Efecto citoprotector y cicatrizante de la Lippia triphylla (Tiquil Tiquil): Taraxacum officinale(Diente de León) y Brassica campestris L.(nabo silvestre) sobre las ulceras Gástricas Experimentales inducidas por etanol en ratas, Arequipa 1995

El presente trabajo demuestra el estudio del efecto citoprotector y cicatrizante de tres plantas utilizadas en el tratamiento de la úlcera gástrica inducidas por etanol de ratas. Las plantas utilizadas fueron: la lippia triphylla "tiquil tiquil" (familia verbenaceae) y la brassica campestris "nabo silvestre" (familia brassicaceae); la primera recolectada en la irrigación Andamayo en el valle de Majes y las otras dos en el distrito de Cerro Colorado. Para el experimento se aplicó el extracto del polvo de las hojas. Las extracciones de los constituyentes químicos fueron obtenidos mediante el método de marcha fitoquímica simplificada. La investigación de principios activos e identificación se hizo mediante reacciones de coloración y pre3cipitación, se logro caracterizar: Sustancias tániucas y saponinas lo que hace suponer que intervienen tanto para el efecto citoprotector como cicatrizante. Se efectuó un ensayo biológico usando la solución del polvo estabilizado de las hojas del tiquil-tiquil, diente de león y del nabo silvestre. Para este ensayo se utilizó ratas albinas machos raza Holtzman aparentemente sanos; en número de 52; los cuales fueron sometidos a un periodo de estandarización en cuanto a las condiciones ambientales y de alimentación, para recientementye administrarles etanol al 45 por ciento y así inducir las lesiones gástricas. Posteriormente, se les administró los extractos acuosos de las plantas de las plantas en estudio con resultados positivos con el grupo control que recibió hidróxido de aluminio y con el grupo de animales que sólo recibieron placebo y ningún tipo de tratamiento. Se encontró similar actividad tanto citoprotectora como cicatrizante en las tres plantas experimentadas.

Effect of aqueous Neem (azadirachta indica) extract on testosterone and other blood constituents in male rats: a pilot study

Effect of oral administration of crude aqueous neem extract on serum testosterone and other blood constituents was studied in the male Wistar rats for 10 weeks. The neem treatment resulted in significant decreases (p,0.01) in total testosterone, total bilirubin and K+ in serum. There were also increases (p<0.05) in packed cell volume, mean corpuscular haemoglobin concentration, red blood cell, white blood cell and lymphocyte counts without showing any cytotoxic effects in the body.

Efeito da temperatura e de ativadores no processo de extracao da bromelina / Effect of temperature and of activators on the extraction process of bromelain

No processo de extracao de bromelina de caules de abacaxi Zeiro ananas comosus cultivar Cayenne, a acetona mostrou menor eficiencia que sulfato e amonio, em relacao ao balanco material. O estudo da estabilidade em diferentes temperaturas, durante 90 dias, das amostras obtidas indicou resultados mais favoraveis na amostra preparada a partir de extrato filtrado a 40 graus centigrados e preciptado por sulfato de amonio

Comportamiento "in vitro" de la spergularia ramosa ("choque takarpo") sobre el mycobacterium tuberculosis / Spergularia ramosa cabessedes in vitro behavior (\"choque takarpo\") with Mycobacterium tuberculosis

Esta investigación sobre propiedades inhibitorias de la planta Spergularia ramosa cabessedes (Choque takarpo) en el crecimiento in vitro del Mycobacterium tuberculosis, demuestra que no cuenta con ningún producto activo en su composición con potencia de inhibir Mycobacterias

Identificacao cromatografica e acao farmacologica de extratos de Styrax camporum Pohl e Caesalpinia ferrea Martius / Chromatographic identification and pharmacologic action of Styrax camporum Pohl and Caesalpina ferrea Martius

As cascas das especies vegetais Styrax camporum Pohl, conhecida popularmente por estoraque do campo ou cuia do brejo, e Caesalpinia ferrea Martius ou pau-ferro, sao ha muito utilizadas em medicina popular como cicatrizantes e no tratamento de ulceras gastroduodenais, recentemente comprovados em trabalhos de experimentacao animal. Em funcao da dificuldade de caracterizacao dos extratos destas especies, foram padronizadas condicoes cromatograficas, que poderao ser uteis em sua identificacao. Tendo em vista que o local da ulceracao encontra-se geralmente inflamado, propoe o presente trabalho verificar se os extratos, alem da acao antiulcera, apresentam tambem acao antiinflamatoria. Como na ulceracao podem estar envolvidos tambem receptores H2 e H1, realizou-se teste de permeabilidade vascular, em que ha envolvimento de histamina, com o objetivo de verificar o possivel mecanismo de acao destes extratos

Evaluation of DNA-binding activity of hydroxyanthraquinones occurring in Rubia tinctorum L.

The naturally-occurring anthraquinones (AQs), alizarin (1,2-dihydroxyanthraquinone) and lucidin (1,3-dihydroxy-2-hydroxymethylanthraquinone), were incubated with DNA in the presence of S9 mix. The isolated DNA was analysed by 32P-postlabelling for the presence of aromatic adducts. Only lucidin formed up to five different DNA adducts in the range from 0.995 to 3.05 adducts/10(8) nucleotides. Lucidin was also incubated with polynucleotides poly[d(A-T)] and polydG*polydC in the presence of S9 mix. Analysis of polydG*polydC revealed a similar adduct pattern to that obtained with lucidin-modified DNA. Alizarin, lucidin, a glycoside mixture containing alizarinprimeveroside and lucidinprimeveroside, and Rubia Teep (a herbal drug made from Rubia tinctorum containing lucidin) were incubated with primary rat hepatocytes for 24 h and the isolated DNA was analysed by 32P-postlabelling. Lucidin, the glycoside mixture and Rubia Teep gave rise to DNA adducts, but alizarin did not. Male Parkes mice were treated orally for 4 days with alizarin (10 mg/d), lucidin (2 mg/d), the glycoside mixture (20 mg/d) or Rubia Teep (1/2 tablet/d) and DNA was isolated from liver, kidney, duodenum and colon. Analysis by 32P-postlabelling revealed that lucidin, the glycoside mixture and Rubia Teep, but not alizarin, formed DNA adducts in all the tissues examined but that the adduct patterns were organ-specific.

[Analysis of volatile oil in pericarpium Zanthoxyli].

Essential oils were extracted from the pericarp of Zanthoxylum bungeanum and Z. schinifolium. The chemical constituents were analysed by means of GC-MS and 33 compounds were identified. Their contents in the essential oil were also determined.

Can ethnopharmacology contribute to the development of antiviral drugs?

In recent years, many compounds having potent antiviral activity in cell cultures and in experimental animals have been detected, but only a few have been approved by Western health authorities for clinical use. Nevertheless, some of these compounds are currently undergoing either preclinical or clinical evaluation, and perspectives for finding new interesting antiviral drugs are promising. Among these antiviral substances are several natural compounds isolated from plants used in traditional medicine including polysaccharides, flavonoids, terpenes, alkaloids, phenolics and amino acids. Some of these plant compounds exhibit a unique antiviral mechanism of action and are good candidates for further clinical research. What follows is a brief summary of the selection methods of plants for antiviral screening and in vitro and in vivo assays, which are currently used for detecting this activity in plant extracts. The importance of the plant kingdom as a source of new antiviral substances will be illustrated by presenting a survey on plant-derived antirhinovirus and anti-HIV agents.

Cytotoxic principles of Securinega virosa: virosecurinine and viroallosecurinine and related derivatives.

Virosecurinine (1) and viroallosecurinine (2) were isolated as two cytotoxic alkaloids from the leaves of Securinega virosa. A comparison of the cytotoxicity of 1 and several of its derivatives indicates that an alpha,beta- and a gamma,delta-unsaturated lactone located in a strained ring system, such as rings -B, -C, and -D of 1, is structurally required for significant cytotoxicity.

Natural products as probes for new drug target identification.

One traditional aspect of natural products in medical research has been their use in the identification and investigation of the physiological/pathological role of receptors and enzymes as possible targets for drug design programmes. Classical examples of this function of natural products in drug research can be seen in the investigation of the cholinergic system. For example, the importance of alkaloids such as nicotine, physostigmine and curare for research into the nicotine receptor and muscarine, pilocarpine and the tropane alkaloids on the muscarinic receptor. On binding of a ligand to its cell surface membrane receptor and prior to a physiological/pharmacological response two mechanisms are currently known to be involved in membrane signal transductance. In the minority of cases signal transductance involves the direct opening of an ion channel, for example sodium ion influx, but in the majority of cases involves stimulation of a family of G-proteins and subsequent activation of second messenger systems. For example, the cyclic-AMP/adenylate cyclase system and the phosphoinositol cycle. In this communication, the part played currently by the tumour-promoting and pro-inflammatory phorbol esters from the plant family Euphorbiaceae in furthering our understanding of the role of a group of related kinases from one arm of the phosphoinositol cycle as a signal transduction pathway will be illustrated. The possibilities of using these new receptors as targets for future drug development will also be described.

A cytotoxic substance from Sangre de Grado.

Taspine has been isolated as a cytotoxic substance from Sangre de Grado, sap of Croton palanostigma (Euphorbiaceae), by bioassay guided fractionation. The cytotoxicity (IC50) of taspine was found to be 0.39 microgram/ml against KB cells and 0.17 microgram/ml against V-79 cells.

Design and synthesis of antitumor compounds based on the cytotoxic diterpenoids from the genus Rabdosia.

Two active sites responsible for antitumor activity, an oxirane ring and an alpha-methylene-cyclopentanone moiety, have been extracted from studies on the structure-activity relationship of the cytotoxic diterpenoids isolated from Rabdosia shikokiana. Series of the simplified cyclopentanone derivatives containing both of the two active sites in the molecule have been synthesized and evaluated for cytotoxicity against P 388 cells. The compounds possessing both of two active sites displayed cytotoxicity at a concentration of 1 microgram/ml, while those possessing a single active site showed no activity.

Structures and cytotoxic activity relationship of casearins, new clerodane diterpenes from Casearia sylvestris Sw.

Casearins G-R, new cytotoxic clerodane diterpenes have been isolated from the leaves of Casearia sylvestris Sw. (Flacourtiaceae). Their structures have been elucidated by spectroscopic methods and chemical conversions, and their structure-activity relationships have been discussed.

Preliminary studies on the antiinflammatory and analgesic activities of Calotropis procera root extract.

A chloroform-soluble fraction from Calotropis procera roots showed significant dose-related antiinflammatory activity in rats using the pharmacologic models of carrageenin-induced pedal oedema, cotton pellet granuloma and formaldehyde-induced arthritis. In addition, significant analgesic potential was demonstrated using acetic acid-induced writhing in mice.

In vitro cytotoxicity of a series of quassinoids from Brucea javanica fruits against KB cells.

A microdilution technique was developed for the assessment of in vitro cytotoxicity against KB cells derived from a human epidermoid carcinoma of the nasopharynx. The test was used to determine the cytotoxicity of a series of quassinoids, isolated from Brucea javanica, and which have previously been shown to demonstrate activity against Plasmodium falciparum. The 50% effective dose (ED50) for 7 quassinoids tested against KB ranged from 0.008 microgram/ml for bruceantin, the most cytotoxic of the compounds tested to greater than 5 micrograms/ml for bruceolide, the least toxic tested. The activities of the quassinoids against KB did not parallel the known activities of the quassinoids against Plasmodium falciparum suggesting that the quassinoid mode of antimalarial action is not a simple cytotoxic effect and lends support to further investigation of the structure activity relationships within this group of compounds.

In vitro activities of acridone alkaloids against Pneumocystis carinii.

Acridone alkaloids isolated from plants of the family Rutaceae have antiplasmodial activity in rodent models of malaria. Because a variety of antimalarial agents have also been shown to have activity against Pneumocystis carinii, we tested six of these alkaloids in an established culture model for P. carinii. Atalaphillinine and glycobismine A inhibited growth of cultured P. carinii at concentrations of 2.7 and 1.7 microM, respectively. This potency of effect is similar to that of chloroquine (3 microM) but somewhat less than that of primaquine (0.4 microM), which was previously evaluated in the same system.

Vasorelaxation of rat thoracic aorta caused by norathyriol isolated from Gentianaceae.

The pharmacological effects of norathyriol on isolated rat thoracic aorta were examined. In the high-K+ (60 mM) medium, Ca2+ (0.03 to 3 mM)-induced vasocontraction was inhibited concentration dependently by norathyriol. Given as pretreatment norathyriol (20 to 200 microM) also inhibited the norepinephrine (NE, 3 microM)-induced tonic contraction. However, the phasic contraction was inhibited only by high concentrations of norathyriol (200 and 400 microM). The tonic contraction elicited by NE was also relaxed by the addition of norathyriol. This relaxing effect of norathyriol was not antagonized by methylene blue (50 microM) or indomethacin (20 microM) and was still seen in denuded rat aorta. Although the cAMP level was not changed by norathyriol, the cGMP level was increased by a high concentration of norathyriol (400 microM). [3H]Inositol monophosphate formation caused by NE was not affected by norathyriol at concentration of either 100 or 400 microM. The 45Ca2+ influx caused by either NE or high K+ was inhibited by norathyriol in a concentration-dependent manner. It is concluded that norathyriol relaxed the rat thoracic aorta mainly by suppressing the Ca2+ influx through both voltage-dependent and receptor-operated calcium channels.

[On the skinning of radix Adenophorae].

Traditional experience calls for the skinning of Radix Adenophorae. Depending on the chemical compositions, this paper presents a comparative study on the skin, the radix with skin and the skinned radix. The experimental results show that the contents of beta-sitosterol, saponins, amino acids and trace elements are highest in the radix with skin, and that the radix with skin and the skinned radix are similar in the contents of polysaccharides.