AMAZON HERB COMPANY

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M Carmen Recio¹, Maite Prieto^1,2, Marina Bonucelli¹, Cecilia Orsi¹, Salvador Máñez¹, Rosa M Giner¹, M. Cerdá-Nicolás³, José-Luis Ríos<sup>1

1</sup> Departament de Farmacologia, Facultat de Farmàcia, Universitat de València, Burjassot, Spain
² Instituto Superior de Ciencias Médicas Carlos J. Finlay, Camagüey, Cuba
³ Departament de Patologia, Facultat de Medicina, Universitat de València, Valencia, Spain

Abstract: Fractionation of an anti-inflammatory extract from Cayaponia tayuya roots yielded two active compounds, identified as 23,24-dihydrocucurbitacin B (1) and cucurbitacin R (2). Both were evaluated for their anti-inflammatory activity on several experimental models of pain and inflammation. In addition, their cytotoxicity and effects on leukotriene B₄ (LTB₄) formation were evaluated in rat polymorphonuclear leukocytes. Both compounds showed activity in the following models: carrageenan-induced mouse paw oedema (1, 4 mg/kg p. o., 46 % inhibition at 3 h), phospholipase A2-induced mouse paw oedema (2, 3 mg/kg i. p., 61 % inhibition at 60 min), serotonin-induced mouse paw oedema (1 and 2, 0.5 mg/kg s. c., 73 % and 79 % inhibition, respectively), 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced acute ear oedema (2, 36 % inhibition at 4 mg/kg p. o., and 87 % inhibition at 0.1 mg/ear topically). The compounds were also active against the inflammation induced by repeated application of TPA on mouse ears, affecting both the oedema itself (1 and 2 at 0.1 mg/ear, 44 % and 56 % inhibition, respectively) as well as cell infiltration (68 % and 69 %, respectively). The activity of both compounds against oedema induced by serotonin was not modified by the glucocorticoid receptor antagonist mifepristone; however, the protein synthesis inhibitor cycloheximide abolished the anti-inflammatory response in both cases. Neither compound modified the production of LTB4 in rat polymorphonuclear leukocytes, nor did they exhibit analgesic properties at the dose assayed.

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Silvia Aquila^{a, b}, Rosa M. Giner^a, María C. Recio^a, Etile D. Spegazzini^b and José Luis Ríos<sup>a

a</sup> Departament de Farmacologia, Facultat de Farmàcia, Universitat de València, Spain
^b Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Argentina

Abstract:

Ethnopharmacological relevance
Taiuiá or tayuya (Cayaponia tayuya, Cucurbitaceae) is a climbing, lignified plant with a large swollen root that has traditionally been used as an anti-inflammatory and anti-rheumatic agent in the folk medicine of Brazil, Peru, and Colombia.

The aim of the study
We have assayed the pharmacological properties of a flavonoid fraction obtained from the butanol extract of Cayaponia tayuya roots using two models of topical mouse ear oedema, paying special attention to its influence on the induction on pro-inflammatory enzymes and peptidic mediators.

Material and methods
The in vivo experiments involved both the acute oedema induced by a single application of TPA and the subchronic inflammation brought on by repeated applications of TPA. The effects on the induction of pro-inflammatory enzymes and peptidic mediators in RAW 264.7 macrophages were analyzed with the aid of Western blot analysis.

Results
The extract was identified as a mixture of flavonoids in which vicenin-2, spinosin, isovitexin, and a mixture of swertisin and isoswertisin were found. In acute TPA-induced oedema in mouse ears, the flavonoid-enriched fraction (at a dose of 0.5 mg/ear) inhibited the oedema by 66% (4.2 ± 0.6 mg vs. 12.3 ± 1.4 mg, P < 0.01) while in the subchronic model, the inhibition reached 37% at a dose of 0.5 mg/ear × 7 applications (7.5 ± 0.6 mg vs. 11.9 ± 1.3 mg, P < 0.05). When assayed in vitro, the flavonoid showed no toxicity at 33.45 µg/mL on RAW 264.7 macrophages. Although the nitric oxide production in these cells was moderately reduced (42%) at 33.45 µg/mL, the flavonoid-enriched fraction had no effect on TNF-a production. In addition, at 22.30 µg/mL, the test sample inhibited both iNOS and COX-2 expression by 98% and 49%, respectively.

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José Miguel Escandell, María-Carmen Recio, Salvador Máñez, Rosa-María Gin, Miguel Cerdá-Nicolás and José-Luis Ríos

^a Departament de Farmacologia, Facultat de Farmàcia, Universitat de València, Av. Vicent Andrés Estellés s/n, 46100 Burjassot, Spain
^b Departament de Patologia, Facultat de Medicina, Universitat de València, Valencia, Spain

Abstract: 23,24-Dihydrocucurbitacin B, from the anti-rheumatic plant Cayaponia tayuya, was tested on arthritis induced by adjuvant to corroborate the anti-inflammatory properties of this plant. Arthritis was induced in Lewis rats; the resulting arthritic rats were then treated with dihydrocucurbitacin B (1 mg/kg orally, daily, 1 week). The effect of dihydrocucurbitacin B on the synthesis, release, and activity of pro-inflammatory enzymes (elastase, cyclooxygenase-2, and nitric oxide synthase-2) as well as its effect on different mediators (tumor necrosis factor-a and interleukin-1ß) were determined. Dihydrocucurbitacin B modified the evolution of the clinical symptoms, reducing the swelling and bone and tissue damage along with the development of the disease, modifying the cell infiltration and the expression of both nitric oxide synthase-2 and cyclooxygenase-2. In addition, it decreased the tumor necrosis factor-a and interleukin-1ß production in lymphocytes, but did not modify it in macrophages.

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Ye YN, Liu ES, Shin VY, Koo MW, Li Y, Wei EQ, Matsui H, Cho CH.


It has been reported that an extract from Angelica sinensis mainly consisting of polysaccharides (95%) prevented ethanol- or indomethacin-induced gastric mucosal damage (Cho CH et al. Planta Med 2000;66:348-51). However, it is not known whether Angelica sinensis has a direct stimulatory effect on the healing of gastric mucosal lesions. To study the hypothesis that Angelica sinensis has a direct mucosal healing effect in rats and in isolated gastric epithelial cells, we assessed the wound repair in both animals and normal cell culture (RGM-1), as well as [3H]thymidine incorporation, ornithine decarboxylase (ODC) activity, and ODC protein and c-Myc protein expression after different treatments in RGM-1 cells. We found that Angelica sinensis crude extract (ASCE) dose-dependently enhanced gastric ulcer healing in rats and promoted wound repair in RGM-1 cells. It also significantly stimulated [3H]thymidine incorporation and ODC activity in RGM-1 cells in a concentration-dependent manner. ODC and c-Myc protein expression was also increased as a result of this process. DL-alpha-difluoromethyl-ornithine repressed the [3H]thymidine incorporation and ODC activity induced by ASCE. Pretreatment with c-Myc antisense oligodeoxynucleotides blocked the stimulatory action of ASCE on [3H]thymidine incorporation and ODC protein expression. These data suggest that ASCE has a direct mucosal healing effect on gastric epithelial cells, while ODC and c-Myc are closely associated with this effect.

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Tona L, Kambu K, Ngimbi N, Mesia K, Penge O, Lusakibanza M, Cimanga K, De Bruyne T, Apers S, Totte J, Pieters L, Vlietinck AJ.


Three major extracts from some traditional preparations, based on medicinal plants, used as antidiarrhoeal agents were investigated for their putative antiamoebic and spasmolytic activities in vitro. Results indicated that both biological activities are concentrated in the polyphenolic fraction, and not in the saponin or alkaloid containing fractions. The most active polyphenolic extracts were those from Euphorbia hirta whole plant, leaves of Alchornea cordifolia, Crossopteryx febrifuga, Nauclea latifolia, Psidium guajava, Tithonia diversifolia, stem bark of Harungana madagascariensis, Mangifera indica, Maprounea africana and Psidium guajava, inhibiting Entamoeba histolytica growth with MAC < 10 micrograms/ml. The same extracts, at a concentration of 80 micrograms/ml in an organ bath, also exhibited more than 70% inhibition of acetylcholine and/or KCl solution-induced contractions on isolated guinea-pig ileum.

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Ruppelt BM, Pereira EF, Gonçalves LC, Pereira NA.


We have observed that several plants used popularly as anti-snake venom show anti-inflammatory activity. From the list prepared by Rizzini, Mors and Pereira some species have been selected and tested for analgesic activity (number of contortions) and anti-inflammatory activity (Evans blue dye diffusion--1% solution) according to Whittle's technique (intraperitoneal administration of 0.1 N-acetic acid 0.1 ml/10 g) in mice. Previous oral administration of a 10% infusion (dry plant) or 20% (fresh plant) corresponding to 1 or 2 g/kg of Apuleia leiocarpa, Casearia sylvestris, Brunfelsia uniflora, Chiococca brachiata, Cynara scolymus, Dorstenia brasiliensis, Elephantopus scaber, Marsypianthes chamaedrys, Mikania glomerata and Trianosperma tayuya demonstrated analgesic and/or anti-inflammatory activities of varied intensity.

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Huguet AI, Máñez S, Alcaraz MJ.


The superoxide anion scavenging activity of 38 flavonoids, some of them isolated from Sideritis mugronensis, Sideritis javalambrensis and Cayaponia tayuya were investigated by measurement of their inhibition of nitroblue tetrazolium reduction. Isoorientin, orientin, amentoflavone, leucocyanidol, eriodictyol, datiscetin and robinetin behaved as potent scavengers and structure-activity relationships were established.

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P. O. Osadebe and F. B. C. Okoye

Department of Pharmaceutical Chemistry, Faculty of Pharm. Sciences, University of Nigeria, Nsukka, Nigeria

Abstract: The leaves of Alchornea cordifolia were collected, identified, dried, and reduced to coarse powder and extracted with aqueous methanol. Using various solvent treatments, the powdered dried leaf was fractionated into five fractions, A1, A2, B, C, D and E. The fractions were subjected to phytochemical analysis to identify the biologically active constituents. The anti-inflammatory effects of crude methanolic extract (ME) of Alchornea cordifolia leaves and the five fractions were evaluated using egg-albumen-induced rat hind paw oedema as a model of inflammation. The crude extract was also subjected to acute toxicity test. Fraction A2, which exhibited the most promising anti-inflammatory effect, was also subjected to analgesic and ulcerogenic tests. Phytochemical analysis of the extracts showed the presence of terpenes, sterols, flavonoids, tannins, carbohydrates, glycosides, saponins and traces of alkaloids. The LD50 of the aqueous ME was found to be 1131.4 mg/kg. The crude ME (50 mg/kg) gave anti-inflammatory activity which was significant (P<0.05) at all the observation times (1–3 h). The different solvent fractions exhibited varying degrees of anti-inflammatory activities, with terpenoid fraction (A2) and the tannin-containing multi-component fraction (D) showing very high and significant (P<0.01) activity at 100 mg/kg, with percentage inhibition of oedema value of 87.69 each. In conclusion, the aqueous ME of Alchornea cordifolia leaves could be beneficial in the management of different inflammatory disease states. Its anti-inflammatory activity may not be attributed only to the terpenoid content.

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Klaus Keplinger, Gerhard Laus, Martin Wurm, Manfred P. Dietrich, Herwig Teppner, Institut fur Hygiene und Ludwig Boltzmann-Institut for AIDS Forschung

Abstract: The medicinal system of the Asháninka Indians in Perú is portrayed. Three categories of medical disorders and healers are recognized. A human is viewed to consist of a physical and a spiritual being who communicate with each other by means of a regulating element. The significance of Uncaria tomentosa (Willd.) DC. (Rubiaceae), locally known as uña de gato, in traditional medicine is emphasized by its exclusive use by priests to influence this regulation. Pharmacological and toxicological results obtained with extracts or isolated compounds are summarized. Pentacyclic oxindole alkaloids stimulate endothelial cells in vitro to produce a lymphocyte-proliferation-regulating factor. Tetracyclic oxindole alkaloids act as antagonists. A significant normalization of lymphocyte percentage was observed in vivo although total leucocyte numbers did not change.