Assessment of Antioxidant and Cytotoxic Activities and Identification of Phenolic Compounds of Centaurea solstitialis and Urospermum picroides from Turkey

HIGHLIGHTS The phenolic composition, antioxidant activity and cytotoxic potential of the extracts of C. solstitialis and U. picroides were investigated. Caffeic acid was found as the most abundant phenolic compound in the extracts. Both species showed promising antioxidant activity towards different assays. The highest cytotoxic potential was observed in the extract of C. solstitialis.

Abstract It is known that some genera of the Asteraceae family are commonly used in Turkish folk medicine. Several studies have investigated the biological effects of different extracts of Centaurea and Urospermum species, but studies involving the phenolic composition of C. solstitialis and U. picroides extracts are very limited. This study aimed to investigate the phenolic composition and antioxidant activity of C. solstitialis and U. picroides and evaluate their possible cytotoxic effect. RP-HPLC analysis was used to elucidate the phenolic profiles of the ethanolic extracts of flowering parts of C. solstitialis and U. picroides.The both ethanolic extracts were assessed for their antioxidant properties using DPPH, FRAP, phosphomolybdenum and metal chelating assays. Furthermore, the effect of the extracts on cell viability was evaluated against MCF-7 and PC-3 cancer cells and HEK293 cell line using the MTT assay. The most abundant phenolic compound in both extracts was determined to be caffeic acid, and the amount of this compound was 24078.03 and 14329.59 µg g-1 in the extracts of C. solstitialis and U. picroides, respectively. The antioxidant activity of the extracts was found similar. Compared with U. picroides extract, C. solstitialis extract had higher potential on the inhibition of cell viability. The IC50 value of C. solstitialis on MCF cells was found as 58.53 µg mL-1. These data suggest that the extracts of C. solstitialis and U. picroides may be considered as novel and alternative natural antioxidant and anticancer sources.

Glabridin alleviates ischemia/reperfusion-induced functional failure of smooth muscle of rat ileum by upregulating the cAMP / Glabridin alivia la falla funcional inducida por isquemia/reperfusión del músculo liso de ileum murino regulando el incremento de cAMP

Despite the development of modern medicine, alternative medicine, which has not lost its timeliness, remains attractive for the treatment of various diseases. Glabridin, a major flavonoid of Glycyrrhiza glabra, is known for its antioxidant and anti-inflammatory activity. The aim of this study was: 1) to determine the possible protective role of glabridin against ischemia/reperfusion (I/R) injury of the intestine; 2) to evaluate the in vitrocontractile responses of ileum smooth muscles to acetylcholine after an intestinal I/R; and 3) to explain the underlying molecular mechanism of its effect. Rats were assigned to groups of six rats each; 1) I/R, 2) gla10, 3) gla20, 4) gla40, 5) N5-[imino(nitroamino)methyl]-L-ornithine, methyl ester monohydrochloride (L-NAME)+gla40, and 6) Sham group. The healing effect of glabridin was abolished by L-NAME. Glabridin did not cause contractility of the smooth muscles to acetylcholine-induced contractile responses in intestinal I/R. Yet, it increased to spontaneous basal activity.

A pesar del desarrollo de la medicina moderna, la medicina alternativa, sin perder su vigencia, sigue siendo atractiva para el tratamiento de varias enfermedades. Glabradina, el flavonoide mayoritario de Glycyrrhiza glabra, es conocido por su actividad antioxidante y antiinflamatoria. Los propósitos de este estudio fueron: 1) Determinar el posible rol protector de glabradina ante daños intestinales por isquemia/reperfusion (I/R) 2) Evaluar in vitrolas respuestas de contracción de los músculos lisos del ileum ante acetilcolina después de I/R intestinal; y 3) Explicar el mecanismo molecular subyacente de este efecto. Se asignaron grupos de seis ratas: 1) I/R, 2) gla10, 3) gla20, 4) gla40, 5) N5-[imino(nitroamino)metil]-L-ornithina, metil ester monohidrochloruro (L-NAME)+gla40, y 6) Grupo testigo. El efecto curativo de glabridina fue abolido por L-NAME. Glabridina no causó contracción en el músculo liso como respuesta acetilcolina-inducida I/R. Además, incrementa la actividad basal expontánea.

Pharmacological importance of Manilkara zapota and its bioactive constituents / Importancia farmacologica de Manilkara zapota y sus constituyentes bioactivos

Manilkara zapota (Sapotaceae), commonly known as Sapodilla, is widely known for its delicious fruit. Various parts of this plant are also used in folk medicine to treat a number of conditions including fever, pain, diarrhoea, dysentery, haemorrhage and ulcers. Scientific studies have demonstrated analgesic, anti-inflammatory, antioxidant, cytotoxic, antimicrobial, antidiarrheal, anti-hypercholesteremic, antihyperglycemic and hepatoprotective activities in several parts of the plant. Phytochemical studies have revealed the presence of phenolic compounds including protocatechuic acid quercitrin, myricitrin, catechin, gallic acid, vanillic acid, caffeic acid, syringic acid, coumaric acid, ferulic acid, etc. as main constituents of the plant. Several fatty acids, carotenoids, triterpenes, sterols, hydrocarbons and phenylethanoid compounds have also been isolated from M. zapota. The present review is a comprehensive description focused on pharmacological activities and phytochemical constituents of M. zapota.

Manilkara zapota (Sapotaceae), comúnmente conocida como Sapodilla, es ampliamente conocida por su delicioso fruto. Variadas partes de esta planta se usan en medicina popular para tratar una serie de afecciones, como fiebre, dolor, diarrea, disentería, hemorragia y úlceras. Estudios científicos han demostrado actividad analgésica, antiinflamatoria, antioxidante, citotóxica, antimicrobiana, antidiarreica, antihipercolesterolémica, antihiperglucémica y hepatoprotectora en diferentes partes de la planta. Los estudios fitoquímicos han revelado la presencia de compuestos fenólicos que incluyen ácido protocatechúico, quercitrina, miricitrina, catequina, ácido galico, ácido vanílico, ácido cafeico, ácido sirínico, ácido cumárico, ácido fúnico y ácido ferúlico como componentes principales de la planta. Varios ácidos grasos, carotenoides, triterpenos, esteroles, hidrocarburos y compuestos feniletanoides también han sido aislados de M. zapota. La presente revisión es una descripción exhaustiva centrada en las actividades farmacológicas y los constituyentes fitoquímicos de M. zapota.

In vitro antimicrobial and antimycobacterial activity and HPLC-DAD screening of phenolics from Chenopodium ambrosioides L

Abstract The main objective of this study was to demonstrate the antimicrobial potential of the crude extract and fractions of Chenopodium ambrosioides L., popularly known as Santa-Maria herb, against microorganisms of clinical interest by the microdilution technique, and also to show the chromatographic profile of the phenolic compounds in the species. The Phytochemical screening revealed the presence of cardiotonic, anthraquinone, alkaloids, tannins and flavonoids. The analysis by HPLC-DAD revealed the presence of rutin in the crude extract (12.5 ± 0.20 mg/g), ethyl acetate (16.5 ± 0.37 mg/g) and n-butanol (8.85 ± 0.11 mg/g), whereas quercetin and chrysin were quantified in chloroform fraction (1.95 ± 0.04 and 1.04 ± 0.01 mg/g), respectively. The most promising results were obtained with the ethyl acetate fraction, which inhibited a greater number of microorganisms and presented the lowest values of MIC against Staphylococcus aureus and Enterococcus faecalis (MIC = 0.42 mg/mL), Pseudomonas aeruginosa (MIC = 34.37 mg/mL), Paenibacillus apiarus (MIC = 4.29 mg/mL) and Paenibacillus thiaminolyticus (MIC = 4.29 mg/mL). Considering mycobacterial inhibition, the best results were obtained by chloroform fraction against M. tuberculosis, M. smegmatis, and M. avium (MIC ranging from 156.25 to 625 µg/mL). This study proves, in part, that the popular use of C. ambrosioides L. can be an effective and sustainable alternative for the prevention and treatment of diseases caused by various infectious agents.

Phenolic profile and antioxidant activity from peels and seeds of melon (Cucumis melo L. var. reticulatus) and their antiproliferative effect in cancer cells

Melon (Cucumis melo L.) has high economic value and in recent years, its production has increased; however, part of the fruit is wasted. Usually, inedible parts such as peel and seeds are discarded during processing and consumption. Extracts of melon residues were prepared and their phenolic compounds, antioxidants and antiproliferative activities were evaluated. Total phenolic compounds were found in hydroethanolic, hydromethanolic, and aqueous extracts, especially for melon peel (1.016 mg gallic acid equivalent/100 g). Flavonoids total content found for melon peel aqueous extract was 262 µg of catechin equivalent (CA)/100 g. In all extracts of melon peel significant amounts of gallic acid, catechin, and eugenol were found. For total antioxidant capacity, reported as ascorbic acid equivalent, the hydroethanolic and hydromethanolic extracts in peels and hydromethanolic in seeds were 89, 74, and 83 mg/g, respectively. Different extracts of melon showed iron and copper ions chelating activity at different concentrations, especially melon peel aqueous extract, reaching values of 61% for iron and 84% for copper. The hydroethanolic extract of melon peel presented a significant ability for hydroxyl radicals scavenging (68%). To assess the antiproliferative potential in human cancer cell lines, such as kidney carcinoma, colorectal carcinoma, cervical adenocarcinoma and cervical carcinoma, MTT assay was performed. The proliferation was inhibited by 20-85% at extracts concentrations of 0.1-1.0 mg/mL in all cancer cell lines. The results suggest that melon residues extracts display a high antioxidant activity in in vitro assays and have effective biological activity against the growth of human tumor cells.

Inhibitor tolerance of a recombinant flocculating industrial Saccharomyces cerevisiae strain during glucose and xylose co-fermentation

ABSTRACT Lignocellulose-derived inhibitors have negative effects on the ethanol fermentation capacity of Saccharomyces cerevisiae. In this study, the effects of eight typical inhibitors, including weak acids, furans, and phenols, on glucose and xylose co-fermentation of the recombinant xylose-fermenting flocculating industrial S. cerevisiae strain NAPX37 were evaluated by batch fermentation. Inhibition on glucose fermentation, not that on xylose fermentation, correlated with delayed cell growth. The weak acids and the phenols showed additive effects. The effect of inhibitors on glucose fermentation was as follows (from strongest to weakest): vanillin > phenol > syringaldehyde > 5-HMF > furfural > levulinic acid > acetic acid > formic acid. The effect of inhibitors on xylose fermentation was as follows (from strongest to weakest): phenol > vanillin > syringaldehyde > furfural > 5-HMF > formic acid > levulinic acid > acetic acid. The NAPX37 strain showed substantial tolerance to typical inhibitors and showed good fermentation characteristics, when a medium with inhibitor cocktail or rape straw hydrolysate was used. This research provides important clues for inhibitors tolerance of recombinant industrial xylose-fermenting S. cerevisiae.

Evaluation of phenolic compounds and lipid-lowering effect of Morus nigra leaves extract

ABSTRACT Morus nigra L. (Moraceae) is a tree known as black mulberry and the leaves are used in folk medicine in the treatment of diabetes, high cholesterol and menopause symptoms. The aim of this study was to evaluate the M. nigra leaves phytochemical profile in different extractions and the hypolipidemic effect of the infusion comparing to the fenofibrate. Morus nigra infusion (MN) showed higher amounts of phenolics and flavonoids (83.85 mg/g and 79.96 µg/g, respectively), as well as antioxidant activity (83.85%) than decoction or hydromethanolic extracts. Although, decoction showed the best result for ascorbic acid (4.35 mg/100 g) than hydromethanolic or infusion (2.51 or 2.13 mg/100 g, respectively). The phenolic acids gallic, chlorogenic and caffeic and the flavonoids quercetin, rutin and catechin were found in the M. nigra extracts. Hyperlipidemic rats treated with 100, 200 or 400 mg/kg of MN decreased serum cholesterol, triglycerides and normalized lipoproteins. Furthermore, MN inhibited lipid peroxidation in liver, kidney and brain of hyperlipidemic rats. This study provides evidence that M. nigra leaves extracts are rich in polyphenols, mainly chlorogenic acid, which normalized hyperlipidemic disturbance. The results suggest a potential therapeutic effect of the M. nigra leaves infusion on dislipidemic condition and related oxidative stress.

In vitro and cellular activities of the selected fruits residues for skin aging treatment

ABSTRACT Peel extracts of litchi and rambutan, and that of tamarind seed coat were investigated in relation to their utility in skin-aging treatments. Standardized extracts of tamarind were significantly (p < 0.05) more efficient at O2 •- scavenging (IC50 = 27.44 ± 0.09) than those of litchi and rambutan (IC50 = 29.57 ± 0.30 and 39.49 ± 0.52 μg/ml, respectively) and the quercetin standard (IC50 = 31.88 ± 0.15 μg/ml). Litchi extract proved significantly (p < 0.05) more effective for elastase and collagenase inhibition (88.29 ± 0.25% and 79.46 ± 0.92%, respectively) than tamarind (35.43 ± 0.68% and 57.69 ± 5.97%) or rambutan (31.08 ± 0.38% and 53.99 ± 6.18%). All extracts were safe to human skin fibroblasts and inhibit MMP-2, with litchi extract showing significantly (p < 0.01) enhanced inhibition over the standard, vitamin C (23.75 ± 2.74% and 10.42 ± 5.91% at 0.05 mg/ml, respectively). Extracts suppress melanin production in B16F10 melanoma cells through inhibition of tyrosinase and TRP-2, with litchi extract being the most potent, even more so than kojic acid (standard). These results highlight the potential for adding value to agro-industrial waste, as the basis for the sustainable production of innovative, safe, anti-aging cosmetic products.

A potent larvicidal agent against Aedes aegypti mosquito from cardanol

ABSTRACT Cardanol is a constituent of Cashew Nut Shell Liquid that presents larvicidal activity against Aedes aegypti. The isolation of cardanol is somewhat troublesome, however, in this work we describe an efficient and inexpensive method to obtain it as a pure material. The compound was used as starting material to make chemical transformation leading to saturated cardanol, epoxides and, halohydrins. These derivatives were tested for toxicity against Aedes aegypti larvae. The results showed that iodohydrins are very promising compounds for making commercial products to combat the vector mosquito larvae presenting a LC50 of 0.0023 ppm after 72 h of exposure.

Total phenolic, flavonoid, alkaloid and iridoid content and preventive effect of Lider-7-tang on lipopolysaccharide-induced acute lung injury in rats

Lider-7-tang, a medicine used for the treatment of respiratory diseases especially pneumonia and fever in Mongolian Traditional Medicine, was selected for this phytochemical and pharmacological study. The objectives of the study were to determine total biological active substances and analyze the effects of Lider-7-tang treatment in rats with acute lung injury (ALI). Quantitative determination of the total active constituents (phenolic, flavonoid, iridoid and alkaloid) of the methanol extract of Lider-7-tang was performed using Folin-Ciocalteu reagent, aluminum chloride reagent, Trim-Hill reagent, and Bromocresol green reagent, respectively. A total of fifty 8-10-week-old male Wistar rats (200-240 g) were randomized into three groups: control group, lipopolysaccharide (LPS) group (7.5 mg/kg) and LPS+Lider-7 group (90 mg/kg Lider-7-tang before LPS administration). The total content of alkaloids was 0.2±0.043%, total phenols 7.8±0.67%, flavonoids 3.12±0.206%, and iridoids 0.308±0.0095%. This study also evaluated the effects of Lider-7 on levels of inflammatory mediators by observing histopathological features associated with LPS-induced ALI. The rats pretreated with Lider-7 had significantly lower levels of IL-6 (at 3 and 6 h), and TNF-α (at 3, 6, 9, and 12 h). The current study showed that Lider-7 exerted a preventive effect against LPS-induced ALI, which appeared to be mediated by inhibiting the release of pro-inflammatory cytokines.

Melipona mondury produces a geopropolis with antioxidant, antibacterial and antiproliferative activities

ABSTRACT Geopropolis is a special type of propolis produced by stingless bees. Several pharmacological properties have been described for different types of geopropolis, but there have been no previous studies of the geopropolis from Melipona mondury. In this study, we investigated the antioxidant, antibacterial, and antiproliferative activities of M. mondury geopropolis, and determined its chemical profile. The antioxidant activity was determined using in vitro ABTS·+, ·DPPH, and β-carotene/linoleic acid co-oxidation methods. The antibacterial activity was determined using a microdilution method with Pseudomonas aeruginosa, Staphylococcus aureus, and methicillin-resistant S. aureus. The antiproliferative effect was determined in tumor cell lines using the Alamar Blue assay. The chemical profile was obtained using UHPLC-MS and UHPLC-MS/MS. The butanolic fraction had the highest concentration of phenolic compounds and more potent antioxidant properties in all assays. This fraction also had bacteriostatic and bactericidal effects against all bacterial strains at low concentrations, especially S. aureus. The hexane fraction had the highest antiproliferative potential, with IC50 values ranging from 24.2 to 46.6 µg/mL in HL-60 (human promyelocytic leukemia cell) and K562 (human chronic myelocytic leukemia cell), respectively. Preliminary chemical analysis indicates the presence of terpenes and gallic acid in the geopropolis. Our results indicate the therapeutic potential of geopropolis from M. mondury against inflammatory, oxidative, infectious, and neoplastic diseases.

Antioxidant activity and phenol content of extracts of bark, stems, and young and mature leaves from Blepharocalyx salicifolius (Kunth) O. Berg / Atividade antioxidante e teor de polifenóis de extratos de cascas (súber), caule, folhas jovens e folhas maduras de Blepharocalyx salicifolius (Kunth) O. Berg (Murta)

Abstract Phenolic compounds are a group of plant secondary metabolites known to have a variety of bioactivities, including the ability to function as antioxidants. Because of the side effects of the use of synthetic substances, the search for natural and less toxic compounds has increased significantly. This study was designed to evaluate the antioxidant activity and phenol content of hexane, ethyl acetate, and aqueous extracts of the bark (suber) and stems as well as the young and mature leaves of Blepharocalyx salicifolius. The extracts were obtained by extraction with organic solvents and subsequent fractionation by chromatographic partition coefficient. Preliminary tests for the presence of antioxidants were performed using bioautography in thin-layer chromatography. The antioxidant activity of the extracts was assessed using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method, and the phenol content of the extracts was quantified using the Folin-Ciocalteu technique. The results showed that 9 of the 12 extracts evaluated displayed very strong antioxidant activity and three displayed moderate activity. Aqueous extracts of the young leaves and bark and the ethyl acetate extract of the young leaves showed the highest levels of antioxidant activity and total phenolic content (TPC). A correlation was observed between TPC and antioxidant activity index (AAI) with a correlation coefficient (r2) of 0.7999. Thus, the high phenol content of B. salicifolius extracts and its correlation with antioxidant activity provide substrates for further studies.

Resumo Os polifenóis são um grupo de metabólitos secundários vegetais que possuem uma variedade de bioatividades conhecidas, dentre elas a capacidade de funcionar como antioxidantes. Devido aos efeitos colaterais do uso excessivo de substâncias sintéticas, a busca por compostos naturais e menos tóxicos têm aumentado significativamente. Esse estudo teve por objetivo avaliar a atividade antioxidante e o teor de polifenóis dos extratos hexânicos, acetato de etila e aquosos de cascas (súber), caules, folhas jovens e folhas maduras de Blepharocalyx salicifolius. Os extratos foram obtidos por meio de extração com solventes orgânicos e subsequente fracionamento em cromatografia por coeficiente de partição. Testes preliminares da presença de compostos com atividade antioxidante foram realizados por meio de bioautografia em cromatografia de camada delgada. Os extratos foram submetidos ao teste da capacidade sequestrante do radical 2,2-difenil-1-picrilhidrazil (DPPH) para quantificação da atividade antioxidante e submetidos ao teste com o reagente de Folin-Ciocalteu para quantificação dos polifenóis. Os resultados mostraram que dos 12 extratos avaliados, 9 apresentaram atividade antioxidante muito forte e 3 atividade moderada. Os extratos aquosos de folhas jovens e cascas e o extrato acetato de etila de folhas jovens apresentaram os maiores índices de atividade antioxidante e teor de polifenóis (TPC). A correlação entre TPC e o índice de atividade antioxidante (AAI) observada foi de r2 = 0,7999. Dessa forma, ficou evidenciado o elevado teor de polifenóis e sua correlação com a atividade antioxidante nos extratos de B. salicifolius, fornecendo subsídios para novos estudos.

Expression analysis of vasa in Asian paddle crab (Charybdis japónica) exposed to Bisphenol A

Background: Bisphenol A (BPA) is an endocrine-disrupting chemical (EDC) with a weak estrogen-like activity in fish that is found ubiquitously in aquatic environments. However, there has been little study about BPA on the endocrine disrupting effects of crab. In the present study, cDNA of vasa was cloned and characterized in the Charybdis japonica. Histological structures of testis and expression patterns of vasa gene in the testis of C. japonica after treatment with BPA were investigated. Results: The cDNA of vasa is composed of 3051 bp with a 2166 bp open reading frame encoding 721 AA. The deduced amino acid sequence contained eight conserved domains of the DEAD-box protein family. The tissue distribution showed that vasa mRNA was specifically expressed in ovary and testis. Histologically, the sperm cells were decreased in number and an acellular zone was seen in the testis. The transcript level of vasa gradually increased with a significant difference between the experimental and control groups. After BPA exposure with 0.50 and 1.00 mg/L for 1,3, 6 and 9 d, the expression levels of vasa increased. Conclusion: These findings suggest that BPA can increase the expression level of vasa mRNA and influence the development of the testis in C. japonica.

Photoprotective effect of verbascoside from Buddleja cordata in SKH-1 mice exposed to acute and chronic UV-B radiation / Efecto fotoprotector del verbascósido de Buddleja cordata en ratones SKH-1 expuestos de forma aguda y crónica a laradiación UV-B

Ultraviolet radiation (UVR) is involved in both sunburn and the development of skin cancer, which has a high incidence worldwide. Strategies to reduce these effects include the use of photoprotective substances. The aim of this work was to investigate the photoprotective effect of verbascoside isolated from the methanolic extract of Buddleja cordata (BCME) in SKH-1 mice exposed to acute and chronic UV-B radiation. The mouse dorsal area was evaluated macroscopically and microscopically for diagnosis; verbascoside penetration into mouse skin was investigated in vivo by the tape stripping method. After acute UV-B exposure, 100 percent of irradiated mice that had been protected with verbascoside showed no signs of sunburn or of inflammatory processes. After chronic exposure, 100 percent of unprotected mice showed skin carcinomas; in contrast, in mice topically treated with either BCME or verbascoside, the presence of lesions was decreased by 90 percent. These results prove that verbascoside penetrates through the skin of mice and suggest that verbascoside and BCME may potentially prevent photodamage on mice’s skin after acute and chronic UVR exposure.

La radiación ultravioleta (RUV) provoca quemaduras solares y el desarrollo de cáncer de piel. El objetivo de este trabajo fue investigar el efecto fotoprotector del verbascósido obtenido del extracto metanólico de Buddleja cordata (EMBC) en ratones SKH-1 expuestos a RUV-B de manera aguda y crónica. El diagnóstico histológico se llevó a cabo en la piel de la zona dorsal de los ratones. La penetración del verbascósido fue cuantificada mediante la técnica de la cinta adhesiva. En el experimento agudo, el 100 por ciento de los ratones protegidos con verbascósido no evidenciaron signos de quemadura ni procesos inflamatorios. En el experimento crónico los ratones sin protección e irradiados presentaron carcinomas cutáneos. En contraste en los ratones protegidos con EMBC o verbascósido las lesiones disminuyeron un 90 por ciento en ambos grupos. El verbascósido penetró en la piel del ratón. Los resultados sugieren que el EMBC y el verbascósido previenen el fotodaño en la piel de ratones expuestos de forma aguda o crónica a la RUV.

Histopathological and immunohistochemical changes induced by Bisphenol A in reproductive tissues of female rat

Background: Bisphenol A [BPA] is an environmental chemical that has been widely used in the manufacture of polycarbonate plastics and epoxy resins for many years. Due to its major applications in the production of plastic food or beverage containers and the coating of food cans, people of different ages are inevitably exposed to BPA in daily life. It is a contaminant with increasing exposure to it and exerts both toxic and estrogenic effects on mammalian cells

Aim of the work: the present study was designated to evaluate the histopathological and immunohistochemical effect of BPA on the histoarchitecture of pituitary ,adrenal, ovarian and uterine axis of female albino rats and the ameliorative effect of antiestrogen drug and stem enhance

Experimental model and methods: 20 female albino rats weighing 100 - 120 g. were kept under observation for about 15 days before the onset of the experiment for adaptation, then the rats were classified into 4 groups 5 rats for each , the first group was left without any treatment for 30 days as negative control group , the second group was administered with 20 mg/kg.bw of BPA for 15 consecutive days as positive control, the third group administered with 20 mg/kg.bw of BPA for 15 consecutive days and then treated with antiestrogen drug as 0.1 mg/100gm.bw for 15 day, the fourth group administered with the same dose for the same period and the treated with stem enhance [4.5 mg/100.bw] for 15 days. All rats are scarified and organs were histologically examined after processing

Results: The results showed that PA has a histopathological effects on vital organs [pituitary, adrenal, ovary, oviduct and uterus] even for a short period with minimal ameliorative effect of antiestrogen drug and stem enhance

Effect of estradiol and bisphenol A on human hepatoblastoma cell viability and telomerase activity

Sex hormones from environmental and physiological sources might play a major role in the pathogenesis of hepatoblastoma in children. This study investigated the effects of estradiol and bisphenol A on the proliferation and telomerase activity of human hepatoblastoma HepG2 cells. The cells were divided into 6 treatment groups: control, bisphenol A, estradiol, anti-estrogen ICI 182,780 (hereinafter ICI), bisphenol A+ICI, and estradiol+ICI. Cell proliferation was measured based on average absorbance using the Cell Counting-8 assay. The cell cycle distribution and apoptotic index were determined by flow cytometry. Telomerase activity was detected by polymerase chain reaction and a telomeric repeat amplification protocol assay. A higher cell density was observed in bisphenol A (P<0.01) and estradiol (P<0.05) groups compared with the control group. Cell numbers in S and G2/M phases after treatment for 48 h were higher (P<0.05), while the apoptotic index was lower (P<0.05) and telomerase activities at 48 and 72 h (P<0.05) were higher in these groups than in the control group. The cell density was also higher in bisphenol A+ICI (P<0.01) and estradiol+ICI (P<0.05) groups compared with the ICI group. Furthermore, cell numbers were increased in S and G2/M phases (P<0.05), while the apoptotic index was lower (P<0.05) and telomerase activities at 48 and 72 h were higher (P<0.05) in these groups than in the ICI group. Therefore, bisphenol A and estradiol promote HepG2 cell proliferation in vitro by inhibition of apoptosis and stimulation of telomerase activity via an estrogen receptor-dependent pathway.

The thyroid hormone receptor β-selective agonist GC-1 does not affect tolerance to exercise in hypothyroid rats

Objective Investigate the effect of GC-1 on tolerance to exercise in rats with experimental hypothyroidism. Materials and methods Hypothyroidism was induced with methimazole sodium and perchlorate treatment. Six groups with eight animals were studied: control group (C), hypothyroid group without treatment (HYPO); hypothyroidism treated with physiological doses of tetraiodothyronine (T4) or 10 times higher (10×T4); hypothyroidism treated with equal molar doses of GC-1 (GC-1) or 10 times higher (10×GC-1). After eight weeks, each animal underwent an exercise tolerance test by measuring the time (seconds), in which the rats were swimming with a load attached to their tails without being submerging for more than 10 sec. After the test, the animals were killed, and blood samples were collected for biochemical analysis, and the heart and soleus muscle were removed for weighing and morphometric analysis of the cardiomyocyte. Results Hypothyroidism significantly reduced tolerance to exercise and, treatment with GC-1 1× or T4 in physiological doses recover tolerance test to normal parameters. However, high doses of T4 also decreased tolerance to physical exercise. Conversely, ten times higher doses of GC-1 did not impair tolerance to exercise. Interestingly, hypothyroidism, treated or not with T4 in a physiological range, GC-1 or even high doses of GC-1 (10X) did not change cardiomyocyte diameters and relative weight of the soleus muscle. In contrast, higher doses of T4 significantly increased cardiomyocyte diameter and induced atrophy of the soleus muscle. Conclusion Unlike T4, GC-1 in high doses did not modify tolerance to physical exercise in the rats with hypothyroidism. .

Determinação de parâmetros farmacognósticos para as folhas de Erythroxylum suberosum A. St.-Hilaire (Erythroxylaceae) coletadas no município de Goiânia, GO. / Determination of pharmacognostic parameters for the leaves of Erythroxylum suberosum A. St.-Hilaire (Erythroxylaceae) collected in the city of Goiania, GO

RESUMO As plantas medicinais representam um dos principais recursos terapêuticos utilizado pelo homem para a cura e prevenção de doenças, no entanto, para que o tratamento seja seguro e eficaz é necessário conhecer seus componentes químicos. Dessa forma, o intuito deste trabalho foi determinar os parâmetros farmacognosticos para o estabelecimento do controle de qualidade da droga vegetal composta pelas folhas de Erythroxylum suberosum A. St.-Hil., pertencentes à família Erythroxylaceae ocorrente no Cerrado. Para tanto, foram coletadas folhas adultas nas proximidades da Universidade Federal de Goiás, Goiânia-GO. Foram determinados o teor de umidade por meio de balança com irradiação de raios infravermelho e o teor de cinzas totais. Na prospecção fitoquímica foram pesquisadas as classes de metabólitos secundários e realizou-se o doseamento de fenóis totais, flavonoides e taninos totais. Os resultados dos testes de pureza realizados, teor de umidade e teor de cinzas totais, estão de acordo com os limites estabelecidos pelas especificações farmacopeicas. As análises fitoquímicas evidenciaram a presença de flavonoides, taninos, cumarinas, saponinas e resinas. No doseamento de fenóis totais, taninos e flavonoides presentes nas folhas de E. suberosum A. St.-Hil. obteve-se respectivamente 17,97%, 6,31%, 3,87%. Estes resultados confirmam os dados da literatura quanto à presença destes compostos em Erythroxylaceae, pois de acordo com nas folhas de E. tortuosum obteve-se valores de 10%, 8,4% e 0,064% de Fenóis, Taninos e flavonoides, respectivamente e nas folhas de E. deciduum foram encontrados 12,04% de fenóis totais, 0,87% de taninos e 1,37% de flavonoides. Os resultados encontrados no presente trabalho também se tornam relevantes quando comparadas as quantidades desses metabólitos com espécies clássicas na biossíntese de compostos fenólicos como o teor de taninos de Stryphnodendron adstringens (Mart.) Coville e em Eugenia uniflora L. foi de 29,9% e 2,96%, respectivamente. Teores de flavonóides que variaram entre 0,65% a 0,79% na Calendula officinalis L. e Ginkgo bilobaL. 0,59%, 0,75% e 0,79%. Sendo assim, a quantidade considerável de compostos fenólicos obtida em E. suberosum A. St.-Hil. sugere que a espécie possua um importante potencial terapêutico e quem sabe potencial antioxidante, a ser explorado em estudos posteriores.

ABSTRACT Medicinal plants represent a major therapeutic resources used by man for the cure and prevention of diseases, however, that the treatment be safe and effective it is necessary to know their chemical components. Thus, the aim of this work was to determine the pharmacognostic parameters for the establishment of the plant drug quality control made by the leaves of Erythroxylum suberosum A. St.-Hil., belonging to the family Erythroxylaceae occurring in the Cerrado. To this end, adult leaves were collected near the Federal University of Goiás, Goiânia-GO. It was determined the moisture content through scale radiating infrared rays and the content of total ash. The phytochemical screening of secondary metabolites classes were surveyed and performed the determination of total phenols, flavonoids and total tannins. The results of the purity tests, moisture content and total ash content, are in accordance with the limits established by the pharmacopeic specifications. The phytochemical analysis revealed the presence of flavonoids, tannins, coumarins, saponins and resins. The determination of total phenols, tannins and flavonoids quantities present in the leaves of E. suberosum A. St.-Hil. were obtained respectively as 17.97%, 6.31%, 3.87%. These results confirm the literature data for the presence of these compounds in Erythroxylaceae, since according to the leaves of E. tortuosum yielded values of 10%, 8.4% and 0.064% of phenols, tannins and flavonoids, respectively. On the E. deciduum leaves were found 12.04% of total phenols, tannins 0.87% and 1.37% of flavonoids. The results of this work also become relevant when comparing the amounts of these metabolites with classic species in the biosynthesis of phenolic compounds such as tannins content in barbatimão and pitanga was 29.9% and 2.96%, respectively. Flavonoid contents ranging from 0.65% to 0.79% in calendula and ginkgo 0.59%, 0.75% and 0.79%. Thus, considerable amount of phenolic compounds obtained in E. suberosum. A. St. Hil. It suggests that the species has an important therapeutic potential and who knows antioxidant potential to be explored in further studies.

Optimization of laccase production by two strains of Ganoderma lucidum using phenolic and metallic inducers / Optimización de la producción de lacasa por dos cepas de Ganoderma lucidum utilizando inductores fenólicos y metálicos

Ganoderma lucidum (Curtis) P. Karst es un hongo causante de pudrición blanca, capaz de degradar la lignina de la madera y otros sustratos en los que crece. En este trabajo se evaluó la capacidad de dos cepas de esta especie de producir la enzima ligninolítica lacasa. Asimismo, se ensayó la inducción de esta enzima con diferentes compuestos fenólicos e iones metálicos, y se encontró que el ácido ferúlico y el cobre fueron los mejores inductores de la lacasa entre los agentes evaluados. También se encontró que los dos tipos de inductores (fenólicos y metálicos) producen distintos patrones electroforéticos de actividad lacasa. Las concentraciones óptimas de los inductores fueron establecidas mediante un diseño factorial. Se estimó la estabilidad térmica de la lacasa en un amplio rango de pH ácidos, y se comprobó que a pH más altos la enzima es más termoestable.

Ganoderma lucidum (Curtis) P. Karst is a white rot fungus that is able to degrade the lignin component in wood. The ability of two strains of this species to produce the ligninolytic enzyme laccase was assessed. After the evaluation of induction with heavy metals and phenolic compounds, it was found that among the tested substances, copper and ferulic acid are the best laccase inducers. It was also observed that the two types of inducers (phenolic and metallic) produce different electrophoretic patterns of laccase activity. Optimized concentrations of inducers were obtained through a factorial design and the thermal stability of optimized supernatants was studied at a wide range of acidic pH. We found that the enzyme is more thermostable at higher pH values.

Estrous cycle disruptor effect of an ethanolic extract from Buddleja globosa leaves and its main component (verbascoside) / Efecto disruptor del ciclo estral de un extracto etanólico de hojas de Buddleja globosa y de su componente principal (verbascósido)

The estrous cycle disruptor effect of an ethanolic extract (EMATst) from Buddleja globosa leaves and standardized in its main component (verbascoside) was determined in rats after the subcutaneous administration of EMATst. Binding of EMATst and verbascoside to the estrogen receptor (ER) of EMATst and verbacoside was also measuredestablished. EMATst produced a significant alteration inof the estrous cycle only at the highest dose (10-5 M), which could be attributed to an antiestrogenic effect. The Bbinding of EMATst and verbascoside to the ER was competitive and occurred in concentrations 1000 times greater than that of 17beta-estradiol.

El efecto disruptor del ciclo estral de un extracto etanólico (EMATst) obtenido a partir de las hojas de Buddleja globosa y estandarizado en su componente mayoritario (verbascósido) fue determinado en ratas después de la administración subcutánea de EMATst. Se estableció además la unión al receptor estrogénico (RE) tanto de EMATst como de verbascósido. EMATst sólo a la dosis más alta (10-5M) produjo una alteración significativa del ciclo estral, lo que podría atribuirse a un efecto antiestrogénico. La unión al RE de EMATst y verbascósido se produjo a concentraciones 1000 veces mayor que el 17beta-estradiol y de forma competitiva.