In Vitro Schistosomicidal Activity of Phytol and Tegumental Alterations Induced in Juvenile and Adult Stages of Schistosoma haematobium

There is renewed interest in natural products as a starting point for discovery of drugs for schistosomiasis. Recent studies have shown that phytol reveals interesting in vivo and in vitro antischistosomal properties against Schistosoma mansoni adult worms. Here, we report the in vitro antischistosomal activity of phytol against Schistosoma haematobium juvenile and adult worms and alterations on the tegumental surface of the worms by means of scanning electron microscopy. The assay, which was carried out with 6 concentrations (25, 50, 75, 100, 125, and 150 μg/ml) of phytol, has shown a promising activity in a dose and time-dependent manner. There was a significant decline in the motility of the worms and a mortality rate of 100% was found at 48 hr after they had been exposed to phytol in the concentration of 150 μg/ml. Male worms were more susceptible. On the ultrastructural level, phytol also induced tegumental peeling, disintegration of tubercles and spines in addition to morphological disfiguring of the oral and ventral suckers. This report provides the first evidence that phytol is able to kill S. haematobium of different ages, and emphasizes that it is a promising natural product that could be used for development of a new schistosomicidal agent.

Bioactive Constituents from the Leaves of Zanthoxylum schinifolium

Activity-guided separation of the methylene chloride-soluble fraction of the leaves of Zanthoxylum schinifolium, resulted in the isolation of four coumarinoids (1 - 4), two triterpenoids (5, 6) and three fatty acid derivatives (7 - 9) as active principles. Their chemical structures were identified as collinin (1), 8-methoxyanisocoumarin (2), 7-(6'R-hydroxy-3',7'-dimethylocta-2',7'-dienyloxy)-coumarin (3), (E)-4-methly-6-(coumarin-7'-yloxy) hex-4-enal (4), lupeol (5), epi-lupeol (6), phytol (7), hexadec-3-enoic acid (8) and palmitic acid (9), on the basis of spectroscopic (1D, 2D and MS) data analyses and comparing with the data published in the literatures. Compounds 1 and 7 showed potent cytotoxicity against Jurkat T cells with IC50 values of 45.58 and 47.51 microM, respectively. The others showed moderate activity with IC50 values ranging around 80.58 to 85.83 microM, while the positive control, auraptene, possessed an IC50 value of 55.36 microM.

Avaliação da toxicidade aguda e das alterações histopatológicas em camundongos tratados com fitol / Assessment of acute toxicity and histopathological changes in mice treated with phytol

O fitol, (3,7,11,15-tetrametilhexadec-2-en-1-ol), é um diterpeno pertencente ao grupo dos álcoois acíclicos insaturados de cadeia longa e ramificada. É um componente da molécula da clorofila, presente em folhas verdes de várias plantas medicinais. Entretanto, pouco é descrito na literatura sobre os possíveis efeitos toxicológicos produzidos pelo fitol. O objetivo do nosso estudo foi avaliar a toxicidade aguda do fitol, após administração intraperitoneal para determinação da dose letal 50% (DL50) e os efeitos sobre os parâmetros bioquímicos, hematológicos e histopatológicos no hipocampo e corpo estriado de camundongos adultos tratados com fitol nas doses de 25, 50 e 75 mg/kg. Os testes para determinação do grau de toxicidade aguda, bem como a investigação da DL50, revelou que o valor é aproximadamente 1153.39 mg/kg. Os camundongos tratados com as doses selecionadas do fitol a partir da DL50 apresentaram todos os parâmetros hematológicos dentro da faixa de referência, observando-se alterações nos valores dos linfócitos. Por sua vez, a maioria dos valores dos parâmetros bioquímicos diminuiu em todas as doses testadas (p<0,05). Em nosso estudo, apenas os animais tratados com fitol na dose de 75 mg/kg demonstraram uma discreta vacuolização no corpo estriado e um discreto comprometimento caracterizado por vacuolização no hipocampo em apenas um dos animais. Nossos resultados indicam que o tratamento com fitol não produz alterações hematológicas, bioquímicas e histopatológicas cerebrais em camundongos. O estudo toxicológico pré-clínico com fitol demonstrou que o produto avaliado possui discreta toxicidade aguda por via intraperitoneal, sendo estes dados uma contribuição para pesquisas com compostos obtidos de plantas medicinais com potencial farmacológico. Porém, ressalta-se a necessidade de futuras pesquisas que possibilitem comparar os resultados em outras vias, bem como para realizar análises anatomopatológicas dos animais tratados com fitol, para assegurar o uso seguro deste diterpeno.

Phytol (3,7,11,15-tetramethylhexadec-2-en-1-ol) is a diterpene belonging to the group of acyclic unsaturated long-chain branched alcohols. It is a component of the chlorophyll molecule, present in green leaves of various medicinal plants. However, there is little in the literature about the possible toxic effects produced by phytol. The aim of our study was to assess the acute toxicity of phytol after intraperitoneal (ip) administration, by determining its 50% lethal dose (LD50) and effects on biochemical parameters, hematology and the histopathology of the hippocampus and corpus striatum of adult mice treated with doses of 25, 50 and 75 mg/kg phytol. The acute toxicity tests and investigation of the LD50 revealed its value to be approximately 1153.39 mg/kg. Mice treated with sublethal doses of phytol based on the LD50 showed all hematological parameters within their reference ranges, with small changes in the lymphocyte count. In turn, most of the biochemical parameters decreased at all doses tested (p<0.05). In our study, only those animals treated with phytol at a dose of 75 mg/kg showed slight vacuolation in the corpus striatum and a slight impairment characterized by vacuolation in the hippocampus in one animal. Our results indicate that treatment with phytol produces no hematological, biochemical or brain histopathological changes in the mice. The preclinical toxicological study with phytol showed that it has slight acute toxicity when injected ip. These data contribute to research on natural compounds obtained from medicinal plants with pharmacological potential. However, we emphasize the need for future research to enable results obtained by other routes to be compared, as well as to conduct pathological analysis in animals treated with phytol, to ensure the safe use of this diterpene.

Studies on chemical constituents of Laurencia tristicha ( II ) / 中国中药杂志

<p><b>OBJECTIVE</b>To search for chemical constituents with structural diversity from Laurencia tristicha to supply for biological assay.</p><p><b>METHOD</b>Compounds were isolated by means of column chromatography over normal phase silica gel and Sephadex LH-20, recrystallization and HPLC. Structures were identified by spectroscopic methods including 1D NMR, IR and MS. Cytotoxicities of the purified compounds were evaluated by MTT method.</p><p><b>RESULT</b>Seven compounds were isolated from L. tristicha. Their structures were elucidated as cholesterol (1), cholesta- 5-en-3beta, 7alpha-diol (2), beta-stigmasterol (3), phytol (4), zeaxanthin (5), 4 -hydroxybenzaldehyde (6), indolyl-3-carbaldehyde (7). In the cytotoxic assay compound 2 was active against human cancer cell lines HCT-8, Bel-7402, BGc-823, A549 and HELA with IC50 values of 1.90, 2.02, 1.99, 6.52 and 1.20 microg x mL(-1), respectively. Compound 4 showed cytotoxicity against HCT-8 and HELA with IC50 value of 3.51 and 2.04 microg x mL(-1), and other compounds were inactive ( IC50 > 10 microg x mL(-1)).</p><p><b>CONCLUSION</b>Compounds 1-7 were isolated from L. tristicha for the first time. In additon, compounds 2 and 4 were cytotoxic against several human cancer cell lines.</p>

Chemical constituents from red alga Corallina pilulifera / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents of red alga Corallina pilulifera.</p><p><b>METHOD</b>Compounds were isolated by normal phase silica gel and Sephadex LH - 20 gel column chromatography, reverse phase HPLC and recrystallization. Their structures were elucidated by spectroscopic methods including MS, 1H-NMR, 13C-NMR, HSQC, HMBC. Cytotoxicity of the compounds was screened by using standard MTT method.</p><p><b>RESULT</b>Seven compounds were isolated from red alga C. pilulifera, their structures were identified as (E) -phytol epoxide (1), phytenal (2), phytol (3), dehydrovomifoliol (4), loliolide (5), 3beta-hydroxy-5alpha, 6alpha-epoxy-7-megastigmene-9-one (6), 4-hydroxybenzaldehyde (7).</p><p><b>CONCLUSION</b>All of the compounds were obtained from this species for the first time. These compounds were inactive (IC50 > 10 microg x mL(-1)) in the MTT assay.</p>

Chemical constituents from herb of Alternanthera philoxeroides / 中国中药杂志

<p><b>OBJECTIVE</b>To study the active constituents from Alternanthera philoxeroides.</p><p><b>METHOD</b>The constituents were isolated with silica gel and Toyopearl HW-40C gel column chromatography and purified by HPLC. Their structures were elucidated by spectroscopy.</p><p><b>RESULT</b>Nine compounds were isolated and identified as phaeophytin a (1), pheophytin a' (2), oleanoic acid (3), beta-sitosterol (4), 3beta-hydroxystigmast-5-en-7-one (5), alpha-spinasterol (6), 24-methylenecycloartanol (7), cycloeucalenol (8), phytol (9).</p><p><b>CONCLUSION</b>Compounds 1,2,5,7-9 were isolated from this plant for the first time.</p>

Study on the chemical constituents of the volatile oil from aerial parts of Isodon eriocalyx var. laxiflora / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of the volatile oil from the aerial parts of Isodon eriocalyx var. laxiflora.</p><p><b>METHOD</b>The oil was obtained by hydrodistillation. The chemical compositions were separated and identified by GC-MS. The relative contents in the oil were determined by area normalization.</p><p><b>RESULT</b>163 peaks were separated and 105 compounds were identified, constituting 85.68% of the total peak area.</p><p><b>CONCLUSION</b>105 compounds characterized by GC-MS analysis were found from I. eriocalyx var. laxiflora for the first time.</p>

Chemical components in essential oils from tender branches and leaves of Rhododendron / 药学学报

<p><b>AIM</b>To analyze and compare the compositions in essential oils from branches and leaves of Rhododendron simsii Planch. and Rhododendron naamkwanense Merr.</p><p><b>METHODS</b>Essential oils were extracted by water distillation according to Chinese Pharmacopoeia and analyzed by capillary gas chromatography-mass spectrometry as well as chemometrics resolution method and authentic compounds. The relative contents of each component in the essential oils were obtained by normalization of peak areas.</p><p><b>RESULTS</b>A total of 124 components were identified, of which 48 compounds were existed in both of the samples. Ninety four compounds accounted for 84.47% of the essential oil from Rhododendron simsii Planch. and seventy eight components accounted for 90.25% of the total essential oil from Rhododendron naamkwanense Merr. were identified. 72.76% and 88.07% of the components in Rhododendron simsii Planch and Rhododendron naamkwanense Merr., respectively, included oxygen element. They are mainly terpenol, acids and esters. 1-octen-3-ol (4.00%, 7.90%), 1,6-octadien-3-ol, 3,7-dimethyl-(12.60%, 3.48%), 9,12,15-octadecatrienoic acid, [Z, Z, Z]- (1.15%, 45.34%), phytol (15.21%, 8.56%), p-menth-1-en-8-ol (2.15%, 3.29%), and 9,12,15-octadecatrienoic acid, ethyl ester, [Z,Z,Z]- (9.16%, 8.01%) were their common main compounds, which accounted for 44. 27% and 76.58% of the total amount of the two essential oil samples, respectively. In addition, n-hexadecanoic acid (7.73%), 9,12-octadecadienoic acid (1.85%) and tetracosanoic acid, methyl ester (1.38%) were also the main compounds in essential oil from Rhododendron simsii Planch.</p><p><b>CONCLUSION</b>Much higher reliability and accuracy were obtained with the help of chemometrics resolution method and authentic n-alkane standard solutions than those of using GC-MS alone.</p>

O papel da clorofila na alimentação humana: uma revisão / The role of chlorophyll in human feeding: a review

Os eventuais efeitos benéficos da clorofila, presente em alimentos, suscitam polêmica e dúvidas entre os consumidores. As informações divulgadas nos meios de comunicação que atribuem à molécula da clorofila numerosos efeitos terapêuticos, quase miraculosos, se contrapõem à falta de aprovação dessas atribuições pela comunidade científica. Tornar disponíveis os resultados das pesquisas mais recentes sobre o assunto e analisar criticamente esses dados foi o objetivo desta revisão. São discutidos os mecanismos de degradação da clorofila durante a senescência, armazenamento e processamento de vegetais, bem como no processo digestivo, considerando que os produtos de degradação podem diferir em cada caso...