Antinociceptive and Gastroprotective Effects of Diterpenes from the Flower Buds of Egletes viscosa

Abstract

Centipedic acid and 12-acetoxy-hawtriwaic acid lactone, diterpenes isolated from the flower buds of Egletes viscosa (Asteraceae) were assayed for antinociceptive and gastroprotective activities in animal models of nociception and gastric ulcer. In the chemical nociception induced in mice by intraperitoneal acetic acid and subplantar formalin injections, both diterpenes (25 and 50 mg/kg, p. o.) exerted potent antinociception in a manner similar to indomethacin (5 mg/kg, p. o.). In the formalin test, only the late phase nociceptive response (20 - 25 min) and not the early phase response (0 - 5 min) was inhibited by these diterpenes. However, these compounds were found to be ineffective against thermal nociception in the hot-plate test. Further, the diterpenes reduced the severity of absolute ethanol-induced gastric lesions in rats. At the dose of 50 mg/kg, both centipedic acid and 12-acetoxy hawtriwaic acid suppressed the gastric lesions by 53 % and 63 %, respectively. Against the gastric ulceration induced by indomethacin, only centipedic acid (25 and 50 mg/kg) showed significant inhibition by about 47 - 49 %. The data suggested the gastroprotective and peripheral analgesic properties of diterpenes isolated from E. viscosa.

References

• 1 Braga R. Plantas do Nordeste, especialmente do Ceará. Centro de Divulgação Universitária 1960: 320
• 2 Lima M A, Silveira E R, Marques M S, Santos R H, Gambardela M T. Biologically active flavonoids and terpenoids from Egletes viscosa .  Phytochemistry. 1996;  41 217-23
• 3 Craveiro A A, Alencar J W, Matos F JA, Machado M IL. Essential oils from flower heads of Egletes viscosa Less.  Journal of Essential Oil Research. 1992;  4 639-40
• 4 Souza M F, Santos F A, Rao V SN, Sidrim J JC, Matos F JA, Machado M IL, Silveira E R. Antinociceptive, anticonvulsant and antibacterial effects of the essential oil from the flower heads of Egletes viscosa L.  Phytotherapy Research. 1998;  12 28-31
• 5 Souza M F, Rao V SN, Silveira E R. Antianaphylactic and anti-inflammatory effects of ternatin, a flavonoid isolated from Egletes viscosa Less.  Brazilian Journal of Medical and Biological research. 1992;  25 1029-32
• 6 Rao V SN, Figueredo E G, Melo C L, Viana G SB, Menezes D B, Matos M SF, Silveira E R. Protective effect of ternatin, a flavonoid isolated from Egletes viscosa Less. in experimental liver injury.  Pharmacology. 1994;  48 392-7
• 7 Rao V SN, Santos F A, Sobreira T T, Souza M F, Melo C L, Silveira E R. Investigations on the gastroprotective and antidiarroeal properties of ternatin, a tetramethoxyflavone from Egletes viscosa .  Planta Medica. 1997;  63 146-9
• 8 Pessoa C, Silveira E R, Wetmore L A, Moraes M O, Leyva A. Antiproliferative effects of compounds derived from plants of Northeast Brazil.  Phytotherapy Research. 2000;  14 187-91
• 9 Brito A R, Rodriguez J A, Hiruma-Lima C A, Haun M, Nunes D S. Antiulcerogenic activity of trans-dehydrocrotonin from Croton cajucara .  Planta Medica. 1998;  64 126-9
• 10 Hiruma-Lima C A, Gracioso J D, Toma W, de Paula A C, de Almeida A B, Brasil D S, Muller A H, Souza Brito A R. Gastroprotective effect of aparisthman, a diterpene isolated from Aparisthmium cordatum on experimental gastric ulcer models in rats and mice.  Phytomedicine. 2001;  23 (8) 94-100
• 11 Koster R, Anderson M, de Beer E J. Acetic acid for analgesic screening.  Federation proceedings. 1959;  18 412-4
• 12 Hunskaar S, Hole K. The formalin test in mice: dissociation between inflammatory and non-inflammatory pain.  Pain. 1987;  103 103-14
• 13 Eddy N B, Leimbach D. Synthetic analgesics. II dithienylbutenyl and dithienylbutylamines.  Journal of Pharmacology and Experimental Therapeutics. 1953;  107 385-93
• 14 Robert A, Nezamis J E, Lancaster C, Hanchar A J. Prevention of gastric necrosis produced by alcohol, HCl, NaOH, hypertonic NaCl, and thermal injury.  Gastroenterology. 1979;  77 433-43
• 15 Bhargava K P, Gupta M B, Tangri K K. Mechanism of ulcerogenic activity of indomethacin and oxyphenbutazone.  European journal of Pharmacology. 1973;  22 191-5
• 16 Szabo S, Teier J S, Brown A, Schnoor J, Homan H D, Bradford J C. A quantification method for assessing the extent of experimental erosions and ulcers.  Journal of Pharmacological Methods. 1985;  13 59-66