bio-stimulant for enhancing in planta forskolin content during cultivation of C. forskohlii.


Assuntos
Alcaligenes faecalis/isolamento & purificação , Colforsina/metabolismo , Endófitos/isolamento & purificação , Folhas de Planta/metabolismo , Plectranthus/metabolismo , Simbiose , Animais , Resistência à Doença , Interações entre Hospedeiro e Microrganismos , Nematoides , Doenças das Plantas/parasitologia
6.
Int Microbiol ; 23(2): 345-354, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-31823202

RESUMO

Endophytes have been shown to play a crucial role in determining the fitness of host plant during their association, yet the cross-functional effect of endophytes of one plant on another plant remains largely uncharacterized. In this study, we attempt to analyze the effect of native endophytes of Coleus forskohlii (Phialemoniopsis cornearis (SF1), Macrophomina pseudophaseolina (SF2), and Fusarium redolens (RF1), isolated from stem and root parts) on plant growth and secondary metabolite enhancement in medicinal plant Andrographis paniculata, and aromatic plants Pelargonium graveolens and Artemisia pallens. Here, we report, endophytic treatments with SF2 (21%) and RF1 (9%) in A. paniculata resulted in significant enhancement of andrographolide along with plant primary productivity. Correspondingly, application of fungal endophytes RF1, SF1, and SF2 significantly improved the plant growth (11 to 40%), shoot weight (28 to 34%), oil content (44 to 58%), and oil yield (72 to 122%) in P. graveolens. Interestingly, treatment of A. pallens with three fungal endophytes resulted in significant enhancement of plant productivity and oil content (12 to 80%) and oil yield (32 to 139%). Subsequently, the endophyte treatments RF1 and SF1 enhanced davanone (13 to 22%) and ethyl cinnamate (11 to 22%) content. However, SF2 endophyte-treated plants did not show any improvement in ethyl cinnamate content but enhanced the content of davanone (10%), a signature component of davana essential oil. Overall, results depict cross-functional role of native endophytes of C. forskohlii and repurposing of functional endophytes for sustainable cultivation of economically important medicinal and aromatic crops.


Assuntos
Endófitos/metabolismo , Plectranthus/microbiologia , Ascomicetos/isolamento & purificação , Ascomicetos/metabolismo , Diterpenos/metabolismo , Fusarium/isolamento & purificação , Fusarium/metabolismo , Interações entre Hospedeiro e Microrganismos , Raízes de Plantas/metabolismo , Raízes de Plantas/microbiologia , Caules de Planta/metabolismo , Caules de Planta/microbiologia , Plantas/metabolismo , Plantas/microbiologia , Plantas Medicinais/metabolismo , Plantas Medicinais/microbiologia , Plectranthus/crescimento & desenvolvimento , Plectranthus/metabolismo , Metabolismo Secundário , Sesquiterpenos/metabolismo
7.
Microb Ecol ; 78(4): 914-926, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31001657

RESUMO

Coleus forskohlii is a perennial medicinal shrub cultivated mainly for its forskolin content. The plant has been used since ancient times in ayurvedic traditional medicines for the treatment of hypertension, glaucoma, asthma, congestive heart failures, obesity, and cancer. Use of endophytic microorganisms presents a special interest for the development of value-added bioactive compounds through agriculture. Limited investigations have been undertaken on in planta enhancement of forskolin content using endophytic fungus in sustainable agriculture. Here we report specific roles of three fungal endophytes, Fusarium redolens (RF1), Phialemoniopsis cornearis (SF1), and Macrophomina pseudophaseolina (SF2), functionally acting as plant probiotic fungus, regulating secondary metabolite (forskolin) biosynthesis in C. forskohlii. The root endophyte, RF1, and shoot endophytes, SF1 and SF2, were found to enhance forskolin content by 52 to 88% in pot and 60 to 84% in field experiments as compared to uninoculated control plants. The three endophytes also enhanced total biomass owing to plant growth promoting properties. The expression of diterpene synthases (CfTPSs) like CfTPS1, CfTPS2, CfTPS3, and CfTPS4 were significantly upregulated in endophyte-treated C. forskohlii plants. Elevated expression of key diterpene synthases (CfTPS2) in the forskolin biosynthesis pathway, exclusively present in the root cork of C. forskohlii, was observed following SF2 endophyte treatment. Furthermore, endophyte treatments conferred a variety of antagonistic activity against nematode galls (80%) and plant pathogens like Fusarium oxysporum, Colletotricum gloeosporioides, and Sclerotium rolfsii. RF1 and SF1 fungal endophytes showed positive for IAA production; however, SF1 also indicated phosphate solubilization activity. Overall, the qualitative and quantitative improvement of in planta forskolin enhancement represents an area of high commercial interest, and hence, our work focused on novel insights for the application of three fungal endophytes for in planta enhancement of forskolin content for C. forskohlii cultivation by a sustainable approach.


Assuntos
Ascomicetos/fisiologia , Colforsina/metabolismo , Diterpenos/metabolismo , Fusarium/fisiologia , Plectranthus/metabolismo , Plectranthus/microbiologia , Endófitos , Hypocreales/fisiologia , Raízes de Plantas/metabolismo , Xylariales/fisiologia
8.
Future Med Chem ; 10(14): 1677-1691, 2018 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-29957070

RESUMO

AIM: Confirm the use of Plectanthus spp. plants in traditional medicine, particularly as anti-inflammatory and anti-infective agents. MATERIALS & METHODS: Compounds previously isolated from Plectranthus spp. were studied for their anti-inflammatory activity using the SNAP assay and RAW 264.7 cells, by the quantification of nitric oxide. An halimane diterpene and its derivatives were tested in infected macrophages with M. tuberculosis H37Rv, using CFU counts assay, at their minimum inhibitory concentration values. Results: The isolated compounds tested at noncytotoxic concentrations, did not reveal nitric oxide scavenging in the S-nitroso-N-acetylpenicillamine and the cellular assays. On the other hand, promising results were obtained regarding one semisynthetic halimane derivative (11R*,13E)-halima-5,13-diene-11,15-diol), previously prepared (2.1 × 105 CFU/mL), with an effect similar to the antitubercular drugs ethambutol (2.0 × 105 CFU/mL) and isoniazid (1.2 × 105 CFU/mL). CONCLUSION: The present report demonstrates the relevance of Plectranthus spp. in medicinal chemistry drug development for TB and other infective respiratory complaints. Also, this work suggests that further studies involving other inflammatory mediators are needed to validate the anti-inflammatory use of these medicinal plants.


Assuntos
Anti-Inflamatórios/química , Antituberculosos/química , Produtos Biológicos/química , Plectranthus/química , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antituberculosos/isolamento & purificação , Antituberculosos/farmacologia , Produtos Biológicos/isolamento & purificação , Produtos Biológicos/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Leucócitos Mononucleares/citologia , Leucócitos Mononucleares/efeitos dos fármacos , Leucócitos Mononucleares/metabolismo , Lipopolissacarídeos/farmacologia , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/efeitos dos fármacos , Óxido Nítrico/química , Óxido Nítrico/metabolismo , Plantas Medicinais/química , Plantas Medicinais/metabolismo , Plectranthus/metabolismo , Células RAW 264.7
9.
J Photochem Photobiol B ; 183: 251-257, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29734113

RESUMO

In modern era, the great interest and demand among chemists and researchers for metal nanoparticles is increasing in the application of biomedical fields, textiles, cosmetics and various sectors. Consequently, the present study reports an eco-friendly, cost-effective, rapid and easy method to produce environment-friendly metal nanoparticles to prevent exhaustion of metal resources. In this context, gold and silver metal nanoparticles were green synthesized using the Root Extract of Coleous forskohlii (RECo) as capping and reducing agent. The synthesized gold (GNPs) and silver nanoparticles (SNPs) were characterized using UV-Visible spectrophotometer, High-resolution transmission electron microscopy (HR-TEM), Particle size analysis (PSA), Fourier-transform infrared spectroscopy (FT-IR) and X-Ray Diffractometer (XRD). Their clinical importance was analysed using anti-oxidant assay (DPPH - 2,2-diphenyl-1-picrylhydrazyl and Phosphomolybdenum PMA) and cytotoxicity (MTT assay) against HEPG2 (liver cancer cell lines). Further, the antimicrobial activity against two microorganisms were tested using disc diffusion method against Proteus vulgaris pathogen and Micrococcus luteus pathogen. RECo-GNPs and SNPs were found to be stable in aqueous medium for a longer time and exhibited favorable anti-oxidant, anti-bacterial and anti-cancer activity. The phytoconstituents present in the root extract of Coleous forskohlii was elucidated using GC-MS analysis.


Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Ouro/química , Nanopartículas Metálicas/química , Plectranthus/química , Prata/química , Anti-Infecciosos/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Química Verde , Células Hep G2 , Humanos , Nanopartículas Metálicas/toxicidade , Micrococcus luteus/efeitos dos fármacos , Microscopia Eletrônica de Transmissão , Extratos Vegetais/química , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Plectranthus/metabolismo , Proteus vulgaris/efeitos dos fármacos , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
10.
Future Med Chem ; 10(10): 1177-1189, 2018 05 01.
Artigo em Inglês | MEDLINE | ID: mdl-29749759

RESUMO

AIM: 6,7-dehydroroyleanone (DHR) is a cytotoxic abietane present in the essential oil of Plectranthus madagascariensis. METHODS/RESULTS: Different extraction parameters were tested, and its extraction optimization was accomplished with a Clevenger apparatus-based hydrodistillation. After isolation, its effect on microtubules, P-glycoprotein and caspases was assessed on several cell lines and the compound was coupled with hybrid nanoparticles. The results show that DHR does not interfere with microtubule formation, but evades the resistance mechanisms of P-glycoprotein. Strong activation of caspases-3 and -9 indicates that DHR is able to induce apoptosis by triggering the intrinsic cell death pathway. Moreover, the assembly of DHR with hybrid nanoparticles was able to potentiate the effect of DHR in cancer cells. CONCLUSION: DHR seems to be a promising starting material with anticancer properties to further be explored.


Assuntos
Abietanos/química , Antineoplásicos Fitogênicos/química , Subfamília B de Transportador de Cassetes de Ligação de ATP/química , Subfamília B de Transportador de Cassetes de Ligação de ATP/metabolismo , Abietanos/isolamento & purificação , Abietanos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Caspases/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Nanopartículas/química , Óleos Voláteis/química , Extratos Vegetais/química , Plectranthus/química , Plectranthus/metabolismo
11.
Chem Biodivers ; 15(3): e1800005, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29393581

RESUMO

A greenhouse experiment was conducted to study the effects of four irrigation intervals (4, 8, 12, and 16 days) and six harvests (2, 4, 6, 8, 10, and 12 months after transplanting) on biomass, essential oil content, and composition of Plectranthus amboinicus (Lour.) Spreng. Fresh weight and essential oil yield decreased with increasing irrigation interval; whereas, essential oil content was stimulated by water stress and increased as the irrigation interval increased. Fresh weight of Plectranthus amboinicus irrigated every 4 days peaked when harvested at 6 months, but essential oil content peaked when irrigated every 16 days and harvested at 2 months after transplantation. On the other hand, essential oil yield peaked when irrigated every 8 days and harvested at 6 months. Thymol, p-cymene, γ-terpinene, and ß-caryophyllene were the major compounds, and they peaked at different irrigation intervals and harvest times. This study showed biomass, essential oil content, and yield as well as the major and minor constituents of Plectranthus amboinicus are influenced by irrigation interval and the timing of harvest.


Assuntos
Irrigação Agrícola/métodos , Produção Agrícola/métodos , Monoterpenos/análise , Óleos Voláteis/análise , Plectranthus/química , Sesquiterpenos/análise , Timol/análise , Biomassa , Monoterpenos Cicloexânicos , Cimenos , Monoterpenos/metabolismo , Óleos Voláteis/metabolismo , Plectranthus/metabolismo , Sesquiterpenos Policíclicos , Sesquiterpenos/metabolismo , Estresse Fisiológico , Timol/metabolismo , Fatores de Tempo , Água/química
12.
Curr Pharm Des ; 24(36): 4207-4236, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30644340

RESUMO

The study of natural sources such as plants, microorganisms and marine organisms has developed interest among the scientific community in recent years for their extensive and diverse chemical composition and consequent biological potential. The search for antitumor compounds is among the lead causes that justify phytochemical studies. Although some natural products have served as FDA approved chemotherapeutic agents, there is still a demand for the search of compounds with those characteristics. The Plectranthus genus has long been used in traditional medicine, and scientific studies have already proven its undeniable value as a source of bioactive compounds. Diterpenes are the most prominent biologically active group of secondary metabolites present in this genus. In particular, abietane diterpenes have long been studied for their biological activities, namely their anti-tumoral potential. In this review, abietane diterpenes isolated from Plectranthus genus with antiproliferative, antitumoral or cytotoxic potential are reported. In addition, a correlation between this subclass of diterpenes with their mechanisms of cell death has been discussed.


Assuntos
Abietanos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Plectranthus/química , Abietanos/isolamento & purificação , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Humanos , Medicina Tradicional , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Extratos Vegetais/farmacologia , Plectranthus/metabolismo , Metabolismo Secundário
13.
Chemosphere ; 188: 231-240, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28886557

RESUMO

The possible phytoremediation capacity of Plectranthus neochilus (boldo) exposed to the commercial pesticide (Aminol) in soil and water through consecutive extractions (days interval) was evaluated. After the exposure period, tea leaves from the plant were analyzed in terms of the presence of 2,4-D, total antioxidant capacity (DPPH), concentration of total polyphenols and flavonoids for plants exposed to soil and water. In water, 2,4-D remained up to 67% in the 60 days of experiment in the control group, which provided the use of two treatment groups with the plant (one group of plants for 30 days and another group in the remaining 30 days in the same system), thus, a decontamination up to 49% of the 2,4-D was obtained in this system with water. In both experiments (soil and water) the 2,4-D was not detected in tea leaves, the reduction of the antioxidant activity, polyphenols and flavonoids of plants exposed to the herbicide was also observed when compared to the non-exposed plants. In tea - plants in water - it was also possible to quantify the phenolic compounds and it was observed that in the group of plants of the first 30 days there was a decrease in caffeic acid and an increase in coumaric and ferulic acids, compared to the group of plants that were not exposed to 2,4-D. In the remaining 30 days with the new seedlings there was a decrease of the coumaric acid and an increase of the caffeic and ferulic acids.


Assuntos
Ácido 2,4-Diclorofenoxiacético/análise , Antioxidantes/análise , Biodegradação Ambiental , Herbicidas/análise , Folhas de Planta/química , Plectranthus/metabolismo , Ácidos Cafeicos/análise , Ácidos Cumáricos/análise , Tolerância a Medicamentos , Flavonoides/análise , Fenóis/análise , Polifenóis/análise
14.
Elife ; 62017 03 14.
Artigo em Inglês | MEDLINE | ID: mdl-28290983

RESUMO

Forskolin is a unique structurally complex labdane-type diterpenoid used in the treatment of glaucoma and heart failure based on its activity as a cyclic AMP booster. Commercial production of forskolin relies exclusively on extraction from its only known natural source, the plant Coleus forskohlii, in which forskolin accumulates in the root cork. Here, we report the discovery of five cytochrome P450s and two acetyltransferases which catalyze a cascade of reactions converting the forskolin precursor 13R-manoyl oxide into forskolin and a diverse array of additional labdane-type diterpenoids. A minimal set of three P450s in combination with a single acetyl transferase was identified that catalyzes the conversion of 13R-manoyl oxide into forskolin as demonstrated by transient expression in Nicotiana benthamiana. The entire pathway for forskolin production from glucose encompassing expression of nine genes was stably integrated into Saccharomyces cerevisiae and afforded forskolin titers of 40 mg/L.


Assuntos
Vias Biossintéticas/genética , Colforsina/metabolismo , Plectranthus/genética , Plectranthus/metabolismo , Biotransformação , Diterpenos/metabolismo , Engenharia Metabólica , Saccharomyces cerevisiae/genética , Saccharomyces cerevisiae/metabolismo , /metabolismo
15.
Artigo em Inglês | MEDLINE | ID: mdl-27816313

RESUMO

The objective of this study was to identify the active compounds in Plectranthus amboinicus (Lour.) Spreng which play a role to inhibit viability of breast cancer MCF-7 cells using HPLC-based metabolomics approach. Five fractions of the plant extract were observed including ethanol, hexane, chloroform, ethyl acetate and water fraction. There were 45 HPLC chromatograms resulted from 5 fractions with 3 replications and 3 wavelengths detection. The chromatograms were compared to the data of IC50 from MTT assay of each fraction against human breast cancer MCF-7 cells using metabolomics. The OPLS analysis result promptly pointed towards a chloroform fraction at retention time of 40.16-41.28min that has the greatest contribution to the cytotoxic activity. The data of mass spectra indicated that an abietane diterpene namely 7-acetoxy-6-hydroxyroyleanone was the main compound that contributed to the cytotoxic activity. This metabolomics application method can be used as a quick preliminary guideline to uncover the most dominant compound related to the bioactivity.


Assuntos
Antineoplásicos Fitogênicos/toxicidade , Neoplasias da Mama/tratamento farmacológico , Cromatografia Líquida de Alta Pressão/métodos , Metabolômica/métodos , Extratos Vegetais/toxicidade , Plectranthus/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/uso terapêutico , Feminino , Humanos , Células MCF-7 , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Folhas de Planta/metabolismo , Plectranthus/metabolismo , Espectrometria de Massas por Ionização por Electrospray/métodos
16.
Enzyme Microb Technol ; 95: 112-117, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27866605

RESUMO

Graphene based nanocomposites are receiving increasing attention in many fields such as material chemistry, environmental science and pharmaceutical science. In this study, a facial synthesis of a reduced graphene oxide-silver nanocomposite (RGO-Ag) was carried out from Plectranthus amboinicus leaf extract. The synthesized nanocomposite was characterized by using X-ray diffraction, scanning electron microscope, Fourier transform infrared spectroscopy, X-ray photoelectron spectroscopy, transmission electron microscope and UV-vis spectroscopy for structural confirmation. The reduction of graphene oxide and silver ions was achieved simultaneously due to the reducibility of the Plectranthus amboinicus leaf extract. We further investigated the electrochemical properties of the biosynthesized RGO-Ag nanocomposite. A nonenzymatic H2O2 electrochemical sensor was shown to be successfully fabricated by using biosynthesized RGO-Ag nanocomposite. Moreover, the fabricated electrochemical sensor also showed good selectivity.


Assuntos
Grafite/química , Nanocompostos/química , Plectranthus/metabolismo , Prata/química , Biotecnologia , Técnicas Eletroquímicas , Química Verde , Nanopartículas Metálicas/química , Nanopartículas Metálicas/ultraestrutura , Nanocompostos/ultraestrutura , Nanotecnologia , Oxirredução , Extratos Vegetais/metabolismo , Folhas de Planta/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
17.
Mater Sci Eng C Mater Biol Appl ; 62: 293-300, 2016 May.
Artigo em Inglês | MEDLINE | ID: mdl-26952426

RESUMO

Wound healing, a complex biological process, has attained a lot of attention as dermatologists are primarily interested in stimulated wound closure without formation of scar or a faint scar. The recent upsurgence of nanotechnology has provided novel therapeutic materials in the form of silver and gold nanoparticles which accelerate the wound healing process. The effect of formulated nanoparticles using Coleus forskohlii root extract (green synthesized) has been tried out for ameliorating full thickness excision wounds in albino Wistar male rats. The evaluation of in vivo activity of nanoparticles in wound healing was carried out on open wounds made by excision on the dorsal sides of albino Wistar rats under anesthesia, and the healing of the wounds was assessed. Histological aspects of the healing process were studied by a HE (Hematoxylin and Eosin) staining method to assess various degrees of re-epithelialization and the linear alignment of the granulation tissue whereas Van Gieson's histochemical staining was performed to observe collagen fibers. The healing action shown by the formulated nanoparticles was remarkable during the early stages of wound healing, which resulted in the substantial reduction of the whole healing period. Topical application of formulated gold nanoparticles was found to be more effective in suppressing inflammation and stimulating re-epithelialization compared to silver nanoparticles during the healing process. The results throw light on the amelioration of excision wounds using nanoparticles which could be a novel therapeutic way of improving wound healing in clinical practice. The mechanism of advanced healing action of both types of nanoparticles could be due to their antimicrobial, antioxidant and anti-inflammatory properties.


Assuntos
Ouro/química , Nanopartículas Metálicas/química , Prata/química , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Química Verde , Masculino , Nanopartículas Metálicas/toxicidade , Extratos Vegetais/química , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Plectranthus/química , Plectranthus/metabolismo , Ratos , Ratos Wistar , Reepitelização/efeitos dos fármacos , Pele/patologia , Cicatrização/efeitos dos fármacos
18.
Environ Sci Pollut Res Int ; 23(8): 7324-37, 2016 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-26681329

RESUMO

The effects of supplemental ultraviolet-B (s-UV-B; 3.6 kJ m(-2) day(-1) above ambient) radiation were investigated on plant metabolite profile, essential oil content and composition, and free radical scavenging capacities of methanolic extracts of Coleus forskohlii (an indigenous medicinal plant) grown under field conditions. Essential oil was isolated using hydrodistillation technique while alterations in metabolite profile and oil composition were determined via gas chromatography-mass spectroscopy (GC-MS). Leaf and root methanolic extracts were investigated via various in vitro assays for their DPPH radical-, superoxide radical-, hydrogen peroxide-, hydroxyl radical-, and nitric oxide radical scavenging activities, ferrous ion chelating activity, and reducing power. Phytochemical analysis revealed the presence of alkaloids, anthocyanins, coumarins, flavonoids, glycosides, phenols, saponins, steroids, tannins, and terpenoids. Oil content was found to be reduced (by ∼7 %) in supplemental UV-B (s-UV-B) treated plants; the composition of the plant extracts as well as essential oil was also considerably altered. Methanolic extracts from treated plant organs showed more potency as free radical scavengers (their EC50 values being lower than their respective controls). Anomalies were observed in Fe(2+) chelating activity for both leaves and roots. The present study concludes that s-UV-B adversely affects oil content in C. forskohlii and also alters the composition and contents of metabolites in both plant extracts and oil. The results also denote that s-UV-B treated plant organs might be more effective in safeguarding against oxidative stress, though further studies are required to authenticate these findings.


Assuntos
Sequestradores de Radicais Livres/metabolismo , Óleos Voláteis/análise , Extratos Vegetais/análise , Plectranthus/metabolismo , Raios Ultravioleta/efeitos adversos , Sequestradores de Radicais Livres/efeitos da radiação , Cromatografia Gasosa-Espectrometria de Massas , Índia , Óleos Voláteis/efeitos da radiação , Extratos Vegetais/efeitos da radiação , Folhas de Planta/química , Folhas de Planta/metabolismo , Folhas de Planta/efeitos da radiação , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Raízes de Plantas/efeitos da radiação , Plantas Medicinais/metabolismo , Plantas Medicinais/efeitos da radiação , Plectranthus/efeitos da radiação
19.
Molecules ; 20(5): 8440-52, 2015 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-25970043

RESUMO

The chemical composition and antimicrobial activity of essential oils obtained from three Brazilian plant species-leaves and branches of Eremanthus erythropappus (Asteraceae), leaves of Plectranthus barbatus, and leaves of P. amboinicus (Lamiaceae)-were determined. Analysis by GC/MS and determination of Kovats indexes both indicated δ-elemene (leaves-42.61% and branches-23.41%) as well as (-)-α-bisabolol (leaves-24.80% and stem bark-66.16%) as major constituents of E. erythropappus essential oils. The main components of leaves of P. barbatus were identified as (Z)-caryophyllene (17.98%), germacrene D (17.35%), and viridiflorol (14.13%); whereas those of leaves of P. amboinicus were characterized as p-cymene (12.01%), γ-terpinene (14.74%), carvacrol (37.70%), and (Z)-caryophyllene (14.07%). The antimicrobial activity against yeasts and bacteria was assessed in broth microdilution assays to determine the minimum inhibitory concentration (MIC) necessary to inhibit microbial growth. In addition, the crude oil of branches of E. erythropappus was subjected to chromatographic separation procedures to afford purified (-)-α-bisabolol. This compound displayed biological activity against pathogenic yeasts, thus suggesting that the antimicrobial effect observed with crude oils of E. erythropappus leaves and branches may be related to the occurrence of (-)-α-bisabolol as their main component. Our results showed that crude oils of Brazilian plants, specifically E. erythropappus, P. barbatus, and P. amboinicus and its components, could be used as a tool for the developing novel and more efficacious antimicrobial agents.


Assuntos
Anti-Infecciosos/farmacologia , Asteraceae/metabolismo , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Plectranthus/metabolismo , Anti-Infecciosos/análise , Anti-Infecciosos/química , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Brasil , Cromatografia Gasosa-Espectrometria de Massas , Testes de Sensibilidade Microbiana , Óleos Voláteis/análise , Óleos Voláteis/química , Folhas de Planta/metabolismo , Óleos de Plantas/análise , Óleos de Plantas/química , Leveduras/efeitos dos fármacos , Leveduras/crescimento & desenvolvimento
20.
Plant Cell Environ ; 38(5): 968-79, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-25311561

RESUMO

We used variegated Plectranthus coleoides as a model plant with the aim of clarifying whether the effects of realistic ultraviolet-B (UV-B) doses on phenolic metabolism in leaves are mediated by photosynthesis. Plants were exposed to UV-B radiation (0.90 W m(-2) ) combined with two photosynthetically active radiation (PAR) intensities [395 and 1350 µmol m(-2) s(-1) , low light (LL) and high light (HL)] for 9 d in sun simulators. Our study indicates that UV-B component of sunlight stimulates CO2 assimilation and stomatal conductance, depending on background light. UV-B-specific induction of apigenin and cyanidin glycosides was observed in both green and white tissues. However, all the other phenolic subclasses were up to four times more abundant in green leaf tissue. Caffeic and rosmarinic acids, catechin and epicatechin, which are endogenous peroxidase substrates, were depleted at HL in green tissue. This was correlated with increased peroxidase and ascorbate peroxidase activities and increased ascorbate content. The UV-B supplement to HL attenuated antioxidative metabolism and partly recovered the phenolic pool indicating stimulation of the phenylpropanoid pathway. In summary, we propose that ortho-dihydroxy phenolics are involved in antioxidative defence in chlorophyllous tissue upon light excess, while apigenin and cyanidin in white tissue have preferentially UV-screening function.


Assuntos
Antioxidantes/metabolismo , Flavonoides/metabolismo , Fotossíntese/efeitos da radiação , Folhas de Planta/efeitos da radiação , Plectranthus/efeitos da radiação , Dióxido de Carbono/metabolismo , Clorofila/efeitos da radiação , Cloroplastos/efeitos da radiação , Cloroplastos/ultraestrutura , Fenóis/metabolismo , Pigmentos Biológicos/metabolismo , Folhas de Planta/metabolismo , Plectranthus/metabolismo , Carbonilação Proteica/efeitos da radiação , Raios Ultravioleta
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