Resumo em Inglês:

ABSTRACT The aim of this study was to analyze the morphology and anatomy of the leaves of Protium ovatum Engl., Burseraceae, and verify the antiproliferative activity in cervical cells. For anatomical analysis, the leaf samples were fixed in formol, acetic acid, alcohol 70, dehydrated, included in hydroxyethyl methacrylate and sectioned at a thickness of 5–10 µm in rotative microtome. The samples were stained with toluidine blue and blades mounted with synthetic resin “Entellan”. Histochemical tests and scanning electron microscopy were also performed. To investigate the antiproliferative effect we used the cells strain of human cervix carcinoma and normal keratinocytes. The anatomical analysis demonstrated that the leaf is hypostomatic and the epidermal cells walls were slightly undulate on both faces. The palisade parenchyma occupies most part of leaf mesophyll. The spongy parenchyma is organized into 3–4 layers of cells. Vascular bundles of smaller diameter and secretory cavities are distributed along the leaf mesophyll. The midrib region was formed by a single vascular bundle with xylem in the center surrounded by phloem. Secretory cavities are distributed along the phloem. The histochemical tests revealed the presence of lipids in the secretory cavities and phenolic compounds in almost cell of mesophyll. Scanning electron microscopy analysis showed the smooth leaf cuticle ornamentation with some striated areas. It was observed antiproliferative effect on human cervix carcinoma cell comparing with normal cells.

Resumo em Inglês:

ABSTRACT The profile of volatile organic compounds, the glandular and non-glandular trichomes of Plectranthus ornatus, obtained by in vitro cultivation, was evaluated in plants grown in Murashide and Skoog medium supplemented with benylaminopurine at 4.5, 9.0, and 18.0 µM + naphthaleneacetic acid at 5.37 µM, kinetin at 4.7, 9.3 and 18.5 µM + naphthaleneacetic acid (5.37 µM) or Murashide and Skoog 0 medium (as a control). Scanning Electron Microscopy was performed on samples of the third leaf node of the 90 days old plants obtained from treatment with 4.5 or 9.0 µM benylaminopurine, and 4.7 or 9.3 µM kinetin. Headspace Solid Phase Micro-Extraction of the 30, 60 and 90 days old in vitro plants permitted to determinate by GC/MS the composition comprised of 62 compounds. The data were analyzed using Principal Component Analysis and Hierarchical Clustering Analysis and, the major constituents of these oils after treatment and aging were monoterpenes and sesquiterpenes. Morphoanatomical analysis of trichomes, by Scanning Electron Microscopy, enabled the identification of non-glandular trichomes and four types of glandular trichomes, which comprised capitate and peltate glandular trichomes that were distributed on both sides of the leaf. We observed that the regulators influenced qualitative and quantitative profiles of the volatile organic compounds and the number and distribution of hairs on the leaf surface.

Resumo em Inglês:

ABSTRACT Stephania venosa (Blume) Spreng., Menispermaceae, has been traditionally used as tonic drug and treatment of various diseases in South East Asian countries. In order to evaluate the quality and standardization of S. venosa roots, the HPLC method for quantification of the content of major components in S. venosa was developed and validated. The chromatographic separation was performed on a Hypersil BDS C18 column using gradient system of 100 mM ammonium acetate in water and methanol with flow rate 1 ml/min. Detection wavelength was set at 210 nm for tetrahydropalmatine, 280 nm for dicentrine and crebanine, and 270 nm for stephanine. The validated method showed good sensitivity, linearity, precision, and accuracy. The suitable solvent that yielded highest alkaloids contents from the matrix was optimized. S. venosa samples collected from various locations were analyzed. The present study provided comprehensive overview of major components in S. venosa. A remarkable variation in the accumulation of alkaloids in each population and the between individual in the same population could be observed. Our results showed the heterogeneity of S. venosa in Thailand which would need a further study for species delimitations.

Resumo em Inglês:

ABSTRACT A new ursane-type triterpene ester, plectraterpene [3β-(decanoyloxy)-19-hydroxy-urs-12-ene] and four known steroidal compounds have been isolated from the aerial parts of Plectranthus montanus Benth. (syn. Plectranthus cylindraceus Hochst. ex Benth.), Lamiaceae. The known compounds were stigmasterol, sitosteryl ferulate, cholest-5-en-3-O-β-D-glucopyranoside and stigmasterol-3-O-β-D-glucopyranoside. Compounds plectraterpene, sitosteryl ferulate and stigmasterol-3-O-β-D-glucopyranoside are reported for the first time from this plant whereas compound cholest-5-en-3-O-β-D-glucopyranoside first time from the genus. The structures of these compounds were determined through spectral analysis, including extensive 2D NMR data as well as chemical methods and comparison with literature.

Resumo em Inglês:

ABSTRACT In general, Passiflora species have been reported for their folk medicinal use as sedative and anti-inflammatory. However, P. caerulea has already been reported to treat pulmonary diseases. Severe pulmonary tuberculosis, generally caused by Mycobacterium tuberculosis strains resistant to multiple drugs, can lead to deleterious inflammation and high mortality, encouraging new approaches in drug discovery. Thus, the aim of this work was to evaluate the Passiflora mucronata Lam., Passifloraceae, potential for tuberculosis treatment. Specifically, related to antimycobacterial activity and anti-inflammatory related effects (based on inhibition of nitric oxide, tumor necrosis factor-alpha production and antioxidant potential), as well as the chemical profile of P. mucronata. High performance liquid chromatography coupled with diode-array ultraviolet and mass spectrometer analyses of crude hydroalcoholic extract and ethyl acetate fraction showed the presence of flavonoids. Ethyl acetate fraction showed to be as antioxidant as Ginkgo biloba standard extract with EC50 of 14.61 ± 1.25 µg/ml. One major flavonoid isolated from ethyl acetate fraction was characterized as isoorientin. The hexane fraction and its main isolated compound, the triterpene β-amyrin, exhibited significant growth inhibitory activity against Mycobacterium bovis BCG (MIC50 1.61 ± 1.43 and 3.93 ± 1.05 µg/ml, respectively). In addition, Passiflora mucronata samples, specially hexane and dichloromethane fractions, as well as pure β-amyrin, showed a dose-related inhibition of lipopolysaccharide (LPS)-induced nitric oxide production. In conclusion, Passiflora mucronata presented relevant biological potential and should be considered for further studies using in vivo pulmonary tuberculosis model.

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ABSTRACT Phytochemical investigation of Bauhinia acuruana Moric., Fabaceae, resulted in the isolation of sixteen constituents, including two new compounds 2'-hydroxy-2,3,5-trimethoxybibenzyl (1), (2R,3S)-2-(3,4'-dihydroxyphenyl)-5-methoxy-6-methylchroman-3,7-diol (2), together with fourteen known ones (3–16). The structures of the compounds were established by spectroscopic analysis including HR-ESI-MS, 1D and 2D NMR data, followed by comparison with previously reported data from the literature. Compounds 1, 2, 6, 7, 8 and 9 were evaluated for their cytotoxicity, which turned out to be marginal in a panel of six human cancer cell lines.

Resumo em Inglês:

ABSTRACT Canarium pimela K.D. Koenig, Burseraceae, have a long history of use in the Chinese traditional medicine treatment of various ailments including hypertension, and our research team has reported the anti-hypertensive activity and delineated the mechanism involved in the action. The following research aims to evaluate the vasorelaxant and antioxidant activities of ethanol extract from C. pimela leaves and to analyze its chemical composition by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS) that may correlate with their pharmacological activities. The results showed that pre-incubation of aortic rings with the extract (0.3, 1, 3, 10, 30 and 100 mg/l) significantly inhibited the contractile response of the rings to norepinephrine-induced contraction (p < 0.01or p < 0.05). Crude ethanol extract and refined ethanol extract showed a highest inhibitory effect against 2,2dipheyl-2-picrylhydrazyl hydrate scavenging activity (IC50 of crude ethanol extract = 15.42 ± 0.14 µg/ml and IC50 of refined ethanol extract = 5.72 ± 0.31 µg/ml) and 2,2′-azinobis (3-ethyl-benzothiazoline-6-sulphonic acid ammonium salt) (ABTS (IC50 of crude ethanol extract = 3.24 ± 0.18 µg/ml and IC50 of refined ethanol extract = 1.88 ± 0.07 µg/ml) scavenging activity, which was considerably higher than that reported for butylated hydroxytoluene and lower of that measured for ascorbic acid. Moreover, its chemical composition was analyzed by UPLC/Q-TOF-MS. Sixteen compounds including nine flavonoids, four tannins, two phenolic acids and one dianthrone were identified for the first time as constituents of this species. And of this, six major phenolic components were simultaneous quantitative analysis by HPLC-UV, chlorogenic acid is the major compounds in C. pimela leaves. These results indicate that the phenolic-rich extract of C. pimela leaves is a promising natural pharmaceutical for combating hypertension and oxidative stress.

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ABSTRACT Roccella montagnei Bél. belongs to lichen family Roccelleceae growing luxuriantly along the coastal regions of India. As Roccella has been shown to be bioactive, we prepared methanolic extract and assessed its anticancer potential. The methanolic extract showed significant in vitro cytotoxic activity against four human cancer cell lines such as colon (DLD-1, SW-620), breast (MCF-7), head and neck (FaDu). This prompted us to isolate bioactive compounds through column chromatography. Two compounds roccellic acid and everninic acid have been isolated, out of which everninic acid is reported for the first time. Both the compounds have been tested for in vitro cytotoxic activity in which roccellic acid showed strong anticancer activity as compared to the everninic acid. Cyclin Dependent Kinase (CDK-10) contributes to proliferation of cancer cells, and aberrant activity of these kinases has been reported in a wide variety of human cancers. These kinases therefore constitute biomarkers of proliferation and attractive pharmacological targets for development of anticancer therapeutics. Therefore both the isolated compounds were tested for in silico molecular docking study against Cyclin Dependent Kinase isomer enzyme to support the cytotoxic activity.

Resumo em Inglês:

ABSTRACT The metabolism of ethanol occurs mainly in the liver, promoting increase of reactive oxygen species and nitrogen, leading to redox imbalance. Therefore, antioxidants can be seen as an alternative to reestablish the oxidizing/reducing equilibrium. The aim of this study was to evaluate the antioxidant and hepatoprotective effect of aqueous extract of Baccharis trimera (Less.) DC., Asteraceae, in a model of hepatotoxicity induced by ethanol. The extract was characterized and in vitro tests were conducted in HepG2 cells. It was evaluated the cells viability exposed to aqueous extract for 24 h, ability to scavenging the radical DPPH, besides the production of reactive oxygen species and nitric oxide, and the influence on the transcriptional activity of transcription factor Nrf2 (12 and 24 h) after exposure to 200 mM ethanol. The results showed that aqueous extract was non-cytotoxic in any concentration tested; moreover, it was observed a decrease in ROS and NO production, also promoting the transcriptional activity of Nrf2. In vivo, we pretreatment male rats Fisher with 600 mg/kg of aqueous extract and 1 h later 5 ml/kg of absolute ethanol was administrated. After two days of treatment, the animals were euthanized and lipid profile, hepatic and renal functions, antioxidant status and oxidative damage were evaluated. The treatment with extract improved liver function and lipid profile, reflecting the reduction of lipid microvesicules in the liver. It also promoted an increase of glutathione peroxidase activity, decrease of oxidative damage and MMP-2 activity. These results, analyzed together, suggest the hepatoprotective effect of B. trimera aqueous extract.

Resumo em Inglês:

ABSTRACT A new C-glycosylflavone, apigenin 7-methyl ether 6-C-[β-xylopyranosyl-(1→3)-β-glucopyranoside] named distemonanthoside was isolated from the stem bark of Distemonanthus benthamianus Baill., Fabaceae, along with six known compounds, sitosterol 3-O-β-D-glucopyranoside, 4-methoxygallic acid, syringic acid, quercetin, 6"-O-acetylvitexin, quercetin 3-O-β-D-glucopyranoside. The structures of those compounds and others were determined through spectral analyses. Compounds distemonanthoside, sitosterol 3-O-β-D-glucopyranoside, 4-methoxygallic acid and quercetin were tested against a clinical isolate strain of Mycobacterium tuberculosis AC 45; they exhibited good to moderate antitubercular activities with MIC values ranged from 31.25 to 125 µg/ml.

Resumo em Inglês:

ABSTRACT Type 2 diabetes is a major health problem in Mexico, as it is in other countries, is a chronic condition that develops when the body cannot produce enough insulin or cannot use it appropriately. Both insulin deficiency and insulin resistance lead to high blood glucose levels. In Mexico, people with diabetes are known to use the decoction of red mangrove (Rhizophora mangle L., Rhizophoraceae) bark to control blood glucose levels. Therefore, in this study, we sought to investigate the chronic hypoglycemic and hypolipidemic effects of R. mangle; we also elucidate some of the major phytochemical compounds of R. mangle. To analyze the hypoglycemic and hypolipidemic effects, we used rats with streptozotocin–nicotinamide-induced hyperglycemia; the rats were classified into four groups (six rats each), based on the treatment given, as follows: group 1, non-hyperglycemic control; group 2, hyperglycemic control; group 3, glibenclamide (5 mg/kg body weight); and group 4, Rhizophora ethanol–water extract (90 mg/kg). The extract or glibenclamide was orally administered, dissolved in 1.5 ml of physiological NaCl-solution, twice a day (in the morning and in the evening) over a period of 42 days. The methanolic extract was used to elucidate the main compounds present in R. mangle via conventional phytochemical methods, such as TLC, HLPC, UPLC–DAD–MS, and NMR. The following compounds were detected: cinchonains Ia and Ib, catechin-3-O-rhamnopyranoside, epicatechin, lyoniside, and nudiposide. The daily administration of Rhizophora ethanol–water extract, similar to the traditional usage to control type 2 diabetes, was shown to exert chronic hypoglycemic and hypolipidemic effects. This effect may be associated whit the constituents in the extract. These findings suggest that R. mangle and its constituents could be potentially used to treat type 2 diabetes.

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ABSTRACT This is the first ethnobotanical exploration with the aim to document the traditional medicinal usage of plants with the therapeutic values in Tehsil Talagang of Punjab province, Pakistan. The study shows the dependence of local people on medicinal plants in their daily life and provides practical evidence regarding the traditional usage of medicinal plants in health care practices. A total of 196 respondents including residents of the study area with gender representation and traditional healers were interviewed by using visual appraisal approach and rapid rural appraisal methods along semi-structured interviews and open-ended questionnaire. The data was quantitatively analyzed by using quantitative indices like use value, the relative frequency of citation, informant consensus factor, fidelity level and relative importance. A comparison with 25 published ethnobotanical and pharmacological studies was carried out to authenticate the ethnomedicinal relevance of the data recorded. The ethnomedicinal practices of 101 medicinal plants belonging to 36 families were reported. The results indicated that the dominant family was Brassicaceae (nine species). Herbs (57%) were the most dominant life form and leaves (29%) were the frequently used plant part with 45 reports. Mentha arvensis was found as highly cited plant species by respondents. The highest informant consensus factor value (0.65) was found for gastrointestinal disease category. There are 25 plant species having 100% fidelity level value. Use value and relative frequency of citation ranges from 0.04 to 0.16 and 0.15 to 0.36, respectively. The majority of the plant species were found to have strong pharmacological evidence. The current study will provide the basis for the preservation of ethnomedicinal heritage, knowledge and practices as well as for the further scientific investigations regarding the development of new herbal drugs.

Resumo em Inglês:

ABSTRACT Our previous work revealed that chrysosplenetin in combination with artemisinin inhibited in vivo P-glycoprotein (P-gp, one of classic multi-drug resistance proteins) mediated digoxin transportation activity by reversing the upregulated P-gp/Mdr1 mRNA expression levels by artemisinin. Therefore, chrysosplenetin might be a potential artemisinin-resistance reversal agent as a P-gp inhibitor. But it still remains unknown if chrysosplenetin has an impact on another pivotal multi-drug resistance protein, breast cancer resistance protein (Bcrp), which is co-expressed with P-gp in apical membrane of intestinal epithelial cell and overlaps some of the substrates and inhibitors. This study, therefore, further addressed the impact of chrysosplenetin, per se or in combination with artemisin, on Bcrp/ABCG2 mRNA expression levels in mice small intestine determined by western blot and real time-quantitative polymerase chain reaction (RT-qPCR) assay. The drugs were intragastrically administrated once per day for 7 days. Novobiocin, a known Bcrp inhibitor, was observed to have no impact on Bcrp/ABCG2 levels with or without artemisinin versus vehicle. Interestingly, artemisinin alone attenuated Bcrp level while chrysosplenetin alone increased it (p < 0.05). Relative mRNA level was significantly decreased when co-used with artemisinin and chrysosplenetin in ratio of 1:2 (p < 0.05). The discrepant results for chrysosplenetin on Bcrp/ABCG2 mRNA expressions might be closely related to the transcriptional or posttranscriptional regulation.

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ABSTRACT The present study describes the impact of chrysosplenetin, in the absence and presence of artemisinin, on in vitro breast cancer resistance protein-mediated transport activity in Caco-2 cell monolayers using aristolochic acid I as a specific probe substrate. We observed that novobiocin, a known breast cancer resistance protein active inhibitor, increased Papp (AP-BL) of aristolochic acid I 3.13 fold (p < 0.05) but had no effect on Papp (BL-AP). Efflux ratio (PBA/PAB) declined 4.44 fold (p < 0.05). Novobiocin, consequently, showed a direct facilitation on the uptake of AAI instead of its excretion. Oppositely, both artemisinin and chrysosplenetin alone at dose of 10 µM significantly decreased Papp (BL-AP) instead of Papp (AP-BL). Chrysosplenetin alone attenuated the efflux ratio, which was suggestive of being as a potential breast cancer resistance protein suppressant. Oddly, Papp (BL-AP) as well as efflux ratio were respectively enhanced 2.52 and 2.58 fold (p < 0.05), when co-used with artemisinin and chrysosplenetin in ratio of 1:2. The potential reason remains unclear; it might be relative to binding sites competition between artemisinin and chrysosplenetin or the homodimer/oligomer formation of breast cancer resistance protein bridged by disulfide bonds, leading to an altered in vitro breast cancer resistance protein-mediated efflux transport function.

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ABSTRACT Chemical investigation of the leaves of Casearia gossypiosperma Briq., Salicaceae, led to the isolation of two known flavonoids, (+)-taxifolin and quercetin, the leaves of Casearia decandra Jacq. have afforded hydroquinone, the leaves of Casearia rupestris Eichler and Casearia lasiophylla Eichler have afforded a diterpene, (E)-phytol, and the leaves of C. rupestris and Casearia obliqua Spreng. have afforded sitosterol. The twigs of Casearia lasiophylla Eichler led to the isolation of two compounds (+)-pinoresinol, and N-trans-feruloyltyramine, and the twigs of C. obliqua have afforded N-trans-feruloyltyramine, N-trans-cumaroyltyramine, and cinamic acid. This is the first report of the compounds (+)-taxifolin, quercetin, hydroquinone, (+)-pinoresinol and N-trans-cumaroyltyramine from the Casearia genus.

Resumo em Inglês:

ABSTRACT In order to compile the empirical use, as well as the chemical, pharmacological and biological aspects of Himatanthus drasticus (Mart.) Plumel, Apocynaceae, a review was carried out by searching PubMed, Google Scholar, Scientific Electronic Online Library, Web of Science, Science Direct, Scopus and Cochrane. For that, works in English, Spanish and Portuguese, preclinical studies and revisions, addressing chemical, pharmacological, biological properties and popular uses, from 1994 to 2017, were used. The therapeutic potential of the “milk-of-janaguba” (a mixture of the latex with water) became widely known for the treatment of neoplasias, mainly lung and lymphatic cancer types, in the 1970s. The available literature presents works related to the anti-inflammatory, antinociceptive, antitumor and gastroprotective properties of the latex from bark and leaves of H. drasticus. In addition, this review presents some of our own results with the triterpene-rich fraction from H. drasticus, attempting to clarify its action mechanisms at the molecular level. The antinociceptive and anti-inflammatory activities of H. drasticus are probably associated with inhibitions of inflammatory mediators, as TNF-alpha, iNOS, COX-2 and NF-kB. Most importantly, a triterpene-rich fraction also inhibited HDAC activity, and compounds with this activity have been considered as therapeutic agents with antitumor activity. In conclusion, although the literature shows several works on species of the Himatanthus genus, including H. drasticus, dealing with some bioactive compounds as triterpenes, translational studies focusing upon the clinical uses of this medicinal species are still in great need.

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ABSTRACT Justicia pectoralis Jacq., Acanthaceae, is a medicinal plant found Central America. In the Northeast of Brazil, it is popularly known as “chambá” being extensively used in homemade preparations for the treatment of cough, bronchitis and asthma. The species is part of a public phytotherapy program in Brazil entitled “Farmácias Vivas”, National Record of Plants of Interest to the National Health System and the National Formulary of Herbal medicines. This paper aims to critically review the available scientific literature regarding the health promoting effects of J. pectoralis var. stenophylla. The traditional uses, phytochemistry, pharmacological activities, toxicology, quality control and potential interactions with conventional drugs were included in the present review. Botanical, chemical and pharmacognostical studies stablished several parameters useful for quality control of plant drug, extracts and phytomedicine from aerial parts of J. pectoralis using as markers two bioactive coumarins. A wide range of evidence have demonstrated the anti-inflammatory, anti-nociceptive, anti-spasmodic, smooth muscle relaxant and anxiolytic effects of J. pectoralis and its chemical constituents. Pilot clinical studies showed the efficacy of a syrup preparation of J. pectoralis in the treatment of mild and moderate asthma. The pharmacological potential make these medicinal plants good candidates for the development of new phytomedicine for the treatment of asthma. However, a strong collaboration to bridge the gap between preclinical and clinical study is still necessary for the development of an effective medicine from J. pectoralis.