Safflower Oil: An Integrated Assessment Of Phytochemistry, Antiulcerogenic Activity, And Rodent And Environmental Toxicity

Gastric ulcers are a significant medical problem and the development of complications lead to significant mortality rates worldwide. In Brazil, Carthamus tinctorius L., Asteraceae, seeds essential oil, the safflower oil, is currently used as a thermogenic compound and as treatment for problems related to the cardiovascular system. In this study, by Raman spectroscopy, it was shown that oleic and linoleic acids are the compounds present in higher concentrations in the safflower oil. We demonstrated that safflower oil (750 mg/kg, p.o.) decrease the ulcerogenic lesions in mice after the administration of hydrochloric acid-ethanol. The gastric ulcers induced by non-steroidal anti-inflammatory drug (NSAID) in mice treated with cholinomimetics were treated with four different doses of safflower oil, of which, the dose of 187.5 mg/kg (p.o.) showed significant antiulcerogenic properties (p < 0.01). Moreover, the safflower oil at doses of 187.5 mg/kg (i.d.) increased the pH levels, gastric volume (p < 0.01) and gastric mucus production (p < 0.001), and decreased the total gastric acid secretion (p < 0.001). The acute toxicity tests showed that safflower oil (5.000 mg/kg, p.o.) had no effect on mortality or any other physiological parameter. Ecotoxicological tests performed using Daphnia similis showed an EC50 at 223.17 mg/l, and therefore safflower oil can be considered “non-toxic” based on the directive 93/67/EEC on risk assessment for new notified substances by European legislation. These results indicate that the antiulcer activity of Safflower oil may be due to cytoprotective effects, which serve as support for new scientific studies related to this pathology.245538544ABNT, Ecotoxicologia aquatica: Toxicidade aguda-metodo de ensaio com (2004) Daphnia, 21p. , spp (Cladocera, Crustacea). NBR 12713, Rio de JaneiroAmandeep, K., Robin, S., Ramica, S., Sunil, K., Peptic ulcer: A review of etiology and pathogenesis (2012) Int. J. Clin. Pharm, 3, pp. 34-38Arakawa, T., Watanabe, T., Tanigawa, T., Tominaga, K., Fujiwara, Y., Morimoto, K., Quality of ulcer healing in gastrointestinal tract: Its pathophysiology and clinical relevance (2012) World J. Gastroenterol, 18, pp. 4811-4822Bae, C.S., Park, C.H., Cho, H.J., Han, H.J., Kang, S.S., Choi, S.H., Uhm, C.S., Therapeutic effects of safflower (Carthamus tinctorius L.) seed powder on osteoporosis (2002) Korean J. Electron. Microscopy, 32, pp. 285-290Baeten, V., Dardenne, P., Aparicio, R., Interpretation of Fourier transform Raman spectra of the unsaponifiable matter in a selection of edible oils (2001) J. Agric. Food Chem, 49, pp. 5098-5107Brito, A.R.M.S., (1994) Manual de ensaios toxicologicos in vivo, 116p. , 1a ed., Campinas, Editora UnicampCEC, (1996) Technical guidance document in support of commission directive 93/67/EEC on risk assessment for new notified substances, , Part II, environmental risk assessment. Commission of the European Communities, Luxembourg: Office for official publication of the European CommunitiesCorley, D.A., Kubo, A., Zhao, W., Quesenberry, C., Proton pump inhibitors and histamine-2 receptor antagonists are associated with hip fractures among at-risk patients (2010) Gastroenterol, 139, pp. 93-101Deplege, M., Pharmaceuticals: Reduce drug waste in the environment (2011) Nature, 36, p. 478Fent, K., Weston, A.A., Caminada, D., Ecotoxicology of human pharmaceuticals (2006) Aquat. Toxicol, 76, pp. 122-159George, P., Concerns regarding the safety and toxicity of medicinal plants-An overview (2011) J. Appl. Pharm. Sci, 1, pp. 40-44Gilbert, N., Drug-pollution law all washed up (2012) Nature, 491, pp. 503-504Isidori, M., Parrella, A., Pistillo, P., Temussi, F., Effects of ranitidine and its photoderivatives in the aquatic environment (2009) Environ. Intern, 35, pp. 821-825Jain, K.S., Shah, A.K., Bariwal, J., Shelke, S.M., Kale, A.P., Jagtap, J.R., Bhosale, A.V., Recent advances in proton pump inhibitors and management of acid-peptic disorders (2007) Bioorg. Med. Chem, 15, pp. 1181-1205Kim, S.K., Cha, J.Y., Jeong, S.J., Chung, C.H., Choi, Y.R., Cho, Y.S., Properties of the chemical composition of safflower (Carthamus tinctorius L.) sprout (2000) Korean J. Life Sci, 10, pp. 68-73Madanick, R.D., Proton pump inhibitor side effects and drug interactions: Much ado about nothing? Cleve (2011) Clin. J. Med, 78, pp. 39-49Malfertheiner, P., Chan, F.K.L., McColl, K.E.L., Peptic ulcer disease (2009) Lancet, 374, pp. 1449-1461Mizui, T., Doteuchi, M., Effect of polyamines on acidified ethanol-induced gastric lesion in rats (1983) Jpn. J. Pharmacol, 33, pp. 939-945Olfert, D., Cross, B.M., McWilliam, A.A., (1993) Guide to the Care and Use of Experimental Animal, 213p. , Canadian Council on Animal Care, OntarioPintao, A.M., Da Silva, I.F., A verdade sobre o acafrao (2008) Workshop Plantas Medicinais e Fitoterapeuticas nos Tropicos. IICT/CCCM, 29, pp. 30, 31. , de Outubro, 1-19Rainsford, K.D., The effects of aspirin and other non-steroid anti-inflammatory/analgesic drugs on gastro-intestinal mucus glycoprotein biosynthesis in vivo: Relationship to ulcerogenic actions (1978) Biochem. Pharmacol, 27, pp. 877-885Rudolphi, S., Becker, H.C., Schierholt, A., Witzke-Ehbrecht, S.V., Improved estimation of oil, linoleic and oleic acid and seed hull fractions in safflower by NIRS.J (2012) Am. Oil Chem. Soc, 89, pp. 363-369Santos, L.H.L.M., Araujo, A.N., Fachinia, A., Pena, A., Delerue-Matos, C., Montenegro, M.C.B.S.M., Ecotoxicological aspects related to the presence of pharmaceuticals in the aquatic environment (2010) J. Hazard Mater, 175, pp. 45-95Saraf, A., Saraf, S., Legal regulations of complementary and alternative medicines in different countries (2012) Pharmacogn. Rev, 6, pp. 154-160Shay, H., Komarov, S.A., Fels, S.S., Meranze, D., Gruenstein, M., Siplet, H., A simple method for the uniform production of gastric ulceration in the rat (1945) Gastroenterol, 5, pp. 43-61Silveira, F.L., Silveira, L., Jr., Villaverde, A.B., Pacheco, M.T.T., Pasqualucci, C.A., Use of dispersive Raman Spectroscopy in the determination of unsaturated fat in commercial edible oil-and fat-containing industrialized foods (2010) Instrum. Sci. Technol, 38, pp. 107-123Silveira, L., Silveira, F.L., Bodanese, B., Zangaro, R.A., Pacheco, M.T.T., Discriminating model for diagnosis of basal cell carcinoma and melanoma in vitro based on the Raman spectra of selected biochemicals (2012) J. Biomed. Opt, 17Stachowska, E., Dolegowska, B., Dziedziejk, V., Rybicka, M., Kaczmarczyh, M., Bober, J., Rac, M., Chlubek, D., Prostaglandin E2 (PGE2) and thromboxane A2 (TXA2) synthesis is regulated by conjugate linoleic acids (CLA) in human macrophages (2009) J. Physiol. Pharmacol, 60, pp. 77-85Sun, X.B., Matsumoto, T., Yamada, H., Effects of a polysaccharide fraction from the root of Bupleurum falcatum L on experimental gastric ulcer models in rats and mice (1991) J. Pharm. Pharmacol, 43, pp. 669-704Szelenyi, I., Thiemer, K., Distention ulcer as a model for testing of drugs for ulcerogenic side effects (1978) Arch. Toxicol, 41, pp. 99-105Takeuchi, H., Matsuo, T., Tokuyama, K., Shimomura, Y., Suzuki, M., Diet-induced thermogenesis is lower in rats fed a lard diet than in those fed a high oleic acid safflower oil diet, a safflower oil diet or a linseed oil diet (1995) J. Nutr, 125, pp. 920-925US EPA, (2002) Methods for Measuring the Acute Toxicity of Effluents and Receiving Waters to Freshwater and Marine Organisms, 266p. , 5th ed. United States Environmental Protection Agency, EPA-821-R-02-012Webb, S., A data-based perspective on the environmental risk assessment of human pharmaceuticals I. collation of available ecotoxicity data and II. aquatic risk characterisation (2001) Pharmaceuticals in the environment sources, fate, effects and risks, pp. 175-230. , Kummerer K editor. 1st ed. Heidelberg, Germany: Springer-Verlag pWHO, (1997) Adverse Drug Reaction Database, , World Health Organization, Uppsala Sweden. 36. Institute of Safe Medication Practices Medication Safety Alert. 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Ethnopharmacology And The Sustainable Development Of New Plant-derived Drugs

This paper presents a reflection based on the experience generated by fifteen years of studies on pharmacology and chemistry of medicinal plants, in a underdeveloped country, Brazil. Although the diversity of the Brazilian flora presents a remarkable opportunity towards the development of new medicinal products, there are only small natural products research groups. Strategies for pharmacological and chemical studies of medicinal plants investigated during this time, major difficulties and ways to bypass them are discussed. The ethnopharmacological approach adopted as a general method by our research team has given good results. Details of our experience in the way to develop new plant drugs are reviewed and updated.4905/06/1540240

Erratum: Avaliação Química E Da Atividade Antidiarréica Das Folhas De Byrsonima Cinera Dc. (malpighiaceae) (revista Brasiliera De Ciencias Farmaceuticas/brazilian Journal Of Pharmaceutical Sciences (2005) 41, 1 (70-83))

[No abstract available]41228

Gastroprotective Effect Of The Ethanolic Extract And Fractions Obtained From Syngonanthus Bisulcatus Rul

Syngonanthus bisulcatus Rul., popularly known in Brazil as "sempre-vivas chapadeira", is a plant of the family Eriocaulaceae, it is found in the states of Minas Gerais and Bahia. In this work, the ethanolic extract (EtOHE), flavonoid-rich (FRF), and flavonoid-deficient (FDF) fractions obtained from scapes of S. bisulcatus were investigated for gastroprotection in both rats and mice. The activity was evaluated in models for induced gastric ulcer (absolute ethanol, stress, non-steroidal anti-inflammatory drugs, and pylorus ligation). The participation of mucus and prostaglandin E2 were also investigated. Sb-EtOHE (50, 100, and 250 mg/kg, p.o.), Sb-FRF (100 mg/kg, p.o.), and Sb-FDF (100 mg/kg, p.o.) significantly reduced gastric injuries in all models. Sb-FRF altered gastric juice parameters after pylorus ligation. Sb-FRF and Sb-FDF (100 mg/kg each, p.o.) significantly increased the amount of adherent mucus in the gastric mucosa. Sb-FRF maintained the mucosal levels of prostaglandin after the administration of indomethacin. The results indicate that Sb-EtOHE, Sb-FRF and Sb-FDF have significant gastroprotective activity. The observed gastroprotective effects of S. bisulcatus probably involve the participation of both mucus and prostaglandins, integral parts of the gastrointestinal mucosa's cytoprotective mechanisms against aggressive factors. © 2013 Reproduction is free for scientific studies.713544Vonkeman, H.E., Klok, R.M., Postma, M.J., Brouwers, J.R., van de Laar, M.A., Direct medical costs of serious gastrointestinal ulcers among users of NSAID (2007) Drugs Aging, 24, pp. 681-690Alqasoumi, S., Al-Sohaibani, M., Al-Howiriny, T., Al-Yahya, M., Rafatullah, S., Rocket Eruca sativa: A salad herb with potential gastric anti-ulcer activity (2009) World J Gastroenterol, 15, pp. 1958-1965Hoogerwerf, W.A., Pasricha, P.J., Agents used for the control of gastric acidity and treatment of peptic ulcers and gastroesopahgeal reflux diseases (2001) Goodman and Gilman's: The Pharmacological Basis of Therapeutics, pp. 1005-1019. , In: J.G Hardman., L.E Limbrid, C.S. Goodman, B.T Gilman. (eds.), 10th ed. New York: McGraw-HillLima, Z.P., Severi, J.A., Pellizzon, C.H., Brito, A.R.M.S., Solis, P.N., Caceres, A., Giron, L.M., Hiruma-Lima, C.A., Can the aqueous decoction of mango flowers be used as antiulcer agent? (2006) J Ethnopharmacol, 106, pp. 29-37Sostres, C., Gargallo, C.J., Arroyo, M.T., Lanas, A., Adverse effects of nonsteroidal anti-inflammatory drugs(NSAIDs, as pirin and coxibs) on upper gastrointestinal tract. Best Practice and Research (2010) Clinical Gastroenterology, 24, pp. 121-132Valle, D.L., Peptic ulcer diseases and related disorders (2005) Harrison's Principles of Internal Medicine, 16, pp. 1746-1762. , In: E. Braunwald, A. S. Fauci, D. L Kasper, S. L Hauser, D.L Longo, J. L. Jameson. 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Plantas com possível atividade hipolipidêmica: uma revisão bibliográfica de livros editados no Brasil entre 1998 e 2008 Plants with possible hypolipidemic activity: a review of books published in Brazil between 1998 and 2008

O objetivo deste trabalho foi realizar levantamento sobre as plantas medicinais indicadas para o tratamento da hiperlipidemia, hipercolesterolemia e/ou aterosclerose. Este estudo foi feito a partir da pesquisa bibliográfica em 32 livros publicados no Brasil entre 1998 e 2008, resultando em lista de 85 espécies distribuídas em 53 famílias, principalmente Asteraceae e Fabaceae, com 54 espécies exóticas e 31 nativas. As espécies mais citadas foram Allium sativum (Alliaceae), Cynara scolymus (Asteraceae), Curcuma longa (Zingiberaceae), Allium cepa (Alliaceae), Echinodorus grandiflorus (Alismataceae), Taraxacum officinale (Asteraceae), Vernonia condensata (Asteraceae), Cuphea carthagenensis (Lythraceae) e Curcuma zedoaria (Zingiberaceae). As espécies nativas, citadas em pelo menos 2 livros, foram investigadas para alguma evidencia científica relacionada a possíveis efeitos hipolipidêmico, hipocolesterolêmico e/ou contra aterosclerose. Somente foram encontrados estudos científicos, relacionados a estes efeitos, para as espécies nativas Cuphea carthagenensis e Echinodorus grandiflorum, indicando a necessidade de pesquisas que possam garantir a segurança e a eficácia do uso destas espécies.<br>The aim of this study was to survey medicinal plants indicated for the treatment of hyperlipidemia, hypercholesterolemia and/or atherosclerosis. This study was performed from a review of 32 books published in Brazil between 1998 and 2008, resulting in a list of 85 species belonging to 53 families, especially Asteraceae and Fabaceae, with 54 exotic and 31 native species. The species most often cited were Allium sativum (Alliaceae), Cynara scolymus (Asteraceae), Curcuma longa (Zingiberaceae), Allium cepa (Alliaceae), Echinodorus grandiflorus (Alismataceae), Taraxacum officinale (Asteraceae), Vernonia condensata (Asteraceae), Cuphea carthagenensis (Lythraceae) and Curcuma zedoaria (Zingiberaceae). Native species cited in at least 2 books were investigated for some scientific evidence related to possible hypolipidemic and hypocholesterolemic effects and/or action against atherosclerosis. Scientific studies related to these effects were found only for the native species Cuphea carthagenensis and Echinodorus grandiflorum, indicating the need for studies capable of assuring the safety and the efficacy as to the use of these species