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Hepatocellular carcinoma (HCC) contributes to more than 80% of all primary cancers globally and ranks fourth in cancer-related deaths, due to the lack of an effective, definite therapeutic drug. Coleus vettiveroides (CV) has been used in Indian traditional medicine to treat diabetes, liver ailments, skin diseases, leukoderma, and leprosy. This study investigates the anticancer effect of CV ethanolic root extract in HepG2 cells. HepG2 cells were treated with CV extract, and its cytotoxicity was analyzed by MTT assay. AO/EB staining, propidium iodide staining, DCFH-DA assay, phalloidine staining, flow cytometry, and qPCR studies were performed for ROS expression, apoptosis and cell cycle analysis. The phytochemical analysis confirmed the presence of quercetin and galangin in CV root extract. The results showed that CV inhibited the proliferation of HepG2 cells, with altered cellular and nuclear morphology. CV was also found to increase intracellular ROS levels and oxidative stress markers in HepG2 cells. CV significantly altered the actin microfilament distribution in HepG2 cells and caused cell cycle arrest at the sub G0 -G1 phase. CV also induced mitochondria-mediated apoptosis, as evidenced by increased expression of p53, Bax, cytochrome C, Apaf-1, PARP, caspase-3 and caspase-9, and downregulated Bcl-2 expression. Therefore, CV exerts its anticancer effect by inducing mitochondrial dysfunction, oxidative stress, cytoskeletal disorganization, cell cycle arrest, and mitochondria-mediated apoptosis, and it could be a potent therapeutic option for HCC.
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Carcinoma Hepatocelular , Coleus , Neoplasias Hepáticas , Humanos , Carcinoma Hepatocelular/tratamiento farmacológico , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patología , Células Hep G2 , Neoplasias Hepáticas/metabolismo , Coleus/metabolismo , Especies Reactivas de Oxígeno/metabolismo , Apoptosis , EtanolRESUMEN
Background: As broad-spectrum antibiotics can cause antimicrobial resistance in sepsis, there is the need for a complementary therapy to combat sepsis. Oxidative stress causes an increased severity and mortality in sepsis, whereas herbal medicines have been considered as an option due to its antioxidant potential. Coleus amboinicus Lour. has been documented for its therapeutic value due to the presence of flavonoid, an antioxidant compound. Objective: To study the effect of Coleus amboinicus Lour. leaf extract on total antioxidant capacity (TAC) and hepatic catalase (CAT) levels in septic rat model. Methods: Twenty-eight male Rattus norvegicus rats were divided into four groups: control (rats without sepsis induction and treatment), group 1 (septic rats treated with antibiotics), group 2 (septic rats treated with antibiotics and 250 mg/kg body weight of Coleus amboinicus Lour. leaf extract), and group 3 (septic rats treated with antibiotics and 500 mg/kg body weight of Coleus amboinicus Lour. leaf extract). The rats were sacrificed at the end of the eighth day of observation, and blood and liver tissues were gathered for examination. Results: Compared to the septic rat groups treated with only antibiotics, there was an increase in the TAC levels and CAT expression levels in septic rat groups given antibiotics and Coleus amboinicus Lour. leaf extract. However, the increase was not significant. Conclusion: Administering Coleus amboinicus Lour. leaf extract increases TAC levels and CAT expression levels in sepsis, decreasing oxidative stress. This will exert protective effects in the cells and therefore alleviate sepsis.
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Coleus , Sepsis , Ratas , Masculino , Animales , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Sepsis/tratamiento farmacológico , Antibacterianos/farmacología , Antibacterianos/uso terapéutico , Peso CorporalRESUMEN
Liver cancer or hepatocellular carcinoma (HCC) has become a leading cause for cancer burden across the globe, and incidences have tripled since the last two decades. Poor diagnosis of primary liver cancer and limited treatment strategies aggravate the challenges. Researchers globally have shown a steep inclination toward the exploration of plant-based compounds for their nutraceutical and anticancer potential to fit into the role of novel chemotherapeutics. Coleus aromaticus is a well-known culinary herb that earlier has been reported for several medicinal attributes. The current investigation deals with exploring the anticancer potential of ethanolic leaf extract of C. aromaticus (CoL-EtOH) against hepatocellular carcinoma HepG2 cell line. The observations made it evident that CoL-EtOH extract impeded the viability of HepG2 at 400 µg/ml (p < .01). Additionally, the extract also succeeded in escalating ROS production (p < .01) which aided dissipation of mitochondrial membrane potential and disruption of nuclear morphology. CoL-EtOH further activated caspase-8, -9, and -3 which was reaffirmed by increase in apoptosis at 400 µg/ml (p < .01). Moreover, post treatment with CaLEt-OH extract significantly reduced the expression of JAK-1 & STAT-3 genes (p < .01) along with regulated expression of Mcl1, Bcl-2, cyclinD1, p21, and p27 within HepG2 cells. This evidence portrays the promising anticancer potential of CoL-EtOH projecting it as a novel chemotherapeutic agent against HCC. PRACTICAL APPLICATIONS: The herb Coleus aromaticus belonging to Lamiaceae family and Coleus genus is known by various names in different regions of the world and several language-specific vernacular names. The herb has been used in therapeutic and medicinal applications as well as in culinary preparations. Various attributes of the nutritional strength and functional characteristics of the leaves in terms of carotenoids, minerals, phenols, dietary fiber, and antioxidant activity have been reported by several researchers. Carvacrol and thymol are majorly found in the plant, while chlorogenic acid and rosmarinic acid etc. as the phenolic components. The herb has been used in therapeutic and medicinal implications as well as in culinary preparations.
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Carcinoma Hepatocelular , Coleus , Neoplasias Hepáticas , Antioxidantes , Apoptosis , Carcinoma Hepatocelular/tratamiento farmacológico , Carotenoides , Caspasa 8 , Proliferación Celular , Ácido Clorogénico , Fibras de la Dieta , Etanol , Células Hep G2 , Humanos , Quinasas Janus/metabolismo , Neoplasias Hepáticas/tratamiento farmacológico , Proteína 1 de la Secuencia de Leucemia de Células Mieloides , Fenoles , Extractos Vegetales/farmacología , Especies Reactivas de Oxígeno , Factores de Transcripción STAT/metabolismo , TimolRESUMEN
Coleus forskohlii Briq. is an important medicinal herb, endowed with a wide range of medicinal properties against the variety of ailments. Seven germplasm of C. forskohlii collected from different phyto-geographical locations and identification of elite chemotype was performed with the help of high performance thin layer chromatography. Data of soil analysis correlated with the bioactive compounds and inhibitory potential of the species. Quantification of forskolin and its isomer (iso-forskolin) content were done in all the collected samples of C. forskohlii, which revealed a wide range of variations, varying from 1.15-0.004% and 0.0091 to 0.1077% per dry weights basic, respectively. Variation in the bioactive content may be due to the soil nature and environmental factors. Soil analysis of collected samples demonstrated that there is significant variation in available NPK and micronutrient content and may be reasoned for existing chemotypic variability. In vitro biological activity (antioxidant and antidiabetic) analyses were performed, which reveals that germplasms have a high amount of forskolin and iso-forskolin, both show more activity. The aim of this study was to elucidate the effect of elicitors and precursors on the production of bioactive compounds and identification of best elite germplasm among the populations, to provide basic lead to the industry for commercial exploitability including its location-specific commercial cultivation.
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Coleus , Plectranthus , Coleus/química , Colforsina/análisis , Colforsina/química , Cromatografía en Capa Delgada , SueloRESUMEN
BACKGROUND: Chronic obstructive pulmonary disease (COPD) is characterized by limited airflow due to pulmonary and alveolar abnormalities from exposure to cigarette smoke (CS). Current therapeutic drugs are limited and the development of novel treatments to prevent disease progression is challenging. Isoforskolin (ISOF) from the plant Coleus forskohlii is an effective activator of adenylyl cyclase (AC) isoforms. Previously we found ISOF could attenuate acute lung injury in animal models, while the effect of ISOF on COPD has not been elucidated. PURPOSE: In this study, we aimed to evaluate the efficacy of ISOF on COPD and reveal its potential mechanisms. METHODS: A rat model of COPD was established by long-term exposure to CS, then the rats were orally administered with ISOF (0.5, 1 and 2 mg/kg). The pulmonary function, lung morphology, inflammatory cells and cytokines in serum or bronchoalveolar lavage fluid (BALF) were evaluated. Transcriptomics, proteomics and network pharmacology analysis were utilized to identify potential mechanisms of ISOF. Droplet digital PCR was used to detect the mRNA expression of AC1-10 in donor lung tissues. AC activation was determined in recombinant human embryonic kidney 293 (HEK293) cells stably expressing human AC isoforms. In addition, ISOF caused trachea relaxation ex vivo were assessed in isolated trachea rings from guinea pigs. RESULTS: ISOF significantly ameliorated pathological damage of lung tissue and improved pulmonary function in COPD rats. ISOF treatment decreased the number of inflammatory cells in peripheral blood, and also the levels of pro-inflammatory cytokines in serum and BALF. Consistent with omics-based analyses, ISOF markedly downregulated the mTOR level in lung tissue. Flow cytometry analysis revealed that ISOF treatment reduced the ratio of Th17/Treg cells in peripheral blood. Furthermore, the expression levels of AC1 and AC2 are relatively higher than other AC isoforms in normal lung tissues, and ISOF could potently activate AC1 and AC2 in vitro and significantly relax isolated guinea pig trachea. CONCLUSION: Collectively, our studies suggest that ISOF exerts its anti-COPD effect by improving lung function, anti-inflammation and trachea relaxation, which may be related to AC activation, mTOR signaling and Th17/Treg balance.
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Adenilil Ciclasas , Colforsina/farmacología , Enfermedad Pulmonar Obstructiva Crónica , Humo , Animales , Coleus/química , Cobayas , Células HEK293 , Humanos , Fitoquímicos/farmacología , Enfermedad Pulmonar Obstructiva Crónica/inducido químicamente , Enfermedad Pulmonar Obstructiva Crónica/tratamiento farmacológico , Ratas , Humo/efectos adversos , FumarRESUMEN
The frequent applications of synthetic chemical insecticides and drugs create resistance among insects and microbes, creating a new threat to human and environmental welfare. This investigation focused on evaluating the possibilities of fabricating and characterizing the titanium dioxide nanoparticles (TiO2 NPs) from titanium dioxide (TiO2) through the aqueous leaf extract of Coleus aromaticus. Their biological applications were studied against the larvae of Aedes aegypti human pathogenic bacteria, and cancer cell line. The results revealed that the aqueous leaf extract had the metal reducing proficiency to produce nanoparticles from TiO2. The synthesized TiO2 NPs were initially confirmed by visible color changes and Ultraviolet-Visible Spectrophotometer analysis that showed a predominant peak at 332 nm. Furthermore, the nanocrystals, structural alignment, functional groups and elemental compositions were studied by following standard operating protocol in XRD (X-ray Powder Diffraction), FTIR (Fourier Transform Infrared Spectroscopy), TEM (Transmission Electron Microscopy), and EDX (Energy-Dispersive X-ray Spectroscopy) techniques, respectively. The results attained from these techniques confirmed that the plant mediated and fabricated particles were in the nanoscale range (12-33 nm) with a hexagonal shape. The synthesized TiO2 NPs had an outstanding (1000 µg mL-1) larvicidal activity against the four stages of instars larvae of Ae. aegypti at 1000 µg mL-1. It also had an excellent antibacterial potential against E. faecalis (33 mm), followed by S. boydii (30 mm) at 30 mg L-1 concentration. The green fabricated TiO2 NPs had a fabulous (92.37%) cytotoxic activity on the HeLa cell line at 100 µg mL-1 dosage within one day of exposure. The entire results concluded that the C. aromaticus mediated TiO2 NPs have excellent biological applications and thus, could be considered for the welfare of human beings.
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Coleus , Insecticidas , Nanopartículas del Metal , Animales , Antibacterianos/toxicidad , Células HeLa , Humanos , Larva , Nanopartículas del Metal/toxicidad , Extractos Vegetales/farmacología , Hojas de la Planta , Espectroscopía Infrarroja por Transformada de Fourier , Titanio , Difracción de Rayos XRESUMEN
BACKGROUND: In Saudi Arabia, the incidence and mortality rates of breast cancer are high. Although current treatments are effective, breast cancer cells develop resistance to these treatments. Numerous studies have demonstrated that active compounds in plant extracts, such as the phenolic compound Rosmarinic Acid (RA), exert anti-cancer effects. OBJECTIVE: We investigated the anticancer properties of methanolic crude extracts of seedlings and calli of Rosmarinus officinalis and Coleus hybridus, two Lamiaceae species. METHODS: MCF-7 human breast cancer cells were treated with methanolic crude extracts obtained from plant calli and seedlings generated in vitro, and cell proliferation was evaluated. Transcriptional profiling of the seedling and callus tissues was also conducted. RESULTS: The mRNA expression levels of RA genes were higher in C. hybridus seedlings than in R. officinalis seedlings, as well as in C. hybridus calli than in R. officinalis calli, except for TAT and C4H. In addition, seedling and callus extracts of both R. officinalis and C. hybridus showed anti-proliferative effects against MCF-7 cells after 24 or 48 h of treatment. DISCUSSION: At a low concentration of 10 µg/mL, C. hybridus calli and seedling extracts showed the most significant anti-proliferative effects after 24 and 48 h of exposure (p < 0.01); controls (doxorubicin) also showed significant inhibition, but lesser than that observed with C. hybridus (p < 0.05). Results with R. officinalis callus and seedling extracts did not significantly differ from those with untreated cells. CONCLUSION: Methanolic extracts of R. officinalis and C. hybridus are potentially valuable options for breast cancer treatment.
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Antineoplásicos Fitogénicos/farmacología , Proliferación Celular/efectos de los fármacos , Cinamatos/farmacología , Coleus/química , Depsidos/farmacología , Extractos Vegetales/farmacología , Rosmarinus/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Supervivencia Celular , Cinamatos/aislamiento & purificación , Depsidos/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Humanos , Células MCF-7 , Extractos Vegetales/aislamiento & purificación , Brotes de la Planta/química , Plantones/química , Ácido RosmarínicoRESUMEN
Greener nanotechnology plays an important role in developing alternative and effective treatment strategies for various diseases. Biological synthesis of metal nanoparticles (MNPs) has known to possess suitable alternatives than the existing chemical methods. Greener synthesis of MNPs by using plant extracts has become an emerging field due to their safe, eco-friendly and non-toxic nature that are suitable for synergistic biological activities. Hence, the greener method is chosen by the present study. In the present study, the greener synthesis of gold nanoparticles (AuNPs) was successfully done by using Coleus aromaticus leaf extract at three different temperatures (30⯰C, 60⯰C and 100⯰C). The formation of AuNPs was initially monitored by visual observation and then characterized with the help of diverse techniques like UV-Vis spectroscopy (UV-Vis), X-ray diffraction (XRD), Fourier transform infrared (FT-IR) spectroscopy, Scanning Electron Microscopy (SEM), High Resolution-Transmission Electron Microscopy (HR-TEM) and dynamic light scattering (DLS). Surface plasmon resonance (SPR) peak and crystalline nature of AuNPs were obtained by UV-Vis and XRD spectroscopies respectively. FT-IR analysis shows the different characteristic functional groups in turn responsible for the bio-reduction of gold ions by using leaf extract. The formations of different nano-sized AuNPs with their different morphologies were observed by SEM and HR-TEM analyses. Surface charge and stability of the AuNPs were measured by zeta potential and DLS respectively. The synthesized AuNPs coated with cotton fabric was analyzed by UV-Diffuse Reflectance Spectroscopy (UV-DRS), which revealed excellent UV protection against UV radiation. The AuNPs coated cotton fabric exhibited remarkable antibacterial sensitivity against Staphylococcus epidermidis and Escherichia coli. Further, the synthesized AuNPs showed significant cytotoxicity against human liver cancer (HepG2) cell line. The findings of this study revealed that, AuNPs synthesized using Coleus aromaticus leaf extract could be an alternative, safe, and effective source of UV protection, antibacterial and anticancer agents.
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Coleus/química , Oro/química , Tecnología Química Verde/métodos , Nanopartículas del Metal/química , Extractos Vegetales/química , Hojas de la Planta/química , Antibacterianos/farmacología , Muerte Celular/efectos de los fármacos , Fibra de Algodón , Dispersión Dinámica de Luz , Células Hep G2 , Humanos , Concentración 50 Inhibidora , Nanopartículas del Metal/ultraestructura , Pruebas de Sensibilidad Microbiana , Espectrofotometría Ultravioleta , Espectroscopía Infrarroja por Transformada de Fourier , Difracción de Rayos XRESUMEN
Copper oxide nanoparticles (CuO NPs) are fabricated using Coleus aromaticus leaf extract with an environmental friendly method and studied using various microscopic and spectroscopic techniques. Also, a new aptamer-conjugated hybrid delivery system using green synthesized CuO NPs is developed to deliver miRNA-29b to A549 cells. This delivery system can effectively deliver miRNAs to cancer cells, with superior performance compared to traditionally available transfection agents, thus acting as an efficient platform for intracellular miRNA delivery and improving therapeutic outcomes for lung cancer.
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Aptámeros de Nucleótidos/química , Cobre/química , Nanopartículas del Metal/química , MicroARNs/metabolismo , Transfección/métodos , Células A549 , Supervivencia Celular/efectos de los fármacos , Coleus/química , Coleus/metabolismo , Dispersión Dinámica de Luz , Tecnología Química Verde , Humanos , Neoplasias Pulmonares/metabolismo , Neoplasias Pulmonares/patología , Nanopartículas del Metal/toxicidad , MicroARNs/química , Microscopía Fluorescente , Extractos Vegetales/químicaRESUMEN
Active plant metabolites (APM) are recognized as modifiers of ruminal microbial fermentation including methanogenesis and biohydrogenation of fatty acids (FA). Coleus amboinicus Lour. leaves (CAL) are rich in several APM, which could serve as ruminal fermentation modulators. A phytochemical analysis showed that CAL contain phenolic acids (10.4 mg·g-1 dry matter [DM]; high in rosmarinic acid), flavonoids (2.6 mg·g-1 DM), diterpenes (2 mg·g-1 DM), and linolenic acid (35.4 g (100 g)-1 FA). This study aimed to investigate the effect of CAL on ruminal methanogenesis and biohydrogenation as well as basic fermentation characteristics and microbial populations. The in vitro experiment was carried out using Hohenheim gas test system with 40 mL of buffered ruminal fluid incubated for 24 h at 39 °C in anaerobic conditions. Approximately 400 mg (DM basis) of total mixed ration (TMR) was used as a control substrate and the CAL substrate was used at doses of 10, 20, 40, and 80 mg DM replacing equal amounts of TMR. Addition of CAL decreased methane production up to 30% linearly as the amount of CAL increased (P < 0.05). In vitro dry matter digestibility and ammonia tended to increase with increasing doses of CAL. Concentration of total volatile fatty acids was not affected by the CAL although there appeared to be a minor positive linear trend; however, acetate, butyrate, and isobutyrate proportion increased quadratically (P < 0.001). CAL tended to linearly increase α-linolenic acid and conjugated linoleic acid as well as increased stearic acid concentration in buffered ruminal fluid. CAL particularly increased total protozoa and bacterial populations during fermentation, but inhibited methanogens. It is concluded that the CAL may be promising to be used as a feed additive to decrease methanogenesis as well as biohydrogenation of FA in the rumen.
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Coleus/química , Suplementos Dietéticos , Ácidos Grasos/metabolismo , Metano/metabolismo , Preparaciones de Plantas/farmacología , Animales , Dieta/veterinaria , Digestión/efectos de los fármacos , Ácidos Grasos Volátiles/análisis , Femenino , Fermentación/efectos de los fármacos , Hidrogenación , Hidroxibenzoatos/análisis , Hojas de la Planta/química , Preparaciones de Plantas/química , Rumen/metabolismo , Rumen/microbiología , Rumen/parasitologíaRESUMEN
INTRODUCTION: Asthma is an IgE-mediated inflammatory response characterized by hyperresponsiveness, airway inflammation, and reversible airflow obstruction. Currently, asthma affects 12 - 22% of the population in the Philippines. Anecdotal reports showed that yerba buena (Mentha arvensis Linn.) and oregano (Coleus amboinicus Lour.) are utilized for treating asthma in the folk culture.OBJECTIVE: The objective of this study was to determine the effect of combined Yerba Buena (Mentha arvensis Linn.) and Oregano (Coleus amboinicus Lour.) leaves extract in asthma-induced mice.METHODS:This study investigated the anti-asthmatic activity of the aqueous and methanolic extracts of the combined herbs in asthma-induced mice using immunoglobulin E (IgE) as a parameter.RESULTS: Aqueous- and methanol-treated mice has 50% and 60% reduction in the IgE level, respectively (p = 0.018). The extracts exhibited a significant (p = 0.001) anti-inflammatory activity in mice that further proved its effect on IgE. Moreover, lung histopathology also established the potential effect of the extract through the widening of the alveoli on treated mice.CONCLUSION: Combined Yerba Buena and Oregano aqueous and methanol extracts may have a potential health benefit against asthma.
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Ratones , Animales , Asma , Origanum , Metanol , Coleus , Mentha , Filipinas , Antiasmáticos , Antiinflamatorios , InflamaciónRESUMEN
RESUMO O presente trabalho descreve a composição físico-química, a avaliação da atividade antioxidante pelo método de sequestro de radicais livres DPPH, determinação de flavonoides e de fenóis totais dos extratos etanol, acetona e aquoso de Plectranthus barbatus Andr. (Lamiaceae), desidratadas em secador solar e em estufa de circulação de ar a 60 oC. Os valores de atividade de água encontrados para as duas secagens foram inferiores ao mínimo necessário para o crescimento e produção de toxina de patógenos de importância alimentar. Os resultados das análises físico-químicas demonstraram que ambos os processos mostraram-se eficientes na desidratação de P. barbatus. Os resultados demonstraram que os extratos acetona (estufa) e etanol (estufa e secador solar) foram os que apresentaram maior conteúdo de fenóis totais. O extrato etanólico (estufa) apresentou maior quantidade de flavonoides e melhor potencial antioxidante (IC50 = 75,71 ± 10,57 µg mL-1).
ABSTRACT This paper describes the physicochemical composition, the evaluation of the antioxidant activity by free DPPH radicals using the scavenging method, the determination of flavonoids and total phenolic compounds of ethanol, acetone and aqueous extracts of the medicinal plant Plectranthus barbatus Andr. (Lamiaceae), dehydrated in solar dryer and circulation oven at 60 °C. Water activity rates for two drying methods were below the minimum necessary for growth and toxin production of important food pathogens. Physicochemical results showed that both processes were effective in the dehydration of P. barbatus. The results demonstrated that the acetone (over) and ethanol (over and solar dryer) extracts showed the highest content of total phenols. The ethanol extract (over) showed the highest amount of flavonoids and better antioxidant activity (75.71 ± 10.57 µg L-1).
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/análisis , Plectranthus/clasificación , /análisis , Antioxidantes/análisis , Coleus/clasificación , Peumus/clasificaciónRESUMEN
Forskolin, a diterpene, 7ß-acetoxy-8,13-epoxy-1α,6ß,9α-trihydroxy-labd-14-en-11-one (C22H34O7) isolated from Coleus forskohlii, exerts multiple physiological effects by stimulating the enzyme adenylate cyclase and increasing cyclic adenosine monophosphate (cAMP) concentrations. Forskolin is used in the treatment of hypertension, congestive heart failure, eczema, and other diseases. A cytogenetic assay was performed in Allium cepa to assess possible genotoxic effects of forskolin. Forskolin was tested at concentrations 5-100 µM for exposure periods of 24 or 48 h. Treated samples showed significant reductions in mitotic index (p < 0.05) and increases in the frequency of chromosome aberrations (p < 0.01) at both exposure times. The treated meristems showed chromosome aberrations including sticky metaphases, sticky anaphases, laggard, anaphase bridges, micronuclei, polyploidy, fragments, breaks, and C-mitosis. Forskolin may cause genotoxic effects and further toxicological evaluations should be conducted to ensure its safety.
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Broncodilatadores/toxicidad , Aberraciones Cromosómicas , Colforsina/toxicidad , Meristema/efectos de los fármacos , Cebollas/efectos de los fármacos , Vasodilatadores/toxicidad , Anafase/efectos de los fármacos , Broncodilatadores/aislamiento & purificación , Coleus/química , Colforsina/aislamiento & purificación , Humanos , Meristema/citología , Meristema/genética , Metafase/efectos de los fármacos , Micronúcleos con Defecto Cromosómico , Pruebas de Mutagenicidad , Cebollas/citología , Cebollas/genética , Poliploidía , Vasodilatadores/aislamiento & purificaciónRESUMEN
This in vivo study in rats evaluated whether Coleus forskohlii extract (CFE) taken orally interacted with tolbutamide, a hypoglycemic drug metabolized by CYP2C enzymes. Rats were fed 0%, 0.3%, 1% (w/w) CFE diet for 2 weeks, followed by 0% CFE diet for 1 day. They were then given 40 mg/kg tolbutamide by intragastric gavage. Blood glucose level was determined up to 6 h after tolbutamide administration. CFE treatment increased total CYP content and various CYP subtypes in the liver. In particular, increases in activity and protein expression were noted for the CYP2B, CYP2C, and CYP3A subtypes. CFE treatment dose-dependently attenuated both the hypoglycemic action of tolbutamide at 6 h and the plasma concentration of tolbutamide. The activity of (S)-warfarin 7-hydroxylase, a CYP2C enzyme was negatively correlated with plasma tolbutamide level, which also showed a negative correlation with the reduction of blood glucose level. These results indicate that CFE induced hepatic CYPs in rats and attenuated the hypoglycemic action of tolbutamide via a hepatic CYP2C-mediated mechanism.
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Coleus , Sistema Enzimático del Citocromo P-450/metabolismo , Interacciones de Hierba-Droga , Hipoglucemiantes/farmacología , Hígado/enzimología , Extractos Vegetales/efectos adversos , Extractos Vegetales/farmacología , Tolbutamida/farmacología , Animales , Masculino , Vacuna contra la Parotiditis , Ratas WistarRESUMEN
OBJECTIVE: Coleus aromaticus, commonly called country borage or Indian borage, is a perennial herb grown throughout the Indian subcontinent. Traditionally, the leaves of the plant are used as a cure for cold, cough, and fever as well as to relieve pain from skin irritations. However, the appetite-enhancing potential of the herb was unexplored. Based on the encouraging results of animal studies, this study was taken up to establish the appetite-enhancing potential of Coleus aromaticus in humans by evaluating its ready-to-drink beverage. METHODS: A homogenous and healthy group of volunteers was selected. Ready-to-drink beverages based on the herb karpurvalli (Coleus aromaticus) containing three different concentrations (12% [sensorily optimized level], 18%, and 24%) of the herb juice and a placebo beverage were evaluated with the volunteers. The fasting and postprandial levels of plasma leptin were measured, and the appetite rating on a structured visual analog scale was obtained. RESULTS: The study revealed a significant reduction in leptin levels with 12% juice, whereas a significant increase was seen after consumption of the beverage containing 24%. A similar pattern was obtained with the structured ratings. CONCLUSION: The appetite-enhancing effect of the beverage was best when it contained the sensorily optimized level of karpurvalli juice and confirms the results obtained in animal study. To our knowledge, this is the first study validating the appetite-enhancing potential of the herb.
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Apetito/efectos de los fármacos , Bebidas/análisis , Coleus/química , Leptina/sangre , Tejido Adiposo/metabolismo , Adulto , Estatura , Índice de Masa Corporal , Peso Corporal , Ayuno , Femenino , Humanos , Masculino , Músculo Esquelético/metabolismo , Extractos Vegetales/farmacología , Hojas de la Planta/química , Periodo Posprandial , Adulto JovenRESUMEN
Host defense peptides (HDP) have both microbicidal and immunomodulatory properties. Specific induction of endogenous HDP synthesis has emerged as a novel approach to antimicrobial therapy. Cyclic adenosine monophosphate (cAMP) and butyrate have been implicated in HDP induction in humans. However, the role of cAMP signaling and the possible interactions between cAMP and butyrate in regulating HDP expression in other species remain unknown. Here we report that activation of cAMP signaling induces HDP gene expression in chickens as exemplified by ß-defensin 9 (AvBD9). We further showed that, albeit being weak inducers, cAMP agonists synergize strongly with butyrate or butyrate analogs in AvBD9 induction in macrophages and primary jejunal explants. Additionally, oral supplementation of forskolin, an adenylyl cyclase agonist in the form of a Coleus forskohlii extract, was found to induce AvBD9 expression in the crop of chickens. Furthermore, feeding with both forskolin and butyrate showed an obvious synergy in triggering AvBD9 expression in the crop and jejunum of chickens. Surprisingly, inhibition of the MEK-ERK mitogen-activated protein kinase (MAPK) pathway augmented the butyrate-FSK synergy, whereas blocking JNK or p38 MAPK pathway significantly diminished AvBD9 induction in chicken macrophages and jejunal explants in response to butyrate and FSK individually or in combination. Collectively, these results suggest the potential for concomitant use of butyrate and cAMP signaling activators in enhancing HDP expression, innate immunity, and disease resistance in both animals and humans.
Asunto(s)
Butiratos/metabolismo , AMP Cíclico/metabolismo , Inmunidad Innata/efectos de los fármacos , beta-Defensinas/biosíntesis , Animales , Péptidos Catiónicos Antimicrobianos/biosíntesis , Células Cultivadas , Pollos , Coleus , Colforsina/administración & dosificación , Colforsina/metabolismo , Quinasas MAP Reguladas por Señal Extracelular/antagonistas & inhibidores , Quinasas MAP Reguladas por Señal Extracelular/metabolismo , Proteínas Quinasas JNK Activadas por Mitógenos/antagonistas & inhibidores , Proteínas Quinasas JNK Activadas por Mitógenos/metabolismo , Yeyuno , Quinasas Quinasa Quinasa PAM/antagonistas & inhibidores , Quinasas Quinasa Quinasa PAM/metabolismo , Sistema de Señalización de MAP Quinasas , Macrófagos , Extractos Vegetales/administración & dosificación , Extractos Vegetales/metabolismo , Transducción de Señal , Proteínas Quinasas p38 Activadas por Mitógenos/antagonistas & inhibidores , Proteínas Quinasas p38 Activadas por Mitógenos/metabolismoRESUMEN
The present study was conducted for optimization of in vitro substrates under aseptic conditions for interaction of Piriformospora indica with the medicinal plant Coleus forskohlii. It aims to test the effects of different substrates on P. indica colonization as well as growth parameters of the in vitro raised C. forskohlii. Interaction of in vitro C. forskohlii with root endophyte P. indica under aseptic condition resulted in increase in growth parameters in fungus colonized plants. It was observed that P. indica promoted the plant's growth in all irrespective of substrates used for co-culture study. The growth was found inferior in liquid compared to semisolid medium as well as there was problem of hyperhydricity in liquid medium. P. indica treated in vitro plantlets were better adapted for establishment under green house compared to the non treated plants due to fungal intervention.
Asunto(s)
Basidiomycota/crecimiento & desarrollo , Coleus/crecimiento & desarrollo , Coleus/microbiología , Desarrollo de la Planta , Raíces de Plantas/microbiología , Medios de Cultivo/química , Endófitos/crecimiento & desarrolloRESUMEN
This paper is to report the study of the metabolism of forscolin in plasma and liver microsomes for guiding clinical therapy. Forscolin was quantified by HPLC-MS/MS. The metabolic stability of forscolin in rat, Beagle dog, monkey and human plasma and liver microsomes, mediated enzymes of forscolin and its inhibition on cytochrome P450 isoforms in human liver microsomes were studied. Results showed that forscolin was not metabolized in plasma of the four species but metabolized in liver microsomes of the four species. The t1/2 of forscolin in rat, Beagle dog, monkey and human liver microsomes were (52.0 +/- 15.0), (51.2 +/- 5.9), (6.0 +/- 0.2) and (11.9 +/- 1.8) min; CL(int) were (75.6 +/- 18.7), (60.9 +/- 6.8), (513.8 +/- 14.3) and (176.2 +/- 25.6) mL x min(-1) x kg(-1); CL were (34.8 +/- 4.5), (23.3 +/- 1.0), (40.3 +/- 0.5) and (17.9 +/- 0.3) mL x min(-1) x kg(-1), respectively. Forscolin was metabolized by CYP3A4 in human liver microsomes. There was definite inhibition on CYP3A4 at the concentrations of forscolin between 0.1 ng x mL(-1) and 5 microg x mL(-1). Therefore, forscolin is rapidly excreted from liver microsomes. Attention should be paid to the drug interaction when forscolin was used along with other drugs metabolized by CYP3A4 in clinics.
Asunto(s)
Coleus/química , Colforsina/metabolismo , Microsomas Hepáticos/metabolismo , Animales , Cromatografía Líquida de Alta Presión , Colforsina/sangre , Colforsina/aislamiento & purificación , Citocromo P-450 CYP3A/metabolismo , Perros , Humanos , Macaca , Tasa de Depuración Metabólica , Plantas Medicinales/química , Ratas , Espectrometría de Masas en TándemRESUMEN
As obesity has reached epidemic proportions, the management of this global disease is of clinical importance. The availability and popularity of natural dietary supplements for the treatment of obesity has risen dramatically in recent years. The purpose of this paper was to review the effect of commonly available over the counter plant-derived supplements used to suppress appetite for obesity control and management. The data were obtained from the electronic databases PubMed, SpringerLink, Google Scholar, ScienceDirect, and MEDLINE with full text (via EBSCOHost) and the databases were accessed during late 2012 - early January 2013. The botanical species discussed in this review include Camellia sinensis, Caralluma fimbriata, Citrus aurantium, Coleus forskohlii, Garcinia cambogia and Phaseolus vulgaris. This review found that many botanical species including crude extracts and isolated compounds from plants have been shown to provide potentially promising therapeutic effects including appetite control and weight loss. However, many of these crude extracts and compounds need to be further investigated to define the magnitude of the effects, optimal dosage, mechanisms of action, long term safety, and potential side effects.
Asunto(s)
Depresores del Apetito/administración & dosificación , Obesidad/tratamiento farmacológico , Extractos Vegetales/administración & dosificación , Pérdida de Peso , Apocynaceae/química , Apetito/efectos de los fármacos , Camellia sinensis/química , Citrus/química , Coleus/química , Suplementos Dietéticos , Garcinia cambogia/química , Humanos , MEDLINE , Phaseolus/química , Fitoterapia , Extractos Vegetales/efectos adversosRESUMEN
OBJECTIVE: To investigate protective effect of Coleus aromaticus leaf extract against naphthalene induced hepatotoxicity in rats. METHODS: Eighteen male rats were divided into three groups. Group I rats were treated as control. Group II rats were intraperitoneally administered with naphthalene (435 mg/kg b.wt) dissolved in corn oil once a day for a period of 30 days. Group III rats were treated with leaf extract (100 mg/kg b.wt) dissolved in 0.9% saline and naphthalene (435 mg/kg b.wt) dissolved in corn oil once a day for a period of 30 days. RESULTS: Significant protective effect was observed against naphthalene induced liver damage, which appeared evident from the response levels of marker enzymes (aspartate transaminase, alanine transaminase, acid phosphatase, alkaline phosphatase and lactate dehydrogenase). The biochemical components viz. triglycerides, free fatty acids, cholesterol acyl transferase, high-density lipoprotein, low-density lipoprotein, cholesterol and bilirubin were found to be increased in liver and serum of naphthalene stressed rats when compared to control. CONCLUSION: Treatment of naphthalene intoxicated rats with plant extract reversed these distorted parameters to near normal levels. Liver histology showed supportive evidence regarding the protective nature of plant extract against fatty changes induced by naphthalene. The present study provides a scientific rationale for using C. aromaticus in the management of liver disorders.