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

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

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

Comparação dos efeitos das folhas de Cestrum axillare Vell. com as saponinas isoladas em caprinos / Comparison of the effects of Cestrum axillare leaves with isolated saponins in goats

Cestrum axillare Vell. (formerly Cestrum laevigatum Schltd.), family Solanaceae, is the most important hepatotoxic plant in Brazil that causes acute poisoning. It occurs in the Southeast and Center-West regions and in coastal areas of the Northeast Brazil. Spontaneous poisoning was described in cattle, goats and sheep, with clinical signs evidenced within 24 hours after ingestion of the leaves and death within 48 hours after signs onset. The clinical signs observed in acute poisoning are apathy, anorexia, ruminal arrest, arched back, constipation with feces in small spheres, sometimes covered with mucus and blood streaks, muscle tremors, staggering gait and sometimes sialorrhoea. Neurological signs may be observed, due to interference in the urea cycle due to hepatic insufficiency resulting in hyperammonemia (hepatic encephalopathy). The main pathological finding is centrilobular hepatic necrosis. The toxic principle present in C. axillare was not yet definitively proven, but some authors attribute the toxicity of the plant to the presence of saponins gitogenin and digitogenin. However, it has not been determined whether the saponins present in C. axillare are responsible for the hepatotoxic effect of the plant. Thus, the objective of this work is to determine if the saponins are the compounds responsible for the hepatotoxic effects produced by the ingestion of the leaves of C axillare, using goats as experimental model. For this, the effects of the administration of the leaves were compared with those produced by the saponins isolated from the leaves in goats. Six goats were randomly assigned to three experimental groups that received [1] dry leaves of C. axillare (animals A1 and A2), [2] saponins extract from leaves (animals S1 and S2) or [3] control group (animals C1 and C2). For goats receiving the dry leaves the administered dose of plant was 10g/kg for one animal (A1) and 5g/kg for the other one (A2). For animals receiving the saponins extract, administration was done at a dose equivalent to 20g/kg repeated after 24 hours. The dry leaves administered at a dose of 10g/kg to a goat produced toxic effects, with alterations in biochemistry (indicating hepatic lesion) and histopathology showing centrilobular hepatic necrosis. At the dose of 5 g/kg of dry leaves, clinical signs of poisoning were not observed, but hepatic necrosis was found; after 15 days after the last administration, the hepatic parenchyma of this animal was already normal, with only hemorrhagic areas, demonstrating full regeneration. The administration of extracts of saponins containing gitogenin and digitogenin to goats did not produce significant toxic effects, proving that these compounds are not responsible for intoxication. In addition, goats are a good experimental model for studies of this intoxication.(AU)

Cestrum axillare Vell. (anteriormente C. laevigatum Schltd.), família Solanaceae, é a mais importante planta hepatotóxica do Brasil que causa intoxicação aguda. Tem ocorrência nas regiões Sudeste e Centro-Oeste e em áreas litorâneas do Nordeste. A intoxicação natural foi descrita em bovinos, caprinos e ovinos, com sinais clínicos evidenciados em até 24 horas após a ingestão das folhas e morte em até 48 horas após o início da sintomatologia. Os sinais clínicos observados na intoxicação aguda são apatia, anorexia, parada ruminal, dorso arqueado, constipação com fezes em formas de pequenas esferas, por vezes recobertas com muco e com estrias de sangue, tremores musculares, andar cambaleante e, às vezes, sialorreia. Podem ser observados sinais neurológicos, devido à interferência no ciclo da ureia pela insuficiência hepática resultando em hiperamonemia (encefalopatia hepática). O principal achado patológico é a necrose hepática centrolobular. O princípio tóxico presente no C. axillare ainda não está definitivamente comprovado, mas alguns autores atribuem a toxicidade da planta à presença das saponinas gitogenina e digitogenina. No entanto, ainda não foi determinado se as saponinas presentes em C. axillare são as responsáveis pelo efeito hepatotóxico da planta. Assim, o objetivo deste trabalho é determinar se as saponinas são os compostos responsáveis pelos efeitos hepatotóxicos produzidos pela ingestão das folhas de C. axillare, usando caprinos como modelo experimental. Para isto, foram comparados os efeitos da administração das folhas com os produzidos pelas saponinas isoladas destas folhas em caprinos. Foram utilizados seis caprinos, distribuídos aleatoriamente em três grupos experimentais que receberam [1] folhas secas de C. axillare (Caprinos A1 e A2), [2] extrato de saponinas das folhas (Caprinos S1 e S2), e [3] grupo controle (Caprinos C1 e C2). Para os caprinos que receberam as folhas secas a dose administrada de planta foi de 10g/kg para um animal (A1) e de 5g/kg para outro (A2). Para os animais que receberam o extrato de saponinas, a administração foi feita na dose equivalente a 20g/kg, repetida após 24 horas. Foi verificado que as folhas secas, quando administradas na dose de 10g/kg a um caprino, produziram efeitos tóxicos, com alterações na bioquímica (indicando lesão hepática) e histopatológica apresentando necrose hepática centrolobular. Na dose de 5g/kg de folhas secas, não foi observado sintomatologia clínica da intoxicação, mas houve necrose hepática; 15 dias após a última administração, o parênquima hepático deste animal já se encontrava normal, apenas com áreas hemorrágicas, demonstrando plena regeneração. A administração do extrato de saponinas contendo gitogenina e digitogenina a caprinos não produziu efeitos tóxicos significantes, comprovando não serem estes compostos os responsáveis pela intoxicação. Além disto, a espécie caprina é um bom modelo experimental para estudos desta intoxicação.(AU)

Antitumor and anti-angiogenic potentials of isolated crude saponins and various fractions of Rumexhastatus D. Don

BACKGROUND: Cancer, being the foremost challenge of the modern era and the focus of world-class investigators, gargantuan research is in progress worldwide to explore novel therapeutic for its management. The exploitation of natural sources has been proven to be an excellent approach to treat or minify the excessive angiogenesis and proliferation of cells. Similarly, based the ethnomedicinal uses and literature survey, the current study is designed to explore the anti-tumor and anti-angiogenic potentials of Rumex hastatus. Anti-tumor and anti-angiogenic activities were carried out using potato-disc model and chorioallantoic membrane (CAM) assay respectively. Moreover, R. hastatus was also assessed for antibacterial activity against Agrobacterium tumefaciens (tumor causing bacterial strain). The positive controls used in anti-tumor, anti-angiogenic and antibacterial activities were vincristine sulphate, dexamethasone and cefotaxime respectively. RESULTS: The crude saponins (Rh.Sp), methanolic extract (Rh.Cr) and other solvent extracts like n-hexane (Rh.Hex), chloroform (Rh.Chf), ethylacetate (Rh.EtAc) and aqueous fraction (Rh.Aq) exhibited notable anti-tumor and anti-angiogenic activities. In potato tumor assay, the chloroform and saponin fractions were observed to be the most effective showing 86.7 and 93.3 % tumor inhibition at 1000 µg/ml with IC50 values 31.6 and 18.1 µg/ml respectively. Similarly, these two samples i.e., chloroform and saponins also excelled among the entire test samples in anti-angiogenic evaluation exhibiting 81.6 % (IC50 = 17.9 µg/ml) and 78.9 % (IC50 = 64.9 µg/ml) at 1000 µg/ml respectively. In contrast, the antibacterial investigations revealed a negligible potential against A. tumefaciens. CONCLUSION: Based on our results we can claim that R. hastatus possesses both anti-tumor and anti-angiogenic potentials. In all of the solvent fractions, Rh.Chf and Rh.Sp were most effective against tumor and angiogenesis while having negligible activity against A. tumefaciens. It can be concluded that Rh.Chf and Rh.Sp might be potential targets in the isolation of natural product having anti-neoplastic action.

Anticholinesterse and antioxidant investigations of crude extracts, subsequent fractions, saponins and flavonoids of atriplex laciniata L: potential effectiveness in Alzheimer's and other neurological disorders

BACKGROUND: Atriplex laciniata L. was investigated for phenolic, flavonoid contents, antioxidant, anticholinesterase activities, in an attempt to explore its effectiveness in Alzheimer's and other neurological disorders. Plant crude methanolic extract (Al.MeF), subsequent fractions; n-hexane (Al.HxF), chloroform (Al.CfF), ethyl acetate (Al.EaF), aqueous (Al.WtF), Saponins (Al.SPF) and Flavonoids (Al.FLVF) were investigated for DPPH, ABTS and H2O2 free radical scavenging activities. Further these extracts were subjected to acetylcholinesterase (AChE) & butyrylcholinesterase (BChE) inhibitory activities using Ellman's assay. Phenolic and Flavonoid contents were determined and expressed in mg Gallic acid GAE/g and Rutin RTE/g of samples respectively. RESULTS: In DPPH free radicals scavenging assay, Al.FLVF, Al.SPF and Al.MeF showed highest activity causing 89.41 ± 0.55, 83.37 ± 0.34 and 83.37 ± 0.34% inhibition of free radicals respectively at 1 mg/mL concentration. IC50 for these fractions were 33, 83 and 82 µg/mL respectively. Similarly, plant extracts showed high ABTS scavenging potential, i.e. Al.FLVF (90.34 ± 0.55), Al.CfF (83.42 ± 0.57), Al.MeF (81.49 ± 0.60) with IC50 of 30, 190 and 70 µg/ml respectively. further, H2O2 percent scavenging was highly appraised in Al.FLVF (91.29 ±0.53, IC50 75), Al.SPF (85.35 ±0.61, IC50 70) and Al.EaF (83.48 ± 0.67, IC50 270 µg/mL). All fractions exhibited concentration dependent AChE inhibitory activity as; Al.FLVF, 88.31 ± 0.57 (IC50 70 µg/mL), Al.SPF, 84.36 ± 0.64 (IC50 90 µg/mL), Al.MeF, 78.65 ± 0.70 (IC50 280 µg/mL), Al.EaF, 77.45 ± 0.46 (IC50 270 µg/mL) and Al.WtF 72.44 ± 0.58 (IC50 263 µg/mL) at 1 mg/mL. Likewise the percent BChE inhibitory activity was most obvious in Al.FLVF 85.46 ± 0.62 (IC50 100 µg/mL), Al.CfF 83.49 ± 0.46 (IC50 160 µg/mL), Al.MeF 82.68 ± 0.60 (IC50 220 µg/mL) and Al.SPF 80.37 ± 0.54 (IC50 120 µg/mL). CONCLUSIONS: These results stipulate that A. laciniata is enriched with phenolic and flavonoid contents that possess significant antioxidant and anticholinestrase effects. This provide pharmacological basis for the presence of compounds that may be effective in Alzheimer's and other neurological disorders.

Investigations of anticholinestrase and antioxidant potentials of methanolic extract, subsequent fractions, crude saponins and flavonoids isolated from Isodon rugosus

BACKGROUND: Based on the ethnomedicinal uses and the effective outcomes of natural products in various diseases, this study was designed to evaluate Isodon rugosus as possible remedy in oxidative stress, alzheimer's and other neurodegenerative diseases. Acetylecholinestrase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of crude methanolic extract (Ir.Cr), resultant fractions (n-hexane (Ir.Hex), chloroform (Ir.Cf), ethyl acetate (Ir.EtAc), aqueous (Ir.Aq)), flavonoids (Ir.Flv) and crude saponins (Ir.Sp) of I. rugosus were investigated using Ellman's spectrophotometric method. Antioxidant potential of I. rugosus was determined using DPPH, H2O2 and ABTS free radicals scavenging assays. Total phenolic and flavonoids contents of plant extracts were determined and expressed in mg GAE/g dry weight and mg RTE/g of dry sample respectively. RESULTS: Among different fractions Ir.Flv and Ir.Cf exhibited highest inhibitory activity against AChE (87.44 ± 0.51, 83.73 ± 0.64%) and BChE (82.53 ± 0.71, 88.55 ± 0.77%) enzymes at 1 mg/ml with IC50 values of 45, 50 for AChE and 40, 70 µg/ml for BChE respectively. Activity of these fractions were comparable to galanthamine causing 96.00 ± 0.30 and 88.61 ± 0.43% inhibition of AChE and BChE at 1 mg/ml concentration with IC50 values of 20 and 47 µg/ml respectively. In antioxidant assays, Ir.Flv, Ir.Cf, and Ir.EtAc demonstrated highest radicals scavenging activities in DPPH and H2O2 assays which were comparable to ascorbic acid. Ir.Flv was found most potent with IC50 of 19 and 24 µg/ml against DPPH and H2O2 radicals respectively. Whereas antioxidant activates of plant samples against ABTS free radicals was moderate. Ir.Cf, Ir.EtAc and Ir.Cr showed high phenolic and flavonoid contents and concentrations of these compounds in different fractions correlated well to their antioxidant and anticholinestrase activities. CONCLUSION: It may be inferred from the current investigations that the Ir.Sp, Ir.Flv and various fractions of I. rugosus are good sources of anticholinesterase and antioxidant compounds. Different fractions can be subjected to activity guided isolation of bioactive compounds effective in neurological disorders.

Toxicity of saponin isolated from Gymnema sylvestre R. Br. (Asclepiadaceae) against Culex tritaeniorhynchus Giles (Diptera: Culicidae) Japanese encephalitis vector mosquito in India / Toxicidade da saponina isolada de Gymnema sylvestre R. Br. (Asclepiadaceae) contra Culex tritaeniorhynchus Giles (Diptera: Culicidae) mosquito vetor da encefalite japonesa na Índia

To determine the larvicidal activity of various extracts of Gymnema sylvestre against the Japanese Encephalitis vector, Culex tritaeniorynchus in Tamilnadu, India. To identify the active principle present in the promising fraction obtained in Chlorofom:Methanol extract of Fraction 2. The G. sylvestre leaf extracts were tested, employing WHO procedure against fourth instar larvae of C. tritaeniorhynchus and the larval mortalities were recorded at various concentrations (6.25, 12.5, 25.0, 50 and 100 µg/mL); the 24h LC50 values of the G. Sylvestre leaf extracts were determined following Probit analysis. It was noteworthy that treatment level 100 µg/mL exhibited highest mortality rates for the three different crude extracts and was significantly different from the mean mortalities recorded for the other concentrations. The LC50 values of 34.756 µg/mL (24.475-51.41), 31.351 µg/mL (20.634-47.043) and 28.577 µg/mL (25.159-32.308) were calculated for acetone, chloroform and methanol extract with the chi-square values of 10.301, 31.351 and 4.093 respectively. The present investigation proved that G. Sylvestre could be possibly utilized as an important component in the Vector Control Program.

O presente trabalho é para identificar a atividade larvicida de vários extratos da Gymnema sylvestre contra o vetor da encefalite japonesa, Culex tritaeniorhynchus em Tamilnadu, Índia. Com este propósito o princípio ativo presente na fração mais promissora foi obtida através de um extrato clorofórmio:metanol da fração 2. Os extratos das folhas do G. sylvestre foram testados empregando o procedimento da WHO contra estágios quaternários da larva do C. tritaeniorhynchus e as mortalidades larvais foram registradas após várias concentrações (6,25, 12,5, 25,0 e 100; 34,756 µg/mL (24,475-51,41), 31,351 µg/mL (20,634-47,043) e 28,577 µg/mL (25,159-32,308) g/mL); os valores de LC50 de 24 horas dos extratos das folhas de G. sylvestre foram determinados seguindo a análise Probit. Foi notado que o nível de tratamento de 100 µg/mL exibiu a mortalidade mais alta para os três diferentes extratos crus e foi significantemente diferente das mortalidades médias registradas para as outras concentrações. Os valores de LC50 de 34,756 µg/mL (24,475-51,41), 31,351 µg/mL (20,634-47,043) e 28,577 µg/mL (25,159-32,308) foram calculados para os extratos de acetona, clorofórmio e metanol com os valores de qui-quadrado de 10,301, 31,351 e 4,093 respectivamente. A presente investigação mostra que o G. sylvestre pode ser usado como componente importante no programa de controle do vetor.

Saponinas esteroidales de la planta Agave brittoniana (Agavaceae) con actividad contra el parásito Trichomona vaginalis

Steroidal saponins from the plant Agave brittoniana with activity against the parasite Trichomona vaginalis. The genus Agave (Agavaceae), includes more than 300 species; around 16 of them show an homogeneous distribution throughout Cuba. Agave brittoniana (ssp. brachypus), is an endemic subspecies that grows in the central region of the country and its leaves are traditionally used in the treatment of parasitic diseases. The parasite Trichomonas vaginalis causes the disease known as trichomoniasis, that infects the genital tract. To test in vitro the plant against Trichomona vaginalis, the dried and powdered leaves were extracted three times with ethanol-water (7 : 3) by maceration at room temperature. The solvent was removed under reduced pressure and the extract was suspended in distilled water, defatted with n-hexane, and extracted with water-saturated n-butanol. After solvent removal, a portion of the n-butanol extract was hydrolyzed. After extraction with ethyl acetate the hydrolysis products were compared with authentic sapogenins samples using thin layer chromatography (TLC). Most of the sapogenins (yuccagenin and diosgenin) were isolated and their structures were confirmed. using nuclear magnetic resonance (NMR) experiments. The n-butanol extract was subjected to a separation process through column chromatography to obtain five fractions. After multiple separation processes by reversed phase high performance liquid chromatography (HPLC), the most active one produced one refined fraction that contained two saponins with the same aglycone (diosgenin) and one yuccagenin based saponin. Best results of the activity were obtained with the yuccagenin derived glycoside. Rev. Biol. Trop. 56 (4): 16451652. Epub 2008 December 12.

El género Agave, familia Agavaceae, tiene más de 300 especies, con aproximadamente 16 distribuidas en toda Cuba. Una de ellas, el Agave brittoniana Trel. (ssp. brachypus), es una subespecie endémica y sus hojas son tradicionalmente utilizadas en el tratamiento de enfermedades parasitarias. Se realizaron estudios "in vitro" de la actividad de productos de esta planta frente a Trichomona vaginalis. Las hojas secas y pulverizadas fueron extraídas tres veces con una mezcla de etanol-agua (7: 3) mediante maceración a temperatura ambiente. El disolvente fue evaporado a presión reducida y el extracto fue suspendido en agua destilada, desengrasado con n-hexano, y extraído con n-butanol saturado con agua. Luego de una extracción con acetato de etilo, los productos de la hidrólisis fueron comparados con patrones de sapogeninas mediante la cromatografía de capa fina (CCD). Aislamos las sapogeninas mayoritarias (yuccagenina y diosgenina) y confirmamos sus estructuras utilizando técnicas de resonancia magnética nuclear. Por otra parte, el extracto n-butanólico fue sometido a un proceso de separación biodirigido mediante cromatografía de columna, obteniéndose cinco fracciones. Después de múltiples separaciones, la más activa rindió una fracción purificada con dos sapogeninas con el mismo aglicón (diosgenina) y un glicósido de yucagenina. Los mejores resultados de esta actividad fueron obtenidos con el glicósido derivado de la yucagenina.

Molluscicidal saponins from leaves of Hedera canariensis

Activity-guided fractionation of the methanol extract of Hedera canariensis [var. Gloire de Maringo] Wild leaves afforded five saponins 1-5. Chemical and spectral methods [MS, [1]HNMR, [13]CNMR] showed that they are glycosides of hederagenin and oleanolic acid. The results showed that 4,5 exhibited molluscicidal properties, compound 1 was inactive. Mortality rate of exposed snails increased by increasing plant extract concentration. Lymnaea cailliaudi was more sensitive to plant extract than Biomphalaria alexandrina. The histopathological study revealed distinct damage in the structure of the stomach and ovotestis of treated L. cailliaudi snails. Saponin content was determined in term of haemolytic index

Antifungal activity of the extracts and saponins from Sapindus saponaria L

Extracts from the dried pericarp of Sapindus saponaria L. (Sapindaceae) fruits were investigated for their antifungal activity against clinical isolates of yeasts Candida albicans and C. non-albicans from vaginal secretions of women with Vulvovaginal Candidiasis. Four clinical isolates of C. albicans, a single clinical isolated of each of the species C. parapsilosis, C. glabrata, C. tropicalis, and the strain of C. albicans ATCC 90028 were used. The hydroalcoholic extract was bioactivity-directed against a clinical isolate of C. parapsilosis, and showed strong activity. The n-BuOH extract and one fraction showed strong activity against all isolates tested. Further column-chromatography on silica gel separation of this fraction afforded two pure triterpene acetylated saponins: 3-O-(4-acetyl-beta-D-xylopyranosyl)-(1->3)-alpha-Lrhamnopyranosyl-(1->2)-alpha-L-arabinopyranosyl-hederagenin (1) and 3-O-(3,4-di-acetyl-beta-D-xylopyranosyl)-(1->3)-alpha-L-rhamnopyranosyl-(1->2)-alpha-L-arabynopyranosyl-hederagenin (2). The structures of the compounds were based on spectral data (¹H and 13C NMR, HSQC, HMBC and MS), and on with literature. The saponins isolated showed strong activity against C. parapsilosis.

Extratos do pericarpo de frutos de Sapindus saponaria L. (Sapindaceae) foram testados para a atividade antifúngica sobre isolados clínicos de leveduras de Candida albicans e C. não-albicans obtidos de secreção vaginal de mulheres com Candidíase Vulvovaginal. Foram avaliados quatro isolados clínicos de C. albicans, um de cada uma das espécies C. glabrata, C. parapsilosis, C. tropicalis e uma cepa referência de C. albicans ATCC 90028. O extrato hidroalcoólico foi biomonitorado contra um isolado clínico de C. parapsilosis, apresentando forte atividade. O extrato butanólico e uma fração apresentaram forte atividade contra todos os isolados testados. Posterior análise desta fração via cromatografia em sílica gel (CHCl3:CH3OH, 1:1, v/v) resultou no isolamento de duas saponinas triterpênicas puras mono e diacetiladas, 3-O-(4-O-acetil-O-beta-D-xilopiranosil)-(1 -> 3)-alfa-L-ramnopiranosil-(1 -> 2)-alfa-L-arabinopiranosil-hederagenina (1) e 3-O-(3,4-di-O-acetil-beta-D-xilopiranosil)-(1 -> 3)-alfa-L-ramnopiranosil-(1 -> 2)-alfa-L-rabinopiranosil-hederagenina (2) respectivamente. A elucidação estrutural das substâncias foi baseada em dados espectrais (RMN de ¹H e de 13C, HSQC, HMBC, ESI/MS) e comparados com dados da literatura. As saponinas triterpênicas isoladas (1) e (2) apresentaram forte atividade contra C. parapsilosis.

In vitro and in vivo antilithiasic effect of saponin rich fraction isolated from herniaria hirsuta / Efeito anti-litiásico, in vitro e in vivo, da fração rica em saponinas extraída da herniaria hirsuta

Accumulated evidence from experiments conducted in vitro and in vivo favors a beneficial effect of the aqueous extract of Herniaria hirsuta in the preventionand cure of urolithiasis. In the current study, we attempted an initial fractionation of the methanol extract of the plant bio-guided by in vitro and in vivocrystallization assays to determine the nature of compound responsible for the beneficial effect of the plant. A ground plant sample was sequentiallysubmitted to ether and methanol extraction by soxhlet apparatus. Methanolic part was further purified by silica gel chromatography using a series of organicsolvents with different increasing polarity. The fractions were then assayed on calcium oxalate crystallization in vitro and in vivo models. In the whole humanurine, only the fraction eluted with ethanol/water was associated to formation of smaller crystals composed of calcium oxalate dihydrate, similarly to theaqueous extract. When tested at 5 mg/day, it reduced significantly crystal deposition in lithiasic rats. Preliminary identification of plant compound found inthat fraction showed the presence of saponins. We conclude that saponins may be responsible for the beneficial effect of Herniaria hirsuta in the treatmentof kidney stones.

A evidência acumulada por resultados de experimentos conduzidos in vitro e in vivo é favorável a uma ação benéfica do extrato aquoso da Herniaria hirsutana prevenção e cura da urolitíase. No presente estudo, nós nos propusemos a fazer um fracionamento inicial do extrato metanólico da planta,biologicamente guiado por ensaios de cristalização in vivo e in vitro, na tentativa de determinar a natureza do composto responsável pelo efeito benéficoda planta. A planta moída foi submetida seqüencialmente à extração por éter e metanol pelo equipamento "soxhlet". A porção metanólica foi adicionalmentepurificada por cromatografia em gel de sílica empregando uma série de solventes orgânicos de polaridade crescente. As frações foram então testadas emmodelos de cristalização de oxalato de cálcio in vivo e in vitro . Nos testes com urina humana total, somente a fração eluída com etanol/água esteveassociada a cristais menores, compostos de oxalato de cálcio di-hidratado, em similaridade com o extrato aquoso. Quando testada na dose de 5mg/dia,uma redução significativa na deposição de cristais foi observada em ratos litiásicos. Uma identificação preliminar dos compostos contidos naquela fraçãorevelou a presença de saponinas. Nós concluímos que saponinas podem ser responsáveis pelos efeitos benéficos da Herniaria hirsuta no tratamento decálculos renais.

Isolation of a new triterpenoid saponin from the root of Anchusa Strigosa L., family Boraginaceae

It was isolated a new triterpenoidsaponin from the root of plant Anchusa Strigosa L. family Boraginaceae The plant Anchusa is widely spread in different places in Syria, and it is used in treatment of some diseases like oedema, and fever and pulmonary diseases. The isolation and purification procedures was performed using thin layer chromatography TLC and column chromatography CC and high performance liquid chromatography HPLC and by using the methods of nuclear magnetic resonance chromatography NMR it was determined the chemical structure of the aglycon as triterpenoid linked by glycoside bond with three sugar parts

Cholesterol-dependent hemolytic activity of Passiflora quadrangularis leaves

Plants used in traditional medicine are rich sources of hemolysins and cytolysins, which are potential bactericidal and anticancer drugs. The present study demonstrates for the first time the presence of a hemolysin in the leaves of Passiflora quadrangularis L. This hemolysin is heat stable, resistant to trypsin treatment, has the capacity to froth, and acts very rapidly. The hemolysin activity is dose-dependent, with a slope greater than 1 in a double-logarithmic plot. Polyethylene glycols of high molecular weight were able to reduce the rate of hemolysis, while liposomes containing cholesterol completely inhibited it. In contrast, liposomes containing phosphatidylcholine were ineffective. The Passiflora hemolysin markedly increased the conductance of planar lipid bilayers containing cholesterol but was ineffective in cholesterol-free bilayers. Successive extraction of the crude hemolysin with n-hexane, chloroform, ethyl acetate, and n-butanol resulted in a 10-fold purification, with the hemolytic activity being recovered in the n-butanol fraction. The data suggest that membrane cholesterol is the primary target for this hemolysin and that several hemolysin molecules form a large transmembrane water pore. The properties of the Passiflora hemolysin, such as its frothing ability, positive color reaction with vanillin, selective extraction with n-butanol, HPLC profile, cholesterol-dependent membrane susceptibility, formation of a stable complex with cholesterol, and rapid erythrocyte lysis kinetics indicate that it is probably a saponin.

Actividad biológica de las saponinas de la corteza de Inga marginata Willd / Biological activity of saponins from the bark of Inga marginata Willd

La corteza de Inga marginata Willd. contiene saponinas, taninos, fitosteroles y triterpenoides. Por cromatografía de capa delgada (CCD) se encontraron 5 saponinas. Con el extracto etanólico y las saponinas crudas se realizaron ensayos para determinar su actividad antibacteriana y antifúngica, farmacológica con ratas Wistar y ratones OF-1, e ictiotóxica sobre el pez Guppy Poecilia reticulata Peters. Las saponinas de la corteza poseen actividad depresora sobre el SNC en ratas y ratones. La actividad contra bacterias es baja mientras que contra hongos es manifiesta. Las saponinas inhiben el crecimiento de tumores en los discos de zanahoria en un 99 porciento. Son tóxicas para el pez Guppy (Poecilia rericulata), CL50 a 96h: 5,5 mg/L

Obtención de crudos de saponinas hipocolesteromizantes del Chenopodium Quinoa Willd / Obtention of crudes of saponins from chenopodium quinoa willd as anticholesteraemia agents

Para su empleo como agente hipocolesteromizante, se procedió a la obtención de crudos de saponinas a partir de la cascarilla de Chenopodium quinoa willd (quinúa), mediante reflujo con etanol al 80 por ciento v/v. Los diferentes lotes de saponinas brutas obtenidos presentaron un rendimiento promedio de 37,12 por ciento, sobre la base del total de cascarilla (8,03 por ciento de la masa de granos) y de 2,98 por ciento sobre la base del total de granos. Estos productos reaccionaron fuertemente en las pruebas de Liebermann-Burchard y Selivoflo, y su potencia hemolítica (H50 en µg/mL) se enmarcó en un recorrido de 42,6 hasta 28,4. Seis muestras de crudos fueron sometidas a saponificación sin que se observaron cambios notables en la potencia hemolítica de los productos saponificados (H50 entre 37,2 y 22,7). Este hecho, unido a que el total de los crudos obtenidos manifestaron una reacción negativa en las pruebas de Fehling y Molish. Sugieren que los productos obtenidos se encuentran en forma de sapogeninas u otros derivados "no saponificables"

Investigation of saponin content and lipoidal matter in two aerva species growing in Egypt

The study included the investigation of saponin contents in Aerva lanata [L.] Juss ex. Schult and Aerva javanica [Burm. fil] growing in Egypt. The crude saponin mixture was prepared and purified by MgO method, further purification of the isolates was carried out by column chromatography followed by centrifugally accelerated rotatory TLC. Three glycosides were isolated. Hydrolysis of glycoside 1 afforded beta-sitosterol and glucose, saponin glycoside, yielded lupeol, galactose and glucose, while saponin glucoside, gave oleanolic acid, galactose, glucose and rhamnose. The genins were identified on the basis of mp, mmp, chromatographic behavior IR, 1HMR and EI-mass spectra. The sugar moieties of the glycosides were identified by PC and GLC analysis. Quantitative estimation of saponin applying the hemolytic index method revealed that it is higher in A. javanica [0.09%] than in A. lanata [0.014%]. Identification of the hydrocarbons, sterols and triterpenes was achieved by chromatographic as well as GC-MS analysis. beta-Sitosterol, campesterol, stigmasterol, stigmasterol acetate and lupeol were identified in both species. Olean-12-en-28 oic acid 3,16 dioxomethyl ester and ergosterol were identified in A. lanata, while oleanolic acid methyl ester was identified only in A. javanica. The total fatty acids of the two species were methylated and analyzed by GLC. The results revealed the presence of lauric, myristic, myrstoleic, palmitolleic, stearic, oleic and linoleic acids in the two aerva species. Palmitic acid was found only in A. javanica

Relación estructura actividad de saponinas con efecto molusquicida / The activity interaction of saponins and mollusquicidal effects

The interactions between mollusquicidal saponins and membrane phospholipids have been investigated using physicochemical calculations and molecular graphics, and liposome and monolayer studies. It is clear that the membrane modifying action of saponins is a subtle process involving precise sites of interaction

Antimicrobial activity of Nigella sativa and Zingber officinal

Aqueous and ethanolic extracts of Zingber officinale had antimicrobial activity against large number of pathogenic bacteria and fungi. Aqueous extract of Nigella sativa possessed antibacterial activity in higher concentration. In addition, all fractions of both Zingber officinale and Nigella sativa exhibited antimicrobial activities against various microorganisms. Saponin and oil fractions of the test plants increased the antibacterial activity of ampicillin against pyogenic microorganisms, while resin fraction decreased that activity

Extraccion, estudio quimico y determinación de la actividad esparmicida de las saponinas de sapindus saponaria L. (boliche) / Extraction, chemical study and determination of spermicid activity of saponines of sapindus saponaria L. (boliche)

En el presente trabajo se ha realizado la extracción, estudio que por determinación de la actividad espermicida de las saponinas de sapindus saponena L. Boliche. La extracción se llevó a cabo con una macerración previa utilizando una solución hidroalcoholica al 50 porciento luego del desangrado y del despegmentado se extraen las saponinas con n-butonol, obteniendose un rendimiento del 34.08 porciento sobre la muestra deseada. Las saponínas crudas aisladas tienen naturalezas twterpénicos según los procedimientos, estanderes de identificación; el aspecto inflarojo indica que las germinas permanecen al grupo coliano. Los restos azucarados fueron identificados como L (-) ramnosa, L(+) arabinosa y D (+) glucosa utilizando la tecnica cromatográfica en papel. La actividad espermicidad se determino utilizando una modificación de la tecnica de la Baker y del test de Harris, se hallo que las saponinas tiene un primer efecto espermostatico y un posterior efecto espermicida. Tambien se encontró relación en la actividad espermicida y el número de espermatozoides. Los valores de la edad varian según el tiempo de contacto de los espermatozoides con las saponinas.

Neurodepressive action of a piscicidal glycoside of plant, Aesculus indica (Colebr.) in fish.

Sublethal concentration (2.6 mg/l) of a triterpene based piscicidal glycoside of A. indica damaged the neurons, fibre tracts and central correlation sites for gustatory, tactile and visceral sensory impulses in medulla oblongata of fish after prolonged poisoning. The fear, sinking to bottom, lack of schooling and non discriminatory pattern in treated fish were because of neurodepression. The jerky movement, ventilatory inefficiency, swallowing air bubbles and light pinkness of gills were due to the degradation of respiratory centres in the vagal lobes of toxified fish.