Mechanism of Vasorelaxation Induced by Coptosapelta flavescens Stems Extract in Rat Thoraric Aorta

Authors

  • Sjarif Ismail Research Center on Drugs and Public Health, Mulawarman University, Samarinda, Indonesia Author
  • Khemasili Kosala Pharmacology Laboratory, Faculty of Medicine Mulawarman University, Samarinda, Indonesia Author
  • Ika Fikriah Pharmacology Laboratory, Faculty of Medicine, Mulawarman University, Samarinda, Indonesia Author
  • Agustina Rahayu Magdaleni Physiology Laboratory, Faculty of Medicine, Mulawarman University, Samarinda, Indonesia Author

DOI:

https://doi.org/10.30872/j.trop.pharm.chem.v4i2.123

Keywords:

Coptosapelta flavescens, vasorelaxation, extract, aorta, In vitro

Abstract

Coptosapelta flavescens Korth. is a liana plant from the Rubiaceae family. In East Kalimantan, it is also known as “Akar Tambolekar†or “Merungâ€, it is called “akar†or root as its trunk spreads like a root. The plant’s stems are used by ethnic Dayak in East Kalimantan to overcome high blood pressure and it has been proven to induce vasorelaxation on blood vessels, but the its action mechanism in the endothelial or vascular smooth muscle cells (VSMC) are unknown. Vasorelaxation on the blood vessels could be mediated by endothelial or by the VSMC. This research aims to study in vitro which of them is the mechanism of action of Coptosapelta flavescens Stems (CFS) extract. CFS were taken from the secondary forest in Paser Regency, East Kalimantan Province. Its simplicia were macerated with methanol solvent for three days and twice repeated. Vasorelaxation activity of the blood vessels was tested with rats’ isolated thoracic aorta with endothelial and with the endothelial removed (endothelium-denuded). Both aorta of 3 mm length were soaked into Krebs-Henselheit solution at 37°C, pH 7.4 and aerated with carbogen gas. After they have acclimatized, both aortas were contracted with phenylephrine solution, after reaching peak contraction and plateau, the solution of extract or its solvent (Control) was administered in cumulatively increasing doses. The results show that CFS extracts induce vasorelaxation both in the endothelial-intact aorta and in the endothelial-denuded aorta. At high concentrations, the vasorelaxation activity in the endothelial-intact aorta was weaker than that on endothelial-denuded aorta. This study proves that action mechanism of blood vessels’ vasorelaxation induced by the methanol extract of CFS were more dominantly mediated by the blood vessels smooth muscle; and at high concentrations the endothelial actually weakened the VSMC vasorelaxation activity. Further study is necessary on the mechanism of  action vasorelaxation through the modulation of intracellular or extracellular calcium ion channels of VSMC.

References

[1] Hajjar I, & Kotchen TA. 2003. Trends in prevalence, awareness, treatment, and control of hypertension in the United States, 1988-2000. Journal of the American Medical Association, 290:199-206.

[2] World Health Report. 2002. Reducing risks, promoting healthy life. Geneva, Switzerland: World Health Organization. 2002. Available at: http://www.who.int/whr/2002/. Acessed 10/23/2017.

[3] Darusman KL. 2004. Final technical report: The potential of medical plants to support sustainable forest management: ecological, economic, and sociocultural aspects. ITTO Pre-Project PPD 55/02 Rev. 2(I). Ministry of Forestry-Biopharmaca Research Center IPB-PT INHUTANI I. International Tropical Timber Organization, Bogor, Indonesia. Available at: http://www.itto.int/files/itto_project_db_input/2766/Technical/PPD-55-02-R2-I-Technical-Report.pdf. Acessed 10/23/2017.

[4] Rezeky FC. 2009. Fakultas MIPA Universitas Lambung Mangkurat, Banjarbaru, Indonesia. Skripsi (not published).

[5] Hounkong K, Sawangjaroen N, Kongyen W, Rukachaisirikul V, & Voravunthikuncai SP. 2014. Anti-intestinal protozoan activities of 1-hydroxy-2-hyddroxymethylanthraquinone from Coptosapelta flavescens. Asian Pacific Journal of Tropical Disease, 4:457-465.

[6] Hounkong K, Sawangjaroen N, Kongyen W, Rukachaisirikul V, & Wootipoom N. 2015. Mechanisms of 1-hydroxy-2-hyddroxymethylanthraquinone from Coptosapelta flavescens as an anti-giardiasis activity. Acta Tropica, 146:11-16.

[7] Komura H, Mizukawa K, Minakata H, Huang H, Qin G, & Xu R. 1983. New anthraquinones from Eleutherine americana. Chemical and Pharmaceutical Bulletin, 31(11):4206-08.

[8] Chung MI, Gan KH, Lin CN, Ko FN, & Teng CM. 1993. Antiplatelet effects and vasorelaxing action of some constituents of Formosan plants. Journal of Natural Products, 56(6):929-34.

[9] Kosala, K, Ismail S, Fikriah I, & Rahayu A. Eksplorasi aktivitas vasodilatasi ekstrak batang Coptosapelta flavescens Korth. secara in vitro. Program Book Seminar Nasional ke-53 Pokjanas TOI, Fakultas Kedokteran Universitas Islam Malang, 11-12 Oktober 2017. Abstrak.

[10] Ismail S, Ali MM, & Soeatmadji DW. 2013, Efek suplemen L-arginin subakut peroral pada kontraksi aorta tikus diabetes. Journal of Experimental Life Science, 3(2):54-64.

[11] Ismail S & Yuniati. 2016. Aktivitas vasodilatasi pembuluh darah secara in vitro dan uji toksisitas akut minuman fungsional herbal Kaltim. Journal of Pharmaceutical Chemistry, 3(3):197-201.

[12] Ismail S, & Kosala K. 2011. In vitro comparison test of vasodilation activity on two types of yellow root plant of the menisperaceae. Jurnal Kimia Mulawarman, 8(2):102-104.

[13] Kosala K, & Ismail S. 2008. Aktivitas Kontraktilitas aorta pada ekstrak daun Andrographis paniculata. The Journal of Indonesian Medical Plant, 1(1):20-24.

[14] Sandoo A, Zanten JJCSV, Metsios GS, Caroll D, & Kitas GD. 2010. The endothelium and its role in regulating vascular tone. The Open Cardiovascular Medicine Journal, 4:302-12.

[15] Giles TD, Sander GE, Nossaman BD. & Kadowitz PJ. 2012. Impaired vasodilation in the pathogenesis of hypertension: focus on nitric oxide, endothelial-derived hyperpolarizing factors, and prostaglandins. The Journal of Clinical Hypertension, 14:198–205.

[16] Jin X, Otonashi-Sastoh Y, Zamani Y, Koyama T, Sun P, Kitamura Y, & Kawasaki H. 2010. Endothelial modulation of agonist-induced vasoconstriction in mesenteric microcirculation. The Pharmaceutical Society of Japan, 130(5):723-728.

[17] Kongyen W, Rukachaisirikul V, Phongpaichit S, Sawangjaroen N, Songsing P, & Madardam H. 2014. Anthraquinone and naphthoquinone derivates from the root of Coptosapelta flavescens. Natural Product Communications, 9:219-220.

[18] Huang H, Qin G, & Xu. 1983. New antraquinones from Eleutherine americana. Chemical and Pharmaceutical Bulletin, 31(11):4206-08.

[19] Dantas BPV, Ribeiro TP, Assis VL, Furtado FF, Assis KS, Alves JS, Silva TMS, Camara CA, França-Silva MS, Veras RC, Medeiros IA, Alencar JL, & Braga VA. 2014. Vasorelaxation induced by a new naphthoquinone-Oxime is mediated by NO-sGC-cGMP pathway. Molecules, 19:9773-85.

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Published

2025-02-01

How to Cite

Mechanism of Vasorelaxation Induced by Coptosapelta flavescens Stems Extract in Rat Thoraric Aorta. (2025). Journal of Tropical Pharmacy and Chemistry , 4(2), 103-107. https://doi.org/10.30872/j.trop.pharm.chem.v4i2.123

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