Optimization of parameters for stir-frying of Kansui Radix with vinegar based on conversion of toxic components / 中国中药杂志

This study aims to optimize the parameters for stir-frying of Kansui Radix with vinegar based on the conversion of representative toxic diterpenes, which is expected to serve as a reference for the standardized production of Kansui Radix stir-fried with vinegar. To be specific, the toxic components [3-O-(2'E,4'Z-decadienoyl)-20-O-acetylingenol(3-O-EZ), kansuiphorin C(KPC)] in Kansui Radix and the products(ingenol, 20-deoxyingenol) after the stir-frying with vinegar were selected. The toxicity to intestine and water-draining activity were evaluated with NCM460(normal human colon mucosal epithelial cell line) and HT-29(a human colorectal adenocarcinoma cell line). An HPLC method was then developed to assess the conversion of toxic components. On this basis, temperature, time, and amount of vinegar for the processing of Kansui Radix were optimized with the Box-Behnken design and the content of ingenol and 20-deoxyingenol as evaluation index. The results showed that after the stir-frying of Kansui Radix with vinegar, 3-O-EZ and KPC were first converted to monoester 3-O-(2'E,4'Z-decadienoyl)ingenol(3-EZ) and 5-O-benzoyl-20-deoxyingenol(5-O-Ben) and finally to almost non-toxic ingenol and 20-deoxyingenol, respectively. Meanwhile, the water-draining activity was retained. Six compounds had a good linear relationship with the peak area in the corresponding concentration ranges(R~2≥0.999 8), and the average recovery fell in the range of 98.20%-102.3%(RSD≤2.4%). The content of representative diterpenes and intermediate products was 14.78%-24.67% lower in the Kansui Radix stir-fried with vinegar than in the Kansui Radix, while the content of the conversed products was 14.37%-71.37% higher. Among the process parameters, temperature had significant influence on the total content of products, followed by time. The optimal parameters were 210 ℃, 15 min, and 30% vinegar. The relative error between the experimental results and the predicted values was 1.68%, indicating that the process was stable and reproducible. The strategy of screening optimal parameters for stir-frying of Kansui Radix with vinegar based on the transformation of toxic components can help improve the production stability, reduce the toxicity, and ensure the efficacy of Kansui Radix stir-fried with vinegar, which can serve as a reference for the process optimization of similar toxic Chinese medicinals.

Effect of different herbicides on Bidens pilosa and Euphorbia heterophylla biotypes resistant to ALS inhibitors

Select herbicides with different mechanism of action is a satisfactory option for resistant weed control. Then, the present work aimed to study the efficiency of different herbicides and their mixtures on Bidens pilosa (blackjack) and Euphorbia heterophylla (wild poinsettia) biotypes, resistant to ALS herbicides in two development stages. The trials we arranged in a completely randomized design with four replications. The treatments tested were (g a.i/a.e ha-1): imazethapyr at 70 and 140 (WG formulation) + 1.0% Assist; imazethapyr at 57.6 and 72 (SL formulation) + 1.0% Assist; imazapic + imazethapyr at 56 and 70 + 1.0% Assist; glyphosate + imazethapyr (596); saflufenacil + glyphosate at 35 + 720 + 0.5% Dash in tank mix, glyphosate at 720 and, a control without herbicide application. Control efficiency was evaluated, as well as dry matter accumulation at the end of the studies. Plants of both species were more susceptible to herbicides at the early stage of development (2 to 4 leaves). The treatments with saflufenacil + glyphosate, (imazethapyr + glyphosate) and glyphosate promoted the best controls, regardless of the species studied and the application stage. The mixture with saflufenacil provided the highest control speed, and the mixture (imazethapyr + glyphosate) was less efficient among three excellent treatments when applied to plants in the 4-6 leaf stage. The treatments (imazethapyr, in both formulations) and (imazethapyr + imazapic) were ineffective in controlling the studied biotypes, regardless of dose and developmental stage studied.

Effect of Kansui Radix stir-fried with vinegar on fecal metabolomics in Walker-256 rats with ascites / 中国中药杂志

Utilizing metabolomics technology, this study explored the change of fecal endogenous metabolites in Walker-256 rats with malignant ascites after the administration with Kansui Radix(KR) stir-fried with vinegar(VKR), sought the potential biomarkers in feces which were related to the treatment of malignant ascites by VKR and revealed the biological mechanism of water-expelling effect of VKR. Ultra-fast liquid chromatography-quadrupole-time-of-flight mass spectrometry(UFLC-Q-TOF-MS) was employed to detect the feces of rats in all groups. Principle component analysis(PCA) and partial least squares discriminant analysis(PLS-DA) were conducted to achieve pattern recognition. Combining t-test and variable importance in the projection(VIP) enabled the screening of potential biomarkers for the malignant ascites. Metabolic pathway analysis was accomplished with MetaboAnalyst. Correlation analysis was finally conducted integrating the sequencing data of gut microbiota to elucidate the mechanism underlying the water-expelling effect of VKR. The results showed that both KR and VKR could restore the abnormal metabolism of model rats to some extent, with VKR being inferior to KR in the regulation. Eleven potential biomarkers were identified to be correlated with the malignant ascites and five metabolic pathways were then enriched. Four kinds of gut microbiota were significantly related to the potential biomarkers. The water-expelling effect of VKR may be associated with the regulation of phenylalanine metabolism, biosynthesis of phenylalanine, tyrosine and tryptophan, tryptophan metabolism, glycerophospholipid metabolism, and glycosylphosphatidylinositol(GPI)-anchor biosynthesis. This study can provide a scientific basis for comprehensive understandings of the interaction between gut microbiota and host which has relation to the water-expelling effect of VKR and guide the reasonable clinical application of VKR.

Chemical ingredient groups B and C in Kansui Radix stir-fried with vinegar affect diversity of gut microbiota in rat model of malignant ascites induced by Walker-256 cells / 中国中药杂志

This study aims to explore the effects of chemical ingredient groups B and C in Kansui Radix stir-fried with vinegar on the diversity of gut microbiota in the rat model of malignant ascites, identify the key differential microbial taxa, and reveal the biological mechanism of water-expelling effect of the two chemical ingredient groups. The rat model of malignant ascites induced by Walker-256 cells was established, and phenolphthalein was used as the positive drug. The rats were orally administrated with corresponding agents for consecutive 7 days. On day 6, fresh feces samples were collected from the rats, and 16 S rDNA high-throughput sequencing and GC-MS were employed to determine the composition of gut microbiota and the content of short-chain fatty acids, respectively. On day 7, serum and intestinal tissue samples were collected for the determination of related indicators. Compared with the control group, the model group showed decreased feces volume and urine volume(P<0.01), increased volume of ascites and levels of Na~+, K~+, and Cl~- in urine(P<0.01), down-regulated mRNA and protein levels of intestinal AQP8(P<0.01), lowered abundance of beneficial Lactobacillus(P<0.01) while risen abundance of potential pathogenic Lachnospiraceae and Anaeroplasma(P<0.01), and reduced content of short-chain fatty acids(P<0.01). Compared with the model group, administration with chemical ingredient groups B and C alleviated all the above indicators(P<0.01). In conclusion, chemical ingredient groups B and C in Kansui Radix stir-fried with vinegar could alleviate the disordered gut microbiota in rats with malignant ascites to expel water through increasing the abundance of beneficial Lactobacillus and reducing the abundance of harmful Lachnospiraceae and Anaeroplasma. This study can provide a reference for the reasonable clinical application of Kansui Radix stir-fried with vinegar.

Structural elucidation, mechanism of action, antibacterial proficiency and synergistic forte of purified Euphorbia hirta whole plant extract against multi-drug resistant otitis media infection / Elucidación estructural, mecanismo de acción, competencia antibacteriana y fuerza sinérgica del extracto de planta entera de Euphorbia hirta purificado contra la infección por otitis media resistente a múltiples fármacos

This study investigated the antibacterial potential of Euphorbia hirtawhole plant extracts, honey and conventional antibiotics and their synergistic effects against selected multidrug resistant and typed bacterial strains associated with otitis media. E. hirtawhole plant extract was purified using column chromatography technique. The antibacterial assays of extracts were done using standard microbiological procedures. Protein, sodium and potassium ion leakage of the synergistic mixtures was determined using flame-photometry. At 100 mg/ml, acetone extracts presented highest inhibition against S. aureus (NCTC 6571) with 32 ± 0.83 mm zone of inhibition. The fractional inhibitory concentration indices displayed higher synergism in combination of plant extract, honey and ciprofloxacin against P. mirabilisat 0.02 compared to drug combination synergy standard (≤ 0.5). This work revealed augmentation of ciprofloxacin potency when combined with purified E. hirta acetone extract and honey and implies their high potential in the treatment of multidrug resistant infectionof otitis media.

Este estudio investigó el potencial antibacteriano de extractos de plantas enteras de Euphorbia hirta, miel y antibióticos convencionales y sus efectos sinérgicos contra cepas bacterianas seleccionadas multirresistentes y tipificadas asociadas con la otitis media. El extracto de la planta entera de E. hirtase purificó usando la técnica de cromatografía en columna. Los ensayos antibacterianos de extractos se realizaron utilizando procedimientos microbiológicos estándar. La fuga de iones de proteínas, sodio y potasio de las mezclas sinérgicas se determinó mediante fotometría de llama. A 100 mg/ml, los extractos de acetona presentaron la mayor inhibición contra S. aureus (NCTC 6571) con una zona de inhibición de 32 ± 0,83 mm. Los índices de concentración inhibitoria fraccional mostraron un mayor sinergismo en combinación de extracto de planta, miel y ciprofloxacina contra P. mirabilisa 0,02 en comparación con el estándar de sinergia de combinación de fármacos (≤ 0,5). Este trabajo reveló un aumento de la potencia de la ciprofloxacina cuando se combina con extracto de acetona purificado de E. hirtay miel e implica sualto potencial en el tratamiento de infecciones de otitis media resistentes a múltiples fármacos.

Large-scale advances in SSR markers with high-throughput sequencing in Euphorbia fischeriana Steud

BACKGROUND: Euphorbia fischeriana Steud is a very important medicinal herb and has significant medical value for healing cancer, edema and tuberculosis in China. The lack of molecular markers for Euphorbia fischeriana Steud is a dominant barrier to genetic research. For the purpose of developing many simple sequence repeat (SSR) molecular markers, we completed transcriptome analysis with the Illumina HiSeq 2000 platform. RESULTS: Approximately 9.1 million clean reads were acquired and then assembled into approximately 186.3 thousand nonredundant unigenes, 53,146 of which were SSR-containing unigenes. A total of 76,193 SSR loci were identified. Of these SSR loci, 28,491 were detected at the terminal position of ESTs, which made it difficult to design SSR primers for these SSR-containing sequences, and the residual SSRs were thus used to design primer pairs. Analyzing the results of these markers revealed that the mononucleotide motif A/T (44,067, 57.83% of all SSRs) was the most abundant, followed by the dinucleotide type AG/CT (9430, 12.38%). Using 100 randomly selected primer pairs, 77 primers were successfully amplified in Euphorbia fischeriana Steud, and 79 were successfully amplified in three other related species. The markers developed displayed relatively high quality and cross-species transferability. CONCLUSIONS: The large number of EST-SSRs exploited successfully in Euphorbia fischeriana Steud for the first time could provide genetic information for research on linkage maps, variety identification, genetic diversity analysis, and molecular marker-assisted breeding.

Keratouveitis caused by Euphorbia milii sap: case report and overview / Ceratouveíte causada pela seiva de Euphorbia millii: relato de caso e visão geral

ABSTRACT Objective: To report a case of anterior uveitis caused by Euphorbia milii sap and review all reported cases of keratouveitis related to this species. Methods: A 64-year-old male patient presented with a 10-day history of reduced visual acuity, pain, and photophobia in the left eye after an accidental contact with Euphorbia milii sap. Best-corrected visual acuity was initially 20/200. Upon examination, ciliary injection, mild corneal edema; fine keratic precipitates, and significant anterior chamber reaction. There was no vitritis, and fundoscopy was unremarkable. The patient initiated on topical steroid and tropicamide. Results: Best-corrected visual acuity in left eye improved to 20/20 after using eyedrops for 3 weeks, associated with complete resolution of anterior uveitis. Over the following 6 months, best-corrected visual acuity remained stable, and no evidence of recurrent inflammation was observed. Conclusion: To the best of our knowledge, this is the third reported case of keratouveitis caused by Euphorbia milii sap. As observed in other cases of keratouveitis caused by sap of this species, the clinical course is benign and characterized by moderate reaction of the anterior chamber, and corneal involvement of variable intensity.

RESUMO O objetivo foi relatar um caso de uveíte anterior induzida pela seiva da Euphorbia milii e revisar todos os casos relatados de ceratouveíte causados por essa espécie. Paciente do sexo masculino, 64 anos, apresentou história de 10 dias de evolução com redução da acuidade visual, dor e fotofobia no olho esquerdo, após contato acidental com a seiva da planta Euphorbia milii. A acuidade visual com melhor correção era inicialmente 20/200. O exame revelou injeção ciliar, edema de córnea leve, precipitados ceráticos finos e reação de câmara anterior significativa. Não havia vitreíte, e a fundoscopia não exibia alterações. Foram iniciados colírios de esteroides e tropicamida. A acuidade visual no olho esquerdo melhorou para 20/20 em 3 semanas com a utilização dos colírios, além de se ter alcançado a resolução completa da uveíte anterior. Nos 6 meses seguintes, a acuidade visual permaneceu estável, e não foi observada evidência de recorrência da inflamação. Até então, este é o terceiro caso relatado de ceratouveíte pela seiva da Euphorbia milii. Como visto nos demais casos de ceratouveíte induzidos pela seiva dessa espécie, o curso clínico é benigno e caracterizado por reação moderada da câmara anterior, com envolvimento corneano de intensidade variável.

Four new lanostane triterpenoids from latex of Euphorbia resinifera / 中国中药杂志

Four new lanostane triterpenoids, 3β-hydroxy-12α-methoxylanosta-7,9(11),24-triene(1), 3β-hydroxy-12α-methoxy-24-methylene-lanost-7,9(11)-dien(2), 3,7-dioxo-lanosta-8,24-diene(3), and 3,7-dioxo-24-methylene-lanost-8-en(4), were isolated from the latex of Euphorbia resinifera with a variety of chromatography methods. Their structures were elucidated based on spectroscopic data and/or comparison with the data reported in previous research. Compounds 1, 2, and 4 showed moderate inhibition of LPS-induced NO production by RAW264.7, with IC_(50) of 30.4, 37.5, and 28.3 μmol·L~(-1), respectively.

Chemical constituents of triterpenoids from Euphorbia resinifera / 中国中药杂志

The combination of normal-phase silica gel column chromatography, octadecyl silica(ODS) column chromatography, semi-preparative high performance liquid chromatography(HPLC), etc. was employed to isolate and purify the chemical components from Euphorbia resinifera, and 7 triterpenoids were separated from the ethanol extract of the medicinal materials. Their structures were identified by various spectroscopy methods as cycloartan-1,24-diene-3-one(1), cycloartan-1,24-diene-3-ol(2), 3β-hydroxy-lanosta-8,24-diene-11-one(3), lnonotusane C(4), eupha-8,24-diene-3β-ol-7,11-dione(5), eupha-24-methylene-8-ene-3β-ol-7,11-dione(6), and eupha-8,24-diene-3β,11β-diol-7-one(7). Compounds 1 and 2 are new compounds, and compound 3 is obtained from nature for the first time.

In vitro antimicrobial activity of mexican plants on bovine mastitis bacteria: preliminary studies / Atividade antimicrobiana in vitro de plantas mexicanas sobre bactérias de mastite bovina: estudos preliminares

The present study aimed to evaluate the efficacy of traditionally used antibacterial plants (Euphorbia prostrata, Schinus molle, Brickellia veronicaefolia and Lepidium virginicum) in Santa Rosa Range in Guanajuato against major mastitis-causing pathogens. The selected plants were phytochemically screened for alkaloids, flavonoids, polyphenols, saponins, anthraquinone, cardiac glycosides, steroids and terpenoids. Moreover, to achieve the main purpose of the present research, extracts of selected plants were tested for in vitro antibacterial activity against Staphylococcus aureus, Escherichia coli, Shigella spp., Bacillus subtilis, Clavibacter spp., Proteus vulgaris and Salmonella spp. All these bacterial were isolated from clinical mastitis in dairy cows. The results indicated that the ethanolic extract of the aerial part of L. virginicum exhibited the strongest antimicrobial activity, and it could be potential candidate specie for the development of novel veterinary drugs with low cost and fewer side effects.

O presente estudo teve como objetivo investigar a eficácia de plantas antibacterianas tradicionalmente usadas (Euphorbia prostrata, Schinus molle, Brickellia veronicaefolia e Lepidium virginicum) na cordilheira Santa Rosa, em Guanajuato, contra os principais patógenos causadores de mastite. As plantas selecionadas foram rastreadas fitoquimicamente quanto a alcalóides, flavonóides, polifenóis, saponinas, antraquinona, glicosídeos cardíacos, esteróides e terpenóides. Além disso, para atingir o objetivo principal da presente pesquisa, extratos de plantas selecionadas foram testados quanto à atividade antibacteriana in vitrocontra Staphylococcus aureus, Escherichia coli, Shigella spp., Bacillus subtilis, Clavibacter spp., Proteus vulgaris e Salmonella spp. Todas essas bactérias foram isoladas de mastite clínica em vacas leiteiras. Os resultados indicaram que o extrato etanólico da parte aérea de L. virginicum exibia a atividade antimicrobiana mais forte e poderia ser uma espécie potencial candidata ao desenvolvimento de novos medicamentos veterinários com baixo custo e menos efeitos colaterais.

Study on chemical constituents from Euphorbia thymifolia / 中国中药杂志

This work was launched to study on the chemical constituents from Euphorbia thymifolia. Thirteen compounds were isolated from the 95% ethanol extract of the aerial parts of E. thymifolia by column chromatographies on silica gel, Sephadex LH-20, MCI, and ODS, and preparative HPLC, including two thymol derivatives(1-2), four alkaloids(3-6), five isocoumarins(7-11), together with two ellagic acids(12-13). All the compounds are listed as follows:(Z)-8,9-dehydro-9,10-diisobutyryloxythymol(1), 8-hydro-xy-9,10-diisobutyryloxythymol(2), N-(N-benzoyl-L-phenylalanyl)-L-phenylalanol(3), aurantiamide acetate(4), 1-carboethoxy-β-carboline(5), isoechinulin A(6), ethyl brevifolincarboxylate(7), euphorhirtin B(8), 4,5-didehydro chebulic acid triethyl ester(9), euphorhirtin G(10), pomegranatate(11), 3,3',4'-tri-O-methylellagic acid(12), 3,3'-di-O-methylellagic acid(13). Compound 1 is a new compound. Except for compound 4, the others were isolated from this plant for the first time. All the compounds were screened for anti-neuroinflammatory activity in vitro, and compounds 1-3 and 7 showed significant activity with IC_(50) values of 0.19,12.93,7.29,25.4 μmol·L~(-1).

Low level resistance of wild poinsettia biotypes to glyphosate and alternative chemical control / Resistência de nível baixo de biótipos de leiteira ao glyphosate e alternativas quimicas de controle

In the State of Rio Grande do Sul (RS), Southern Brazil, glyphosate has not been capable of controlling wild poinsettia (Euphorbia heterophylla L.) in soybean fields, thus, suggesting resistanceto this herbicide. Therefore, this study aimed at evaluating sensitivity of wild poinsettia biotypes to glyphosate, identifying the occurrence of resistance of wild poinsettia to the herbicide in RS state and determining the resistance factor of wild poinsettia biotypes under suspicion, besides assessing other herbicides as alternative controls. Two greenhouse experiments, which lasted two years, were conducted by a completely randomized design with four replications. Six biotypes (Factor A) and eight doses of glyphosate (Factor B) were used for getting the dose-response curve. Regarding the alternative control, post-emergence herbicides for soybean and corn crops were tested. Control and dry mass of the shoot were analyzed as variables. Resistance factors of resistant biotypes 20.2 and 21.1 were 4.83 and 5.29, respectively, by comparison with the susceptible biotype (11.4). In RS state, there has currently been high selection pressure due to the intensive use of glyphosate against wild poinsettia plants, as the result of the occurrence of biotypes 20.2 and 21.1 which have low levels of resistance to glyphosate and very little control by ALS-inhibiting herbicides. Therefore, an alternative to mitigate the problem is the use of herbicides with different mechanisms of action.

As falhas de controle de leiteira (Euphorbia heterophylla L.) após aplicação de glyphosate em lavouras de soja do Rio Grande do Sul (RS) são frequentes, sugerindo a resistência ao herbicida. Diante disso, os objetivos foram avaliar a sensibilidade de biótipos de leiteira ao herbicida glyphosate, identificar a ocorrência da resistência, determinar o fator de resistência de biótipos de leiteira com suspeita de resistência e avaliar herbicidas alternativos para o seu controle. Foram conduzidos dois experimentos em casa de vegetação, em delineamento inteiramente casualizado com quatro repetições ambos realizados em dois anos. No experimento de curva dose-resposta foram utilizados cinco biótipos (fator A) e oito doses do herbicidaglyphosate (fator B). Para o controle alternativo, foram testados herbicidas em pós emergência das culturas de soja e milho. As variáveis analisadas foram controle e massa seca da parte aérea. O fator de resistência dos biótipos resistentes (20.2 e 21.1) foram 4,83 e 5,29 comparativamente ao biótipo suscetível (11.4) respectivamente. Existe elevada pressão de seleção pelo glyphosate em plantas de leiteira no RS, observando-se a ocorrência de biótipos 20.2 e 21.1 com resistência de nível baixo ao herbicida e com controle reduzido pelos herbicidas inibidores de ALS. Portanto, uma alternativa para atenuar o problema é o uso de herbicidas com diferentes mecanismos de ação

Evaluación de la actividad antioxidante de Cnidoscolus chayamansa (Chaya), Euphorbia prostrata (Hierba de la Golondrina) y Jatropha dioica (Sangre de Drago) en ratas Wistar inducidas a hiperglicemia / Evaluation of the antioxidant activity of Cnidoscolus chayamansa (Chaya), Euphorbia prostrata (Herb of the Swallow) and Jatropha dioica (Drago blood) in Wistar rats induced to hyperglycemia

RESUMEN: Estudios recientes han demostrado que los compuestos activos presentes en extractos de C. chayamansa, E. prostrata y J. dioica tienen propiedades antioxidantes. Los resultados obtenidos en nuestro estudio fueron compuestos fenólicos solubles mostraron en C. chayamansa 6,34, E. prostrata 10,67, J. dioica 1,83 mg equiv de ácido gálico/gm BS respectivamente. Los antioxidantes solubles en agua por el método ABTS fueron para C. chayamansa 5.9, E. prostrata 12.7 y para J. dioica 2.5 mM equiv. de trolox/gr BS. Los resultados histopatológicos muestran una mejoría en los tejidos tratados con los extractos después de la inducción a hiperglicemia.

SUMMARY: Recent studies have shown that the active compounds present in extracts of C. chayamansa, E. prostrata and J. dioica have antioxidant properties. The results obtained in our study were soluble phenolic compounds showed in C. chayamansa 6.34, E. prostrata 10.67, J. dioica 1.83 mg equiv of gallic acid/gm BS respectively. The antioxidants soluble in water by the ABTS method were for C. chayamansa 5.9, E. prostrata 12.7 and for J. dioica 2.5 mM equiv. of trolox/gr BS. The histopathological results show an improvement in the tissues treated with the extracts after the induction to hyperglycemia.

Development of a natural molluscicide prototype kit (MoluSchall) for the control of schistosomiasis mansoni transmission

Abstract INTRODUCTION In Brazil, Biomphalaria glabrata, B. tenagophila, and B. straminea are intermediate hosts of Schistosoma mansoni, the etiological agent of schistosomiasis mansoni. Molluscicide use is recommended by the WHO for controlling the transmission of this parasite. Euphorbia milii latex has shown promising results as an alternative molluscicide. Thus, a natural molluscicide prototype kit based on freeze-dried E. milii latex was developed and evaluated against Biomphalaria spp. METHODS E. milii latex was collected, processed, and lyophilized. Two diluents were defined for freeze-dried latex rehydration, and a prototype kit, called MoluSchall, was produced. A stability test was conducted using prototype kits stored at different temperatures, and a toxicity assay was performed using Danio rerio. Additionally, MoluSchall was tested against B. glabrata under semi-natural conditions according to defined conditions in the laboratory. RESULTS MoluSchall was lethal to three Brazilian snail species while exhibiting low toxicity to D. rerio. Regardless of storage temperature, MoluSchall was stable for 24 months and was effective against B. glabrata under semi-natural conditions, with the same LD100 as observed under laboratory conditions. CONCLUSIONS MoluSchall is a natural, effective, and inexpensive molluscicide with lower environmental toxicity than existing molluscicides. Its production offers a possible alternative strategy for controlling S. mansoni transmission.

Vasorelaxant activity of Euphorbia furcillata Kunth mainly by activation of NO/cGMP pathway and calcium channel blockade / Actividad vasorrelajante de Euphorbia furcillata Kunth principalmente por activación de la vía NO/GMPc y bloqueo de canales de calcio]

The aim of current study was to determinate ex vivo and chromatographic fingerprint by HPLC of four extracts of Euphorbia furcillata K. Ethyl acetate extract of Euphorbia furcillata (EaEEf) was the most effective and potent extract (Emax=98.69±1.24%) and its effect was partially endothelium-dependent. Functional vasorelaxant mechanism of action of EaEEf was determinate, EaEEf showed efficient relaxation of KCl [80 mM]-induced contraction and norepinephrine and CaCl2 contraction curves showed diminution of maximal contraction in the presence of EAEEf and EaEEf-relaxation curve was shifted to the right in the presence of L-NAME (nitric oxide synthase inhibitor) and ODQ (guanylate cyclase inhibitor). Chromatographic fingerprints analysis suggests presence of diterpenoid such as abietane, tigliane, and ingenane skeletons. Our experiments suggest the EaEEf vasorelaxant activity could be attributed to diterpenoid molecules whose mechanism involves nitric oxide production and calcium channel blockade.

Se determinó el efecto vasorrelajante ex vivo y los perfiles cromatográficos mediante HPLC de cuatro extractos de Euphorbia furcillata K.. El extracto de acetato de etilo de E. furcillata (EaEEf) fue el más eficaz y potente en la contracción inducida por norepinefrina (Emax=98.69±1.24%) y el efecto fue parcialmente dependiente del endotelio vascular. Se determinó el mecanismo de acción vasorrelajante para EaEEf, este mostró ser eficaz sobre la contracción inducida por KCl [80 mM] y la curva de contracción en respuesta a norepinefrina y CaCl2 en presencia de EaEEf mostró disminución en la contracción máxima, mientras que la curva de relajación de EaEEf en presencia de L-NAME (inhibidor de óxido nítrico sintasa) y ODQ (inhibidor de guanilato ciclasa) se desplazó hacia la derecha. El análisis cromatográfico de EaEEf sugiere la presencia de moléculas diterpenoides como abietano, tigliano y esqueletos de ingenano. Nuestros resultados sugieren que el efecto vasorrelajante de EaEEf podría atribuirse a moléculas diterpenoides, cuyo mecanismo de acción involucra la producción de óxido nítrico y bloqueo de canales de calcio.

Determinación de fitoconstituyentes y evaluación de la actividad catártica en el extracto hidroalcohólico de Euphorbia huachanhana (huachangana) / Determination of phytoconstituents and evaluation of cathartic activity of Euphorbia huachanhana (Klotzsch & Garcke) Boiss (huachangana) hydroalcoholic extract

Objetivo. Determinar los fitoconstituyentes del extracto hidroalcohólico de Euphorbia huachanhana (Klotzsch & Garcke) Boiss (huachangana) y evaluar su actividad catártica. Materiales y métodos. Se elaboró un extracto hidroalcohólico con etanol al 70% (70:30) del tubérculo fresco de Euphorbia huachanhana (Klotzsch & Garcke) Boiss (huachangana), el cual fue analizado mediante un perfil fitoquímico cualitativo y el uso de espectroscopia UV/V y espectroscopia infrarroja (IR). Se tuvieron 36 ratones albinos, distribuidos en seis grupos de seis cada uno: Grupo I, suero fisiológico 0,9%); Grupo II, control positivo (senósido 250 mg/kg), y Grupos III, IV, V y VI (experimentales) a los que se les administró el extracto hidroalcohólico de Euphorbia huachanhana (Klotzsch & Garcke) Boiss (EH) a dosis 200 mg/kg, 400 mg/kg, 600 mg/kg y 800 mg/kg. Se evaluó la actividad catártica mediante la frecuencia de defecación y el porcentaje de motilidad intestinal con administración de carbón activado al 10%. Resultados. Se evidenció la presencia de flavonoides, compuestos fenólicos, carbohidratos, taninos, esteroides, azúcares reductores, aminoácidos y antraquinonas. Mediante espectroscopia UV/V se tuvo una banda de absorción de 290 nm lo que corresponde a una antraquinona; por espectroscopia infrarroja (IR) se evidenció la presencia de grupos hidroxilo y carbonilo. La mayor frecuencia de defecación (7,7 por hora) y el mejor tránsito intestinal (92,3%) fueron encontrados en el grupo que recibió EH a 200 mg/kg, estas diferencias fueron significativas en comparación al grupo blanco (p<0,05). Conclusiones. Se encontró, como molécula de interés, la presencia de una antraquinona con grupos funcionales hidroxilo y carbonilo; asimismo, la administración del extracto hidroalcohólico de Euphorbia huachanhana (Klotzsch & Garcke) Boiss a dosis de 200 mg/kg ofreció los mejores resultados en actividad catártica. Sin embargo, el diseño utilizado no permite establecer que la presencia de estas moléculas son la causa directa del efecto catártico observado.

Objective. To determine the phytoconstituents of the Euphorbia huachanhana (Klotzsch & Garcke) Boiss (huachangana) tuber hydroalcoholic extract and to evaluate its cathartic activity. Materials and methods. An hydroalcoholic extract was elaborated with 70% ethanol (70:30) using fresh tuber of Euphorbia huachanhana (Klotzsch & Garcke) Boiss (huachangana). That extract was analyzed for its phytochemical profile, and by UV/V spectroscopy and infrared spectroscopy (IR) to search some bioactive molecules. Thirty-six albino mice were distributed in six groups of six each one: Group I, 0.9% saline solution; Group II, Positive Control (Sennoside 250 mg/kg); and Groups III, IV, V and VI (Experimental) to which hydroalcoholic extract of Euphorbia huachanhana (Klotzsch & Garcke) Boiss (EH) were administered at doses 200 mg/kg, 400 mg/kg; 600 mg/kg and 800 mg/kg. The cathartic activity was evaluated by frequency of defecation and percentage of intestinal motility with administration of 10% activated carbon. Results. Presence of flavonoids, phenolic compounds, carbohydrates, tannins, steroids, reducing sugars, amino acids and anthraquinones was evidenced. An absorption band of 290 nm was observed by UV / V spectroscopy and infrared spectroscopy (IR), which corresponds to an anthraquinone, and the presence of hydroxyl and carbonyl groups was evidenced. The highest frequency of defecation (7.7 per hour) and the best intestinal transit (92.3%) were found on group which received EH at 200 mg/kg, these differences were statistically significant in comparison to the 0.9% saline solution group (p<0.05). Conclusions. The presence of an anthraquinone with hydroxyl and carbonyl groups was found as a molecule of interest. Additionally, the administration of Euphorbia huachanhana (Klotzsch & Garcke) Boiss hydroalcoholic extract at a dose of 200 mg / kg gave the best cathartic activity. However, this experimental design does not allow establishing that the presence of these molecules are the direct cause of the observed cathartic effect.

Ethnomedicinal uses of tawatawa (Euphorbia hirta Linn.) in selected communities in the Philippines: A non-invasive ethnographic survey using pictures for plant identification

@#<p style="text-align: justify;"><strong>BACKGROUND:</strong> There is a growing interest in the use of Euphorbia hirta Linn. as herbal remedy for dengue, supposedly based on folkloric practice. However, there has been no ethnobotanical documentation of such use in the Philippines. Because of this, the medical community cautions the public against the sole use of E. hirta in treating dengue.</p><p style="text-align: justify;"><b>OBJECTIVE:</b> To describe the ethnomedicinal uses of Euphorbia hirta Linn. In selected communities in the Philippines. Specific Objectives. (1) To identify the vernacular names of the plant; (2) to identify the earliest known use of the plant against dengue infection and for other indications; (3) to document the methods of preparation and administration, side effects, and contraindications of use.</p><p style="text-align: justify;"><strong>METHODS:</strong> Cross-sectional descriptive design using the snowball sampling of interviewer-guided key informants for the ethnobotanical interview.</p><p style="text-align: justify;"><strong>LIMITATIONS:</strong> The results of this study may be limited by its convenient sampling design and the use of plant pictures with different magnifications.</p><p style="text-align: justify;"><strong>RESULTS AND CONCLUSION:</strong> Majority of the respondents were female (93%), 41-60 years old (39%), had high school education (43%), and resided in Quezon City (31%). The plant is locally known as tawatawa, butobutonesan, malagatas, and mangagaw. It has been used to treat fever in the Philippines as early as 1948. Its use as a treatment for dengue started only in the 1980s. The plant is either squeezed, crushed, or boiled, and is administered topically or orally. The only reported side-effect is increased urinary frequency.</p><p style="text-align: justify;"><b>RECOMMENDATIONS:</b> It is recommended that more comprehensive and large scale studies be conducted, including (1) identification of folkloric uses of E. hirta for the treatment of other diseases; (2) determination of different concentrations of extract (crude or semicrude) using the various reported preparations for optimal outcomes for the different reported medicinal uses.</p>

Preliminary investigation on processing mechanism of Kansui Radix by liquorice based on thermal analysis technology / 中国中药杂志

In the thermal analysis, the pyrolysis characteristics of crude Kansui Radix, alcohol extract of Kansui Radix, petroleum ether extract, chloroform extract, ethyl acetate extract, n-butanol extract, and licorice vinegar were analyzed with simulated air (N₂-O₂ 4:1) as the carrier gas, at a temperature increase rate of 10 °C·min⁻¹ and a volume flow rate of 60 mL·min⁻¹, respectively. The results showed that due to the different polarity of the extraction solvent, the type and quantity of the chemical components contained in each polar part were different, and with the increase in the amount of solid powder of licorice, the peak of the maximum heat loss rate occurred in advance. For petroleum ether, chloroform, and ethyl acetate fractions, (157.40±1.06), 3.50, (25.83±1.66) °C in advance respectively, but the weight loss rate of the chloroform fraction was increased by (2.62±5.19) °C, while decreased by (33.90±1.72), (19.28±1.11) °C for the petroleum ether and ethyl acetate fractions. So we can conclude that with the addition of licorice, the pyrolysis rate of the petroleum ether and chloroform fractions in the toxic part of Kansui Radix was increased; the temperature point at the peak of the maximum weight loss rate was decreased, and the ethyl acetate fraction (effective part) showed a decrease in temperature rising process, but its overall ratio of weight loss and weight loss rate were relatively small, retaining the effect of medicinal ingredients. This proved the mechanism of licorice system Kansui Radix on attenuating toxicity after processing and the scientificity and rationality of licorice system Kansui Radix. At the same time, as the proportion of glycyrrhizin was increased, the peak of the maximum heat loss rate of petroleum ether, chloroform and ethyl acetate fractions occurred in advance; the peak temperature was decreased, with easy pyrolysis. Among them, the thermogravimetric rate of the mixture of petroleum ether and chloroform fractions (10:1) was relatively large, with a low peak temperature, while ethyl acetate fraction showed opposite results. This conclusion has certain guiding significance for the ratio of gansui to licorice.

Anti-proliferation activity of terpenoids isolated from Euphorbia kansui in human cancer cells and their structure-activity relationship / 中国天然药物

Euphorbia kansui is a commonly used traditional Chinese medicine for the treatment of edema, pleural effusion, and asthma, etc. According to the previous researches, terpenoids in E. kansui possess various biological activities, e.g., anti-virus, anti-allergy, antitumor effects. In this work, twenty five terpenoids were isolated from E. kansui, including thirteen ingenane- and eight jatrophane-type diterpenoids (with two new compounds, kansuinin P and Q) and four triterpenoids. Eighteen of them were analyzed by MTS assay for in vitro anticancer activity in five human cancer cell lines. Structure-activity relationship for 12 ingenane-type diterpenoids in colorectal cancer Colo205 cells were preliminary studied. Significant anti-proliferation activities were observed in human melanoma cells breast cancer MDA-MB-435 cells and Colo205 cells. More than half of the isolated ingenane-type diterpenoids showed inhibitory activities in MDA-MB-435 cells. Eight ingenane- and one jatrophane-type diterpenoids possessed much lower IC values in MDA-MB-435 cells than positive control staurosporine. Preliminary structure-activity relationship analysis showed that substituent on position 20 was important for the activity of ingenane-type diterpenoids in Colo205 cells and substituent on position 3 contributed more significant biological activity of the compounds than that on position 5 in both MDA-MB-435 and Colo205 cells.

Use of raw Euphorbia tirucalli extract for inhibition of ascitic Ehrlich tumor / Avaliação do uso do extrato bruto de Euphorbia tirucalli na inibição do tumor ascítico de ehrlich

Objective: to evaluate the effect of the Euphorbia tirucalli hydroalcoholic extract (ETHE) on the development of Ehrlich Tumor, in its ascitic form. Methods: we intraperitoneally inoculated 15 Swiss mice with 10.44 x 107 cells of Ehrlich Tumor and divided them in two groups one day after: ETHE Group (eight mice), treated with a dosage of 125 mg/kg/day of EHTE for five days; and Control Group (seven mice), treated only with 0.9% isotonic saline solution over the same period. The treatment was done by gavage. Ten days after inoculation, four mice from each group were sacrificed for quantification of tumor cell number, ascitic fluid volume and bone marrow cell number. The remaining animals were maintained to evaluate survival. Results: The ascitic fluid volume and the tumor cell number were decreased in the ETHE group when compared with the control group, but with no statistical significance. On the other hand, survival was higher in the ETHE group, as well as the number of bone marrow cells. Conclusion: Treatment with ETHE after inoculation of Ehrlich Tumor decreases its development and increases survival and the bone marrow cellularity, thus reducing the myelosuppression present in the Ehrlich Tumor bearing mice.

Objetivo: avaliar o efeito do extrato hidroalcoólico de Euphorbia tirucalli (ETHE) sobre o desenvolvimento do tumor de Ehrlich em sua forma ascítica. Métodos: quinze camundongos Swiss foram inoculados via intraperitoneal com 10,44x107 células do tumor de Ehrlich e um dia depois foram divididos em dois grupos: Grupo ETHE (oito camundongos), tratados com a dose de 125mg/kg/dia de ETHE por cinco dias e Grupo Controle (sete camundongos), tratado apenas com 0,9% de solução salina isotônica em relação ao mesmo período. O tratamento foi realizado por gavagem. Dez dias após a inoculação, quatro animais de cada grupo foram sacrificados para a quantificação do número de células de tumor, do volume de fluido ascítico e do número de células da medula óssea. Os demais animais foram mantidos, para avaliar a sobrevivência. Resultados : o volume de líquido ascítico e do número de células tumorais foram menores no grupo ETHE quando comparado ao grupo controle, porém sem significância estatística. Por outro lado, a sobrevivência dos animais foi maior no grupo de ETHE, bem como, a quantidade de células de medula óssea. Conclusão: o tratamento com ETHE, após a inoculação do tumor, diminuiu o seu desenvolvimento e aumentou sobrevida, bem como, a celularidade da medula óssea, reduzindo assim, a mielossupressão presente nos animais portadores de tumor de Ehrlich.