Alpha antiadrenergic effect of Achyrocline bogotensis extract (“Vira Vira”) in isolated rat aortic ring
Keywords:Achyroclines, antiadrenergics, male lower urinary tract symptoms (LUTS), phenylephrine, aorta, flavonoids, nitric oxide.
Background: The treatment of symptoms of prostatic hyperplasia is among the traditional uses of Achyrocline bogotensis (Kunth) [N.V. “Vira Vira”, Compositae] in Colombia. Pharmacological therapy for this disorder depends mainly on alpha-1 antiadrenergic agents, and the mechanism has not been studied previously using A. bogotensis. Objectives: To assess the alpha-1 antiadrenergic effect of the extract obtained from the aerial parts of A. bogotensis in isolated aortic rings from Wistar rats. Methods: The study compared the effects of the ethanol extract of A. bogotensis, prazosin (reference) and DMSO (control) in rings stimulated with phenylephrine (PE) or KCl. The capacity to reduce the PE pressor effect by the ethanol extract (pD2’ value) was determined. To quantify the A. bogotensis relaxant potency, increasing concentrations of the ethanol extract (0.1 µg/mL-0.1 mg/mL), were added cumulatively to isolated aortic rings pre-contracted with PE (0.1 µM) or KCl (80 mM). To explore the possible participation of nitric oxide (NO), L-NAME (100 µM) was administered to aortic rings exposed to cumulatively increasing concentrations of PE in isolated aortic rings in the presence of the extract (10 µg/mL). Aqueous, butanol and dichloromethane fractions (10 µg/mL) obtained from the ethanol extract were assayed. Phytochemical screening was also performed. Results: Prazosin and A. bogotensis extract notably reduced the contraction induced by PE whereas their inhibitory effect in rings contracted with KCl were lower. A. bogotensis ethanol extract showed a high capacity for reducing the PE pressor response (pD´2 : 5.51) as well as total efficacy for relaxing rings previously precontracted with PE. The relaxant efficacy and potency of A. bogotensis extract against rings previously contracted with KCl were notably lower. L-NAME partly reverted the inhibitory effect of A. bogotensis. Aqueous, butanol and dichloromethane fractions gave inhibitory responses lower than that obtained with the ethanol extract. Phytochemical screening of A. bogotensis extract revealed the significant presence of flavonoid and triterpene metabolites. Conclusions: These results suggest that A. bogotensis elicits a smooth muscle relaxant effect related to the alpha-1 antiadrenergic mechanism. This response is partially NO dependent and seems to be due to interactions among active metabolites likely to be of flavonoid and/or terpenoid nature.
Torrenegra RD, Escarria S, Tenorio E, Achenbach H. Estudio fitoquimico del Achirocline bogotensis. Rev Latinoam Quim. 1982; 13:75-76.
Sagawa T, Takaishi Y, Fujimoto Y, Duque C, Osorio C, Ramos F, Garzon C, Sato M, Okamoto M, Oshikawa T, Ahmed SU. Cyclobutane dimers from the Colombian medicinal plant Achyrocline bogotensis. J Nat Prod. 2005; 68(4):502-505.
Téllez MA, Téllez AN, Vélez F, Ulloa JC. In vitro antiviral activity against rotavirus and astrovirus infection exerted by substances obtained from Achyrocline bogotensis (Kunth) DC. (Compositae). BMC Complement Altern Med. 2015; 15(1):428.
Thomas CM, Wood RC 3rd, Wyatt JE, Pendleton MH, Torrenegra RD, Rodriguez OE, Harirforoosh S, Ballester M,
Lightner J, Krishnan K, Ramsauer VP. Anti-neoplastic activity of two flavone isomers derived from Gnaphalium elegans and Achyrocline bogotensis. PLoS One. 2012; 7(6):e39806.
Zorzi GK, Caregnato F, Moreira JC, Teixeira HF, Carvalho EL. Antioxidant effect of nanoemulsions containing extract of Achyrocline satureioides (Lam) D.C.-Asteraceae. AAPS PharmSciTech. 2016 Aug;17(4):844-50
Cariddi LN, Sabini MC, Escobar FM, Bacchetti R, Montironi I, Merckis C, Reinoso EB, Núñez Montoya S, Zanon SM, Comini LR, Sabini LI. In vitro and in vivo cytogenotoxic effects of hot aqueous extract of Achyrocline satureioides (Lam.) DC. Biomed Res Int. 2015; 2015:270973.
Bidone J, Bica VC, Petrovick PR, Simoes CM, Koester LS, Bassani VL, Teixeira HF. Simultaneous quantification of flavonoids from Achyrocline satureioides by a polar-reversed phase LC method--application to skin permeation/retention studies. Pharmazie. 2014; 69(1):5-9.
De Souza KC, Schapoval EE, Bassani VL. LC determination of flavonoids: separation of quercetin, luteolin and 3-Omethylquercetin in Achyrocline satureioides preparations. J Pharm Biomed Anal. 2002; 28(3-4):771-777.
Bueno-Sánchez JG, Martínez-Morales JR, Stashenko EE, Ribón W. Anti-tubercular activity of eleven aromatic and medicinal plants occurring in Colombia. Biomedica. 2009; 29(1):51-60.
Demarque DP, Fitts SM, Boaretto AG, da Silva JC, Vieira MC, Franco VN, Teixeira CB, Toffoli-Kadri MC, Carollo CA.
Optimization and technological development strategies of an antimicrobial extract from Achyrocline alata assisted by statistical design. PLoS One. 2015; 10(2):e0118574.
Toffoli-Kadri MC, Carollo CA, Lourenço LD, Felipe JL, Néspoli JH, Wollf LG, Resende GM, de Lima JR, Franco VN, Vieira Mdo C, de Siqueira JM. In vivo and in vitro anti-inflammatory properties of Achyrocline alata (Kunth) DC. J Ethnopharmacol. 2014; 153(2):461-468.
Labuckas DO, Maestri DM, Grosso NR, Zygadlo JA. Essential oils of Achyrocline satureioides, Achyrocline alata and Achyrocline tomentosa. Planta Med. 1999; 65(2):184-186.
alliwell B, Rafter J, Jenner A. Health promotion by flavonoids, tocopherols, tocotrienols, and other phenols: direct or indirect effects? Antioxidant or not? Am J Clin Nutr. 2005; 81(1):268S-276S.
Qin CX, Chen X, Hughes RA, Williams SJ, Woodman OL. Understanding the cardioprotective effects of flavonols: discovery of relaxant flavonols without antioxidant activity. J Med Chem. 2008;51(6):1874-1884.
Van der Graaf PH, Shankley NP, Black JW. Analysis of the activity of alpha 1-adrenoceptor antagonists in rat aorta. Br J Pharmacol. 1996;118(2):299-310.
Hancock AA. α-Adrenoceptor Assays. Curr Protoc Pharmacol. John Wiley & Sons, Inc. 1998; 4(5).1-28.
Chang DF, Campbell JR. Intraoperative floppy iris syndrome associated with tamsulosin. J Cataract Refract Surg. 2005; 31(4):664-673.
Hollingsworth JM, Wilt TJ. Lower urinary tract symptoms in men. BMJ. 2014;14;349:g4474.
Ohmura T, Oshita M, Kigoshi S, Muramatsu I. Identification of alpha 1-adrenoceptor subtypes in the rat vas deferens: binding and functional studies. Br J Pharmacol. 1992;107(3):697-704.
How to Cite
Copyright (c) 2017 Vitae
This work is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License.
Copyright Notice and Open Access Statement
The Journal Vitae works under the Open Access license, and the published manuscripts remain available for the public, both on the Journal's website and in databases, under the Creative Commons license, "Noncommercial Attribution" and "Share alike" systems, adopted in Colombia. Hence, when the authors agree to publish in the Journal Vitae, they will not have the right to economic retributions on publications and reproductions through different diffusion media. The documents are freely available to the internet public, permitting users to read, download, copy, distribute, print, search, or link to the full texts and pass them as data to software. The only constraint on reproduction and distribution, should be to give authors control over the integrity of their work and the right to be appropriately acknowledged and cited.
Authors declare that:
They are the intellectual property owners and are responsible for all the information stated in the article.
This manuscript has not been submitted or published in other printed or digital media. They accept the responsibility for the judgments, opinions, and points of view expressed in the published article and, therefore, they exonerate Universidad de Antioquia and Journal Vitae from any process.
They exempt Universidad de Antioquia and Journal Vitae from settling conflicts or disputes related to the authorship of the referred article.
They accept the revision of the original manuscript by suitable personnel, and they bind themselves to perform the corrections appointed or suggested by the assessors.
Therefore, they know the editorial process and will not bind the Editorial Board of the Journal to assume any obligations regarding the volume and issue in which the article is published.
They transfer the rights of publication, reprinting, and distribution of the article from the moment of its approval, in print and digital format, without the right to economic rewards, and under the licensing conditions considered relevant by Journal Vitae.
They fully authorize Universidad de Antioquia and Journal Vitae to submit the published material to the diverse databases and indexing systems where the Journal can be found to comply with the requirements of the regulatory authorities to maintain the national classification of journals.
They will assume the article publication costs established for the current issue, and they will make the payment as soon as they are informed about the volume and the issue in which the final version of the article is published.
After the article is published, you can share digital or printed copies in a noncommercial manner. You will be able to use the paper in your institution or company for educational or research purposes, including the use in course programs.
Conflict of interest: Authors are responsible for recognizing and disclosing any financial or other benefits that could be perceived to bias their work, acknowledging all financial support and any personal connections with potential sponsors. Examples of such conflicts include receiving research funds or honoraria, serving on advisory boards, stock ownership, or employment and consulting arrangements. Authors without such connections should clearly state that they have no financial support or personal relationships that could be perceived to bias their work. All conflicts of interest should be disclosed on the author's identification page of the manuscript.