RSS-Feed abonnieren
DOI: 10.1055/s-2000-8563
In Vivo Studies on the Anti-Inflammatory Activity of Pachymic and Dehydrotumulosic Acids
Publikationsverlauf
Publikationsdatum:
31. Dezember 2000 (online)
![](https://www.thieme-connect.de/media/plantamedica/200003/lookinside/thumbnails/10.1055-s-2000-8563-1.jpg)
Abstract
Pachymic and dehydrotumulosic acids were studied in different models of acute and chronic inflammation. They proved to be active in most of the methods applied. None of them were active against arachidonic acid-induced ear edema. Dehydrotumulosic acid significantly diminished the mouse ear edema induced by ethyl phenylpropiolate, while pachymic acid was ineffective. When the putative corticoid-like mechanism of both compounds was explored, pachymic acid activity was partially abolished by the glucocorticoid receptor antagonist progesterone, but dehydrotumulosic acid activity was not affected. In vivo experiments demonstrated the inhibition by both principles of the phospholipase A2 (PLA2)-induced extravasation. The previous report on the effects of both compounds in vitro against PLA2, together with the present in vivo results, support the idea that the inhibition of this enzyme probably constitutes their main mechanism of action.
Abbreviations
AA:arachidonic acidCOX:cyclooxygenaseEPP:ethyl phenylpropiolateLOX:lipoxygenaseMPO:myeloperoxidasePLA2:phospholipase A2PMNL:polymorphonuclear leukocytesTPA:12-O-tetradecanoylphorbol-13-acetate
Key words
Pachymic acid - dehydrotumulosic acid - anti-inflammatory activity - dermatitis - Poria cocos - Polyporaceae - phospholipase A2 inhibition
References
-
1 Chang H M,, But P PH..
Pharmacology and Applications of Chinese Materia Medica. Vol. 2. World Scientific, Singapore; 1987: 875-7 -
2 Hikino H..
Recent Research on Oriental Medicinal Plants. In: Wagner H, Hikino H, Farnsworth NR, editors Vol. 1. Academic Press, London; 1985: 64-5 - 3 Hattori T,, Hayashi K,, Nagao T,, Furuta K,, Ito M,, Suzuki Y.. Studies of antinephritic effects of plant components (3). Effects of pachyman, a main component of Poria cocos Wolf on original-type anti-GBM nephritis in rats and its mechanisms. Jpn. J. Pharmacol.. 1992;; 59 89-96
- 4 Tai T,, Akita Y,, Kinoshita K,, Koyama K,, Takahachi K,, Watanaba K.. Anti-emetic principles of Poria cocos. Planta Medica. 1995;; 61 527-30
- 5 Cuéllar M J,, Giner R M,, Recio M C,, Just M C,, Máñez S,, Ríos J L.. Effect of the basidiomycete Poria cocos on experimental dermatitis and other inflammatory conditions. Chem. Pharm. Bull.. 1997;; 45 492-4
- 6 Tseng J,, Chang J G.. Suppression of tumor necrosis factor-α, interleukin-1β, interleukin-6 and granulocyte-monocyte colony stimulating factor secretion from human monocytes by an extract of Poria cocos. Chin. J. Microbiol. Immunol.. 1992;; 25 1-11
- 7 Cuéllar M J,, Giner R M,, Recio M C,, Just M J,, Máñez S,, Ríos J L.. Two fungal lanostane derivatives as phospholipase A2 inhibitors. J. Nat. Prod.. 1996;; 59 977-9
- 8 Kaminaga T,, Yasukawa K,, Takido M,, Tai T,, Nunoura Y.. Inhibitory effect of Poria cocos on 12-O-tetradecanoylphorbol-13-acetate-induced ear oedema and tumour promotion in mouse skin. Phytother. Res.. 1996;; 10 581-4
- 9 Kaminaga T,, Yasukawa K,, Kanno H,, Tai T,, Nunoura Y,, Takido M.. Inhibitory effect of lanostane-type triterpene acids, the components of Poria cocos, on tumor promotion by 12-O-tetradecanoylphorbol-13-acetate in two-stage carcinogenesis in mouse skin. Oncology. 1996;; 53 382-5
- 10 Yasukawa K,, Kaminaga T,, Kitanaka S,, Tai T,, Nunoura Y,, Natori S et al.. 3β-p-Hydroxybenzoyldehydrotumulosic acid from Poria cocos, and its anti-inflammatory effect. Phytochemistry. 1998;; 48 1357-60
-
11 Young J M,, De Young L M..
Cutaneous models of inflammation for the evaluation of topical and systemic pharmacological agents. In: Spector J, Back N, editors. Alan R. Liss, New York; 1989: 215-31 - 12 Stanley P L,, Steiner S,, Havens M,, Tramposch K M.. Mouse skin inflammation induced by multiple topical applications of 12-O-tetradecanoylphorbol-13-acetate. Skin Pharmacol.. 1991;; 4 262-71
- 13 De Young L M,, Kheifets J B,, Ballaron S J,, Young J M.. Edema and cell infiltration in the phorbol ester-treated mouse ear edema are temporally separate and can be differentially modulated by pharmacological agents. Agents Actions. 1989;; 26 335-41
- 14 Neves P CA,, Neves M CA,, Bella Cruz A,, Sant'ana A EG,, Yunes R A,, Calixto J B.. Differential effects of Mandevilla velutina compounds on paw oedema induced by phospholipase A2 and phospholipase C. Eur. J. Pharmacol.. 1993;; 243 213-9
- 15 Brattsand R,, Thalén A,, Roempke K,, Källström L,, Gruvstad E.. Influence of 16α,17α-acetal substitution and steroid nucleus fluorination on the topical to systemic activity ratio of glucocorticoids. J. Steroid Biochem.. 1982;; 16 779-86
- 16 Sugishita E,, Amagaya S,, Ogihara Y.. Studies on the mechanism of anti-inflammatory activities of Papyriogenin A and C. J. Pharm. Dyn.. 1983;; 6 287-94
- 17 Recio M C,, Giner R M,, Máñez S,, Guého J,, Julien H R,, Hostettmann K et al.. Investigations on the steroidal anti-inflammatory activity of triterpenoids from Diospyros leucomelas. Planta Medica. 1995;; 61 9-12
- 18 Brain S,, Lewis G P,, Whittle B JR.. Actions of phospholipase-A on mast-cell histamine release and paw oedema in the rat. Br. J. Pharmacol.. 1977;; 59 440P
- 19 Hambleton P,, McMahon S.. Investigation of phospholipases-induced paw oedema in the rat. Br. J. Pharmacol.. 1989;; 97 543P
- 20 Marshall L A,, Chang J Y,, Calhoun W,, Yu J,, Carlson R P.. Preliminary studies on phospholipase A2-induced mouse edema as a model to evaluate anti-inflammatory agents. J. Cell Biochem.. 1989;; 40 147-55
- 21 Cirino G,, Peers S H,, Wallace J L,, Flower R J.. A study of phospholipase A2-induced oedema in rat paw. Eur. J. Pharmacol.. 1989;; 166 505-10
- 22 Cirino G,, Peers S H,, Flower R J,, Browning J L,, Pepinsky R B.. Human recombinant lipocortin 1 has acute local anti-inflammatory properties in the rat paw oedema test. Proc. Natl. Acad. Sci. USA. 1989;; 86 3428-32
- 23 Safayhi H,, Sailer E R.. Anti-inflammatory actions of pentacyclic triterpenes. Planta Medica. 1997;; 63 487-93
-
24 Ríos J L,, Recio M C,, Máñez S,, Giner R M..
Natural triterpenoids as anti-inflammatory agents. In: Atta-Ur-Rahman, editor Vol. 21. Elsevier, Amsterdam; 2000: in press - 25 Nukaya H,, Yamashiro H,, Furazawa H,, Ishida H,, Tsuji K.. Isolation of inhibitors of TPA-induced mouse ear edema from Hoelen, Poria cocos. Chem. Pharm. Bull.. 1996;; 44 847-9
- 26 Ansari S H,, Ali M.. Analgesic and anti-inflammatory activity of tetracyclic triterpenoids isolated from Pistacia integerrima galls. Fitoterapia. 1996;; 67 103-5
- 27 Jain M K,, Yu B Z,, Rogers J M,, Smith A E,, Boger E TA,, Ostrander R L et al.. Specific competitive inhibitor of secreted phospholipase A2 from berries of Schinus terebinthifolius. Phytochemistry. 1995;; 39 537-47
- 28 Takei M,, Umeyama A,, Shoji N,, Arihara S,, Endo K.. Mechanism of inhibition of IgE-dependent histamine release from rat mast cells by penasterol and penasterone. J. Pharm. Sci.. 1995;; 84 228-30
- 29 Hirotani M,, Asaka L,, Ino C,, Furuya T,, Shiro M.. Studies on the metabolites of higher funge.7. Ganoderic acid derivatives and ergosta-4,7,22-triene-3,6-dione from Ganoderma lucidum. Phytochemistry. 1987;; 26 2797-803
- 30 Young J M,, Spires D A,, Bedord C J,, Wagner B,, Ballaron S J,, De Young L M.. The mouse ear inflammatory response to topical arachidonic acid. J. Invest. Dermatol.. 1984;; 82 367-71
- 31 Suzuki K,, Ota H,, Sasagawa S,, Sakatani T,, Fujikura T.. Assay method for myeloperoxidase in human polymorphonuclear leukocytes. Anal. Biochem.. 1983;; 132 345-52
- 32 Aldaz C M,, Conti C J,, Giménez I B,, Slaga T J,, Klein-Szanto A JP.. Cutaneous changes during prolonged application of 12-O-tetradecanoylphorbol-13-acetate on mouse. Cancer Res.. 1985;; 45 2753-9
- 33 Baxter C S,, Andringa A,, Chalfin K,, Miller M L.. Comparative histomorphometric changes in SENCAR mouse epidermis in response to multiple treatments with complete and stage-specific tumor promoting agents. Carcinogenesis. 1989;; 10 1855-61
- 34 Schmitt D.. Le système immunitaire cutané. CR Soc. Biol.. 1994;; 188 207-21
- 35 Chapman J R,, Ruben Z,, Butchko G M.. Histology of and quantitative assays for oxazolone-induced allergic contact dermatitis in mice. Am. J. Dermatopathol.. 1986;; 8 130-8
- 36 Zang L,, Ding Q,, Zhang P Y,, Zhu R P,, Zhou Y H.. Molecular weight and aggregation behaviour in solution of β-D-glucan from Poria cocos sclerotium. Carbohydrate Res.. 1997;; 303 193-7
- 37 Cameron G S,, Baldwin J K,, Klann K C,, Patrick K E,, Fischer S M.. Tumor-promoting activity of ethyl phenylpropiolate. Cancer Res.. 1991;; 51 5642-8
Prof. Dr. J. L. Ríos
Departament de Farmacologia Facultat de Farmàcia Universitat de València
Avda. Vicent Andrés Esés s/n
Burjassot, 46100
Spain
eMail: riosjl@uv.es
Telefon: +34 963864943
Fax: +34 963864973