Trichilin-type limonoids isolated from the fruits of Trichilia connaroides / 药学学报

Two new trichilin-type limonoids were isolated from the fruits of Trichilia connaroides along with two known limonoids, 3α-deacetylamoorastatin (3) and mesendanins K (4). Their planar structure and relative configuration were elucidated by comprehensive analyses of HR-ESI-MS, 1H NMR, 13C NMR, HSQC, HMBC and ROESY data. An antitumor activity assay showed that compounds 1, 2 and known compound 4 had weak cytotoxicity against a human cervical cancer cell line (HeLa).

Anxiolytic-like and proneurogenic effects of Trichilia catigua ethyl-acetate fraction in mice with cerebral ischemia

Abstract Trichilia catigua A. Juss., Meliaceae, known as "catuaba" in Brazil, has been popularly used as a tonic for fatigue, impotence and memory deficits. Previously, we have demonstrated that T. catigua ethyl-acetate fraction exerted antidepressive-like effects in mice. Affective-like symptoms are also well recognized outcome of cerebral ischemia in clinical and preclinical settings. Therefore, here we evaluated the effects of ethyl-acetate fraction on the emotional outcomes and its relation with hippocampal neurogenesis in ischemic mice. Male Swiss mice were subject to the bilateral common carotid occlusion during 20 min. The animals received ethyl-acetate fraction (400 mg/kg, orally) 30 min before and once per day during 7 days after reperfusion. Emotional outcomes were assessed using the open field test, elevated zero maze, and the tail suspension test. After the behavioral testing, the animals were sacrificed and their brains were processed to immunohistochemistry and Nissl staining. Ischemic mice exhibited anxiogenic-like behaviors in the elevated zero maze, hippocampal neurodegeneration and decreased hippocampal neurogenesis. The anxiogenic-like effect was counteracted by ethyl-acetate fraction administration. Furthermore, ethyl-acetate fraction restored the number of newborn neurons in the dentate gyrus of hippocampus of ischemic mice. In conclusion, T. catigua ethyl-acetate fraction promoted functional recovery and restored hippocampal neurogenesis in ischemic mice.

Highly oxygenous trichilin-type limonoids from Trichilia sinensis / 中国天然药物

Six new trichilin-type limonoids (1-6) with C-19/29 lactol or acetal bridge and a new ring intact limonoid (7) were isolated from the desiccative ripe fruits of Trichilia sinensis. Their structures were determined by extensive spectroscopic methods including H NMR, C NMR, HSQC, HMBC, ROESY experiments as well as HRESI-MS data. All isolated compounds were evaluated for toxicities against human pulmonary carcinoma A549 and Hela cell lines by sulforhodamine B (SRB) method. Compound 7 showed weak inhibitory activity in Hela cell line at 40 μmol·L.

Trichilia catigua: therapeutic and cosmetic values

ABSTRACT Medicinal plants play an important role in human health care. It is estimated that about 25–30% of all drugs are evaluated as therapeutic agents derived from natural products. Research in the pharmaceutical industry has demonstrated that for complex diseases, natural products still represent a valuable source for the production of new chemical compounds, since they possess privileged structures. Among Brazilian biodiversity, "catuaba" is popularly used as a tonic to treat fatigue, stress, impotence, memory deficits, and digestive disorders. Studies show antibacterial, trypanocidal, antioxidant, antiarrhythmic, antidepressant, improvement of memory, anti-inflammatory and antinociceptive activities, as well as phytocosmetic activity in cellulite treatment and in anti-ageing. The Brazilian plants known and used as catuaba are represented by more than twenty different species; however, the plant most commonly found in Brazil as "catuaba" is the species Trichilia catigua A. Juss., Meliaceae. Thus, the aim of this paper is to present a review of T. catigua, with emphasis on biological activities, chemical and analytical development and formulations in order to provide a broader and deeper insight, seeking a herbal medicine and/or phytocosmetic as well as future prospects for commercial exploitation and directions for future studies.

Positive Effects of Aqueous and Ethanolic Extracts of Stem Bark from Trichilia emetica (MELIACEAE) on Cellular Immunity Markers in Rats.

Aims: This study was designed to evaluate the effect of aqueous and ethanolic extracts of stem bark from Trichilia emetica on the cellular immunity markers (TCD4+ count, Lymphocytes, WBC, RBC) in rats wistar. Study Design: Forty-two rats have been divided into seven groups of six and each was administered a single oral dose of the samples for 8 days. Experimental design was as follows: Group I served as control and received distilled water, group II received Isoprinosine at a dose of 50 mg/kg body weight (b.w.), group III was administered Methylprednisolone (15 mg/kg b.w), group IV and group V received aqueous extract at a dose of 100 and 200 mg/kg b.w. respectively, group VI and VII were administered ethanolic extract at a doses of 100 and 200 mg/kg b.w. respectively. At the end of the treatment, some blood was collected in EDTA tubes for the determination of TCD4+ count by flow cytometry and hematological parameters by hemogram. Results: Concerning TCD4+ count, the results show that there is a significant difference (P<0.05) between the control group and all groups of the treated rats. There is also a significant difference between both extracts. But the ethanolic extract at a dose of 100 mg/kg b.w. showed pronounced activity by TCD4+ increasing in relation with control and all the treated groups. Thus, the haematological parameters show that there is no significant difference (p˃ 0.05) between the control group and the other treated groups by aqueous extract (100 and 200 mg/kg b.w.) and ethanolic extract at a dose of 200 mg/kg b.w. concerning WBC count and total lymphocytes level. However, there is a significant increase (P<0.05) of WBC and total lymphocytes in blood of rats treated by ethanolic extract at a dose of 100 mg/kg b.w. compared with control group. Conclusion: The present study revealed that both extracts of Trichilia emetica have positive effects on cellular immunity markers such as TCD4+, total lymphocytes, WBC, RBC. However, lower concentration of ethanolic extract showed much positive effects compared to the aqueous extract. The results of this preliminary study could be used to explore the spleenocyte proliferation and the analysis of spleen cells in order to see the real immunomodultory activity.

Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)

BACKGROUND: Limonoids are highly oxygenated compounds with a prototypical structure. Their occurrence in the plant kingdom is mainly confined to plant families of Meliaceae and Rutaceae. Owing to their wide range of pharmacological and therapeutic properties, this study was aimed at investigating the potential nitric oxide (NO) and acetylcholinesterase (AChE) inhibitory activity and the cytotoxicity of three limonoids: trichilia lactone D5 (1), rohituka 3 (2) and dregeanin DM4 (3), isolated from Trichilia welwitschii C.DC. RESULTS: Results indicated that the three limonoids had low cytotoxicity towards Vero cells with LC50 values ranging from 89.17 to 75.82 µg/mL. Compounds (2) and (3) had lower cytotoxicity compared to puromycin and doxorubicin used as reference cytotoxic compounds. Compound (1) (LC50 of 23.55 µg/mL) had good antiproliferative activity against RAW 264.7 cancer cells. At the lowest concentration tested (0.5 µg/mL), compound (2) and (3) released the lowest amount of nitric oxide (2.97 and 2.93 µM, respectively). The three limonoids had anti-AChE activity with IC50 values ranged of 19.13 µg/mL for (1), 34.15 µg/mL for (2) and 45.66 µg/mL for (3), compared to galantamine (IC50 of 8.22 µg/mL) used as positive control. CONCLUSION: The limonoid compounds studied in this work inhibited nitric oxide production in LPS-stimulated macrophages and had anti-AChE activity. Trichilia lactone D5 had potential antiproliferative activity against RAW 264.7 cancer cells. The limonoids had low cytotoxicity towards Vero cells lines. This study provided further examples of the importance of limonoids compounds as potential AChE inhibitors and anti-inflammatory agents targeting the inhibition of NO production.

Antidiarrheal and antimicrobial profiles extracts of the leaves from Trichilia emetica Vahl. (meliaceae)

Objective: To evaluate anti-diarrhoeal and antimicrobial activities of the bioactive fraction of Trichilia emetica in order to provide a scientific basis for the management of gastroenteritis in Burkina Faso. Methods: To do this, polyphenols content of extract and fractions were investigated. Folin- Ciocalteu, AlCl

Actividad citotóxica de extractos acuosos de hojas de Trichilia hirta sobre células tumorales humanas / Cytotoxic activity of water extracts of Trichilia hirta leaves on human tumor cells

La planta Trichilia hirta L. (Meliaceae) es utilizada tradicionalmente por pacientes con cáncer como recurso antitumoral. Por ello, los objetivos de este estudio fueron evaluar la actividad citotóxica de extractos acuosos de hojas de Trichilia hirta sobre células tumorales e identificar mediante un tamizaje fitoquímico las principales familias de fitocomponentes presentes en éstos. La actividad citotóxica de los extractos se evaluó sobre células de melanoma humano (SK-mel-3) y adenocarcinoma humano de mama (T-47D). Las células epiteliales de riñón de mono verde Cercopithecus aethiops (Vero) fueron utilizadas como control de células no tumorales. Los resultados mostraron la presencia de triterpenos/esteroides, saponinas, cumarinas, azúcares reductores, fenoles y taninos, flavonoides y carbohidratos/glicósidos en los extractos. Los extractos acuosos de hojas mostraron actividad citotóxica fundamentalmente sobre las células tumorales, lo cual contribuye a explicar la mejoría referida por pacientes con cáncer que consumen estos extractos de forma tradicional

Trichilia hirta L. (Meliaceae) is traditionally used by patients suffering from cancer as an antitumoral resource. Therefore, the objectives of this study were to evaluate the cytotoxic activity of water extracts of Trichilia hirta leaves on tumour cells and identify through a phytochemical screening the principal families of phytocomponents contained in these extracts. The cytotoxic activity of these extracts was also evaluated on human melanoma cells (SK-mel-3) and human breast carcinoma (T-47D). The African green monkey kidney (AGMK) cells Cercopithecus aethiops (Vero) were used as a non-tumour cells control. The results showed the presence of triterpenes/steroids, saponins, coumarins, reductor sugars, phenols and tannins, flavonoids and carbohydrates/glycosides in the extracts. The water leaf extracts showed cytotoxic activity mainly on tumour cells, which contributes to explain the referred recovery by patients suffering form cancer that traditionally consume these extracts

Ethnopharmacological evaluation of Trichilia hirta L. as anticancer source in traditional medicine of Santiago de Cuba / Evaluación etnofarmacológica de Trichilia hirta como una fuente anticancer en la medicina tradicional de Santiago de Cuba

Trichilia hirta L. (Meliaceae) is traditionally used as antitumor source in Santiago de Cuba. Therefore, the aim of this study was to document and analyze the traditional medicinal use of this plant by cancer patients in Santiago de Cuba and to evaluate its antiproliferative activity on human normal and cancer cells. Cancer patients consuming Trichilia hirta extracts (Jubabán) were randomly selected and interviewed. The antiproliferative activity of a polysaccharide-rich fraction from leaves was evaluated against normal (MRC-5) and cancer cells (A-549, HeLa and Hep-2) by MTT assay. The study revealed that Trichilia hirta extracts are mainly used as anticancer source (46 percent. Moreover, the majority of cancer patients consuming Trichilia hirta extracts had carcinoma (86 percent). In particular, the most frequent were lung (26 percent) and prostate (18 percent) carcinoma. The majority (90 percent) of patients were consuming the extracts simultaneously, or after the chemotherapy and radiotherapy treatment. The polysaccharide-rich fraction showed antiproliferative activity against human lung cancer cells (A-549) and human cervix carcinoma (HeLa) cancer cells. However, no toxicity was observed in human normal fibroblasts (MRC-5). These results suggest that polysaccharide-rich fraction from Trichilia hirta contribute to the antitumor properties of this specie.

Trichilia hirta L. (Meliaceae) es tradicionalmente usada como recurso antitumoral en Santiago de Cuba. Por lo que, el objetivo de este estudio fue documentar y analizar el uso tradicional de esta planta por pacientes con cáncer en Santiago de Cuba y evaluar su actividad antiproliferativa sobre células humanas normales y tumorales. Pacientes con cáncer consumiendo los extractos de Trichilia hirta (jubabán) fueron aleatoriamente seleccionados y entrevistados. La actividad antiproliferativa de la fracción rica en polisacáridos de hojas fue evaluada en células normales (MRC-5) y en células tumorales (A-549, HeLa y Hep-2) a través del ensayo con MTT. El estudio reveló que los extractos de Trichilia hirta eran usados mayoritariamente como recurso antitumoral (46 por ciento). Además, la mayoría de los pacientes consumiendo extractos de Trichilia hirta presentaron carcinoma (86 por ciento). En particular, los más frecuentes fueron carcinomas de pulmón (26 por ciento) y próstata (18 por ciento). También la mayoría de los pacientes (90 por ciento) consumieron los extractos simultáneamente o después de tratamientos con quimioterapia y radioterapia. La fracción rica en polisacáridos mostró actividad antiproliferativa contra las células de cáncer de pulmón humano (A-549) y carcinoma de cerviz humano (HeLa). Sin embargo, no se observó toxicidad en fibroblastos humanos normales (MRC-5). Estos resultados sugieren que la fracción rica en polisacáridos de hojas de Trichilia hirta contribuye a la actividad antitumoral de esta especie.

Actividad larvicida de extractos etanólicos de Tabernaemontana cymosa y Trichilia hirta sobre larvas de estadio III y IV de Aedes aegypti (Diptera: Culicidae) / Larvicidal activity of ethanol extracts of Tabernaemontana cymosa and Trichilia hirta against III and IV stage larvae of Aedes aegypti (Diptera: Culicidae)

Introducción: el mosquito Aedes aegypti es el principal vector de los virus del dengue y la fiebre amarilla. Una de las formas actuales para combatir estas enfermedades es el control del vector. Sin embargo, los problemas causados por los insecticidas sintéticos y la resistencia adquirida por los mosquitos, hacen cada vez más difícil esta lucha. Las plantas constituyen una fuente alternativa al uso de insecticidas sintéticos. Objetivos: evaluar la actividad larvicida para el mosquito Aedes aegypti, de los extractos etanólicos y fracciones activas, de diferentes órganos vegetales de las especies Trichilia hirta L. y Tabernaemontana cymosa Jacq. Métodos: en este estudio se utilizaron larvas de Aedes aegypti en estadios III y IV. Los extractos etanólicos totales se obtuvieron por maceración del material vegetal seco y molido, durante una semana y posterior secado a presión reducida con un rotoevaporador. La obtención de fracciones y subfracciones, se realizó por cromatografía de columna abierta, usando solventes de diferentes polaridades. La actividad larvicida se evaluó bajo protocolos recomendados por la Organización Mundial de la Salud. Resultados: los extractos etanólicos de corteza de Trichilia hirta y flores, corteza y hojas de Tabernaemontana cymosa, no mostraron actividad larvicida. El extracto de semillas de Trichilia hirta mostró una actividad moderada con una CL50 y CL90 de 219,2 y 331,4 mg/L respectivamente. El extracto etanólico de semillas de Tabernaemontana cymosa, la fracción F008 y la subfracción F011, mostraron una buena actividad larvicida con CL50 de 35,1; 20,9, y 14,98 mg/L, respectivamente. Conclusiones: según los resultados, se consideró como promisorio el extracto de semillas de Tabernaemontana cymosa para la obtención de metabolitos secundarios con actividad larvicida.

Introduction: Aedes aegypti is the main vector of dengue and yellow fever. One way to combat these diseases today is the vector control. However, the problems caused by synthetic insecticides and the acquired resistance by mosquitoes, turn this control into a more difficult struggle every day. The plants offer an alternative source to the use of synthetic insecticides. Objectives: the objective of this study was to evaluate the larvicidal activity of the ethanol extracts and active fractions of different organs of Trichilia hirta L. and Tabernaemontana cymosa Jacq. Methods: in this study, Aedes aegypti larvae in III and IV stages were used. The total ethanol extracts were obtained by maceration of dried and ground plant material for a week and then dried at reduced pressure. The fractionation was performed by open column chromatography with the use of different polarity solvents. The larvicidal activity was assessed following protocols recommended by the World Health Organization. Results: the ethanol extracts from Trichilia hirta bark and flowers, and Tabernaemontana cymosa bark and leaves showed no larvicidal activity. The Trichilia hirta seed extract showed a moderate activity with an LC50 and LC90 of 219.2 and 331.4 mg/L respectively. The ethanol extract from Tabernaemontana cymosa seeds, the fraction F008 and the subfraction F011, showed good larvicidal activity with LC50 of 35.1, 20.9, and 14.98 mg/L, respectively. Conclusions: according to the results obtained in this study, the extract from Tabernaemontana cymosa seeds could be considered as a potential source of secondary metabolites with larvicidal activity.

Antimicrobial Activity of Crude Extracts of Endophytic Fungi Isolated from Medicinal Plant Trichilia elegans A. Juss.

Endophytes are microorganisms which inhabit inside plants. These microorganisms are identified as being fungi or bacteria and can be useful for prospectionof bioactive compounds that may have medical and pharmaceutical applications.Trichilia elegans (Meliaceae) is a native tree in Brazil. Preparations using leaves, seeds, bark and roots and some members of the Trichilia genus are used in Brazilian popular medicine.The aim of the present work was to investigate biotechnological potential of fungal endophytes (Cordyceps memorabilis, Phomopsis longicolla, Dothideomycete sp. and one non-indentified) isolated from T. elegans, that have been assayed against five pathogenic bacteria. The fungi were incubated in Potato Dextrose and the secondary metabolites was extracted from fermentation medium with ethyl acetate, also was used directly extraction with methanolfrom mycelium. The extraction by ethyl acetate from C. memorabilis inhibited growing of Enterococus hirae, Micrococcus luteus and Escherichia coli. Fungal Phomopsis sp. inhibited M. luteus, E. hirae and Salmonella typhi, Dothideomycetes sp. and G8-25 inhibited M. luteus and E. hirae. Noextract by ethyl acetate inhibited Staphylococcus aureus and also no extract obtained by methanol inhibited the growing of tested bacteria. The present study helped justified the traditional use of T. elegans against human pathogenic bacteria.

Avaliação do fator de proteção solar em fotoprotetores acrescidos com extratos da flora brasileira ricos em substâncias fenólicas / Evaluation of the Sun Protection Factor in sunscreens added to with vegetable extracts rich in phenolic substances

Sabe-se que o número de casos de câncer de pele tem crescido muito nos últimos anos. Com isso, novos produtos são constantemente desenvolvidos no intuito de aumentar a gama de substâncias para proteção solar. O principal objetivo desse trabalho foi a análise in vitro da propriedade fotoprotetora de uma formulação contendo filtros solares químicos, adicionada de extratos brutos de Guazuma ulmifolia, Maytenus ilicifolia, Stryphnodendron adstringens e Trichilia catigua, respectivamente, e a avaliação quanto ao acréscimo do Fator de Proteção Solar (FPS). O ensaio foi conduzido pelo método espectrofotométrico in vitro do Fator de Proteção Solar (FPS). O teor de Polifenóis Totais (PT) e sua correlação com a Capacidade Antioxidante (CA) dos extratos avaliados foram realizados. Os resultados demonstram que as formulações foram estáveis após a adição dos extratos, quanto a características físico-químicas (características macroscópicas, ensaio de centrifugação e pH) quando comparadas ao controle. O ensaio de FPS in vitro demonstrou decaimento do FPS das formulações acrescidas de extratos vegetais ricas em compostos fenólicos, exceto para o extrato de S. adstringens. Os FPS obtidos para os extratos foram ≤2. O teor em PT foram (%): G. ulmifolia, 24,26±0,34; M. ilicifolia, 14,66±0,18; S. adstringens, 34,38±0,62 e T. catigua, 41,60±0,13. Os valores da CA (IC50) frente ao radical DPPH foram (miug/mL): vitamina C (7,52±0,12), G. ulmifolia (8,94±0,13), M. ilicifolia (38,41±0,93), S. adstringens (7,31±0,15) e T. catigua (5,48±0,04). A CA foi diretamente proporcional ao teor de PT.

It is known that the number of cases of skin cancer has increased greatly in recent years. Therefore, new products are constantly developed in order to increase the range of substances for sun protection. The aim of this study was evaluate in vitro the property the sunscreen containing chemical sunscreens, with added to extracts of Guazuma ulmifolia, Maytenus ilicifolia, Stryphnodendron adstringens and Trichilia catigua, Sun Protection Factor (SPF). The test was conducted by the spectrophotometric method of in vitro Sun Protection Factor (SPF). The percentage of the Total Polyphenol (TP) and its correlation with Antioxidant Capacity (CA) of the extracts evaluated were performed. The results show that the formulations were stable after the addition of extracts, in relation as the physico-chemical characteristics (macroscopic characteristics, test centrifugation and pH) when compared to control (time 0). The FPS test in vitro showed decrease SPF of the formulations added of plant extracts rich in phenolic compounds, except for the extract of S. adstringens. The FPS for the extracts obtained were ≤2. The percentage of the PT were (%): G. ulmifolia, 24,26±0,34; M. ilicifolia, 14,66±0,18; S. adstringens, 34,38±0,62 e T. catigua, 41,60±0,13. The values of CA (IC50) against the DPPH radical were (miug/mL): vitamin C (7,52±0,12), G. ulmifolia (8,94±0,13), M. ilicifolia (38,41±0,93), S. adstringens (7,31±0,15) e T. catigua (5,48±0,04). CA was directly proportional to the content of PT.

Comportamento meiótico durante a microsporogênese em espécies da família meliaceae / Comportamiento meiótica durante la microsporogénesis en especies de la familia meliaceae / Meiotic behavior during microsporogenesis of some species of meliaceae family

A família Meliaceae inclui espécies de grande interesse agronômico, ecológico, econômico e ornamental de alto potencial madeireiro no mundo. No Brasil ocorrem cerca de seis gêneros e 100 espécies. Considerando a falta de estudos citológicos para esse grupo, este trabalho descreve o comportamento meiótico durante a microsporogênese de seis espécies (Trichilia pallida, Trichilia elegans, Trichilia catigua, Cedrela fissilis, Cabralea canjerana, Guarea guidonea) da família Meliaceae, representando quatro dos seis gêneros que estão presentes no Brasil. Inflorescências foram coletadas e fixadas em etanol/ácido acético (3:1 v/v) por 24 horas, transferidos para álcool a 70%, e acondicionadas sob refrigeração. As lâminas foram preparadas pela técnica de esmagamento, coradas com carmim acético a 1%. A análise citogenética revelou poucas irregularidades meióticas, sendo estas relacionadas a segregação dos cromossomos, fusos irregulares e conexão citoplasmática. Como consequência da segregação irregular dos cromossomos na meiose I e II e da organização irregular dos fusos na meiose II, o padrão de citocinese também foi irregular originando tétrades com micrócitos e tríades, resultando em micrósporos desbalanceados e de núcleo restituído (2n).

The Meliaceae family includes the most important species with great agronomic, ecological, economic and ornamental value and high timber potential in the world. In Brazil, approximately six genera and 100 species are found. Considering the lack of cytological studies for its genera, the present study describes the meiotic behavior during microsporogenesis of six species of the Meliaceae family, representing four of the six genera that are present in Brazil; these species are: Trichilia pallida, Trichilia elegans, Trichilia catigua, Cedrela fissilis, Cabralea canjerana, Guarea guidonea. Inflorescences were collected and fixed in ethanol/acetic acid (3:1 v/v) for 24 hours, transferred to alcohol at 70%, and stored under refrigeration. The slides were prepared by squashing, and stained with acetic carmine 1% and observed under optical microscopy. Cytogenetic analysis revealed few meiotic irregularities, which are related to segregation of chromosome spindles and irregular cytoplasmic connection. As a result of irregular segregation of chromosomes during meiosis I and II and the irregular organization of the spindles in meiosis II, the pattern of cytokinesis was also irregular resulting in microcytic tetrads and triads, unbalanced microspores and restored nuclei (2n).

La familia Meliaceae incluye especies de gran interés agronómico, ecológico, económico y ornamental de alto potencial maderero en el mundo. En Brasil ocurren cerca de seis géneros y 100 especies. Considerando la falta de estudios citológicos para ese grupo, este trabajo describe el comportamiento meiótica durante la microsporogénesis de seis especies (Trichilia pallida, Trichilia elegans, Trichilia catigua, Cedrela fissilis, Cabralea canjerana, Guarea guidonea) de la familia Meliaceae, representando cuatro de los seis géneros que están presentes en Brasil. Inflorescencias fueran colectadas y fijadas en etanol/ácido acético (3:1 v/v) por 24 horas, transferidos para alcohol a 70%, y acondicionadas bajo refrigeración. Las láminas fueron preparadas por la técnica de aplastamiento, coloradas con carmín acético a 1%. El análisis citogenética reveló pocas irregularidades meióticas, siendo éstas relacionadas a la segregación de los cromosomas, fusos irregulares y conexión citoplasmática. Como consecuencia de segregación irregular de cromosomas en la meiosis I y II y de la organización irregular de los fusos en la meiosis II, el estándar de citocinesis también fue irregular originando tétradas con micrófitos y tríades, resultando en micros poros desbalanceados y de núcleo restituido (2n).

Immunorestorative in immunosuppressed Balb/c mice and cytotoxic activity of water extract from Trichilia hirta root / Actividad inmunorestauradora en ratones Balb/c inmunodeprimidos y citotóxica del extracto acuoso de raíz de Trichilia hirta

Patients receiving chemotherapy treatment in Santiago de Cuba traditionally use water extracts from Trichilia hirta roots. The study aim was to evaluate the immunorestorative and cytotoxic activity of water extracts from Trichilia hirta root. Administration of root water extract increased the total and differential leukocyte counts in inmunosupressed Balb/c mice. Thymus weight recovered significantly as well as bone marrow cellularity. Moreover, water extract (125 ug/mL) showed selective cytotoxicity against cancer cells T-47D and SK-mel-3 in comparison with non-cancer cells (Vero). The results indicate that Trichilia hirta has significant immunorestorative effects in vivo and selective cytotoxicity in vitro. Therefore, it might be a promising alternative for cancer therapy.

Pacientes bajo tratamiento quimioterapéutico tradicionalmente usan extractos acuosos de raíz de Trichilia hirta en Santiago de Cuba. El objetivo de este estudio fue evaluar la actividad inmunorestauradora y citotóxica de extractos acuosos de raíz de Trichilia hirta. La administración del extracto acuoso de raíz incrementó los conteos globales y diferenciales de leucocitos en ratones inmunodeprimidos. El peso del timo, así como, la celularidad de la médula ósea se recuperaron significativamente. Además, el extracto acuoso (125 ug/mL) mostró citotoxicidad selectiva contra las células tumorales T-47D y SK-mel-3 en comparación con la línea no tumoral (Vero). Los resultados indican que Trichilia hirta posee significativos efectos inmunorestauradores in vivo y citotoxicidad selectiva, por lo cual podría ser una promisoria alternativa para la terapia del cáncer.

Accelerated chemical stability data of O/W fluid emulsions containing the extract of Trichilia catigua Adr. Juss (and) Ptychopetalum olacoides Bentham

Development of topical dosage forms requires physical, physicochemical and chemical assays that provide, as soon as possible, the formulation with the best stability profiles. This study evaluated the stability of O/W fluid emulsions, by total flavonoids determination, expressed in rutin, containing the standardized extract of Trichilia catigua Adr. Juss (and) Ptychopetalum olacoides Bentham. Samples were evaluated for 90 days stored at 24.0 ± 2.0 ºC, 5.0 ± 0.5 ºC and 40.0 ± 0.5 ºC, following a protocol for the assessment of accelerated chemical stability assay, also known as Normal Stability Test. A sensitive UV-spectrophotometric method at 361.0 nm was previously validated for the determination of the active substance. By Normal Stability Test, the O/W fluid emulsions presented acceptable chemical stability, for at least 90 days, when the samples were stored at 24.0 ± 2.0 ºC and 5.0 ± 0.5 ºC. The storage condition at 40.0 ± 0.5 ºC has accelerated the degradation process of the total flavonoids, consequently, those O/W emulsions containing this kind of natural active substance or a similar preparation must not be stored at elevated temperatures.

O desenvolvimento de formas farmacêuticas tópicas necessita ensaios físicos, físico-químicos e químicos que selecionem rapidamente a formulação de melhor desempenho de estabilidade. Este estudo avaliou a estabilidade de emulsões O/A fluidas, por meio da determinação de flavonóides totais, expressos em rutina, contendo o extrato padronizado de Trichilia catigua Adr. Juss (e) Ptychopetalum olacoides Bentham. As amostras foram armazenadas a 24,0 ± 2,0 ºC; 5,0 ± 0,5 ºC e 40,0 ± 0,5 ºC durante 90 dias e foram avaliadas segundo o protocolo para a determinação da estabilidade acelerada, conhecida como Teste de Estabilidade Normal. A quantificação da substância ativa foi determinada por espectrofotometria na região do ultravioleta a 361,0 nm, previamente validado. Após os ensaios de estabilidade, as emulsões O/A fluidas apresentaram estabilidade adequada, pelo menos, no período de 90 dias, quando armazenadas a 24,0 ± 2,0 ºC e 5,0 ± 0,5 ºC. A condição de armazenamento a 40,0 ± 0,5 ºC acelerou a cinética de degradação dos flavonóides totais, expressos em rutina, portanto, preparações possuindo esta categoria de substância ativa natural ou formulações similares não devem ser armazenadas em temperaturas elevadas.

Virucidal activity presence in Trichilia glabra leaves / Presencia de actividad antiviral en hojas de Trichilia glabra

Different immunomodulatory activities present in Trichilia glabra (TG) leaf extracts have already been described. Particularly, chloroform-methanol extracts were responsible for an in-vivo anti-inflammatory effect. The effect of such extracts on the infectivity of enveloped and naked viruses were investigated. Methanolic fraction extracts were active against herpes simplex virus type 1 (HSV-1) and vesicular stomatitis virus (VSV), while no activity against poliovirus type 3 was observed. VSV was slightly more affected than HSV-1: 2.8 log10 reduction in VSV titer against 2.4 log10reduction in HSV-1 titer when 0.25 mg/ml F2 fraction was tested and a reduction of 2.7 log10in VSV virus titer and of 1.5 log10in HSV-1 virus titer was observed when 0.25 mg/ml F3 fraction was tested. Results obtained in this work suggest a potential pharmaceutical use of TG extract components.

Previamente se han descripto distintas actividades inmunomoduladoras, presentes en extractos de hojas de Trichilia glabra (TG). En particular, se ha demostrado una actividad antiinflamatoria presente en extractos metanólicos. En este trabajo se investigó la actividad virucida de dichos extractos sobre virus envueltos y desnudos. Distintos extractos metanólicos han inactivado en forma moderada los virus herpes simplex tipo 1 (HSV-1) y el virus de la estomatitis vesicular (VSV), mientras no evidenciaron actividad sobre poliovirus tipo 3. VSV resultó algo mas afectado que HSV-1: se observó una reducción en el título viral de 2,8 log10para VSV y de 2,4 log10para HSV-1 cuando se uso una concentración de 0,25 mg/ml de la fracción F2 y una reducción de 2,7 log10para VSV y de 1,5 log 10para HSV-1 cuando se usó una concentración de 0,25 mg/ml de la fracción F3. Los resultados obtenidos en este trabajo, sugieren un potencial uso farmacéutico de los componentes presentes en los extractos de TG.

Atividade inseticida de extratos aquosos de meliáceas sobre a mosca-branca Bemisia tabaci (Genn. ) biótipo B (Hemiptera: Aleyrodidae) / Insecticidal activity of aqueous extracts of meliaceae plants on the silverleaf whitefly, Bemisia tabaci (Genn. ) biotype B (Hemiptera: Aleyrodidae)

Avaliou-se a atividade inseticida de extratos aquosos (na concentração de 3 por cento p/v) de ramos, folhas, frutos verdes e frutos maduros de Melia azedarach L. e de ramos, folhas e córtex de Trichilia pallida Swartz, ambas Meliaceae, sobre ovos e ninfas da mosca-branca Bemisia tabaci (Genn.) biótipo B, criada em tomateiro. No primeiro experimento, os extratos foram aplicados sobre ovos, enquanto no segundo, a aplicação foi feita sobre ovos e ninfas com três dias de idade. Foram conduzidos experimentos independentes para cada espécie vegetal. Os parâmetros avaliados foram mortalidade e duração das fases de ovo e ninfa. Os frutos verdes de M. azedarach foram a estrutura vegetal mais efetiva, seguindo-se as folhas e os frutos maduros. Para T. pallida, os ramos foram os mais efetivos, vindo a seguir as folhas. Os extratos de ramos de M. azedarach e de córtex de T. pallida não apresentaram efeito inseticida significativo. Nenhum dos extratos testados afetou a duração das fases imaturas.

The insecticidal effect of aqueous extract of twigs, leaves, fresh fruits and ripe fruits of Melia azedarach L. and twigs, leaves and cortex of Trichilia pallida Swartz was evaluated on eggs and nymphs of silverleaf whitefly Bemisia tabaci (Genn.) biotype B reared on tomato plants. The extracts were tested at the concentration of 3 percent (w/v). In the first experiment, the extracts were applied only on the egg stage. In the second experiment, the extracts were applied on eggs and 3-day old nymphs. Independent experiments were carried out for each plant species. The parameters evaluated were mortality and duration of egg and nymphal stages. Concerning M. azedarach, fresh fruits were the most effective plant structure followed by leaves and ripe fruits. For T. pallida, twigs were the most effective structure followed by leaves. The extract of twigs of M. azedarach and cortex of T. pallida did not show significant insecticidal activity. None of the plant extracts affected the duration of the immature stages.