title: In vivo and in vitro immunomodulatory potential of swertiamarin isolated from Enicostema axillare (Lam.) A. Raynal that acts as an anti-inflammatory agent.
abstract: Swertiamarin is a secoiridoid glycoside found in Enicostema axillare (Lam) A. Raynal, a medicinal plant used as a depurative in the Indian system of traditional medicine. The present study evaluated the immunomodulatory activity of isolated swertiamarin. In vivo immunomodulatory activity of swertiamarin (2, 5, and 10 mg/kg b.w.) was evaluated in a model of sheep red blood cells (SRBC) by assessing its effect on organ weight, hemagglutinating antibody titer (HA), plaque-forming cells (PFC), quantitative hemolysis of SRBC, and delayed type hypersensitivity (DTH). In vitro immunomodulatory potential was studied on isolated splenocytes, neutrophils, and peritoneal macrophages. In silico immunomodulatory effects were evaluated by docking of swertiamarin on proinflammatory cytokines to confirm its potential. In in vivo studies, the animals treated with swertiamarin showed a significant (P ≤ 0.05) increase in antibody titer, plaque-forming cells, and also in weight of the thymus and spleen. A decreased response to DTH reaction was recorded with the treatment of swertiamarin. In in vitro studies, treatment with swertiamarin modulated the messenger RNA (mRNA) and protein expression of IFN-γ, IL-10, and IL-4 significantly (P ≤ 0.05) and also favored Th2-mediated response on concanavalin A (Con A)-induced splenocytes. The compound inhibited the release of free radicals significantly (P ≤ 0.05) in phytohemagglutinin (PHA)-induced neutrophils and also ameliorated the mRNA and protein expression of proinflammatory cytokines (TNF-α, IL-1β, and IL-6) in lipopolysaccharide (LPS)-induced macrophages. In in silico, the best docked pose of swertiamarin with the target proteins (TNF-α, IL-1β, and IL-6) was confirmed that swertiamarin acted as an anti-inflammatory mediator.
authors.affiliation: Division of Ethnopharmacology, Entomology Research Institute, Loyola College, Chennai, 600 034, Tamil Nadu, India.
authors.forename: S
authors.initials: S
authors.lastname: Saravanan
authors.forename: P
authors.initials: P
authors.lastname: Pandikumar
authors.forename: N
authors.initials: N
authors.lastname: Prakash Babu
authors.forename: V I
authors.initials: VI
authors.lastname: Hairul Islam
authors.forename: K
authors.initials: K
authors.lastname: Thirugnanasambantham
authors.forename: M
authors.initials: M
authors.lastname: Gabriel Paulraj
authors.forename: K
authors.initials: K
authors.lastname: Balakrishna
authors.forename: S
authors.initials: S
authors.lastname: Ignacimuthu
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D029965:Gentianaceae; D007155:Immunologic Factors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018836:Inflammation Mediators / Q000037:antagonists & inhibitors / Q000378:metabolism; D057888:Iridoid Glucosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D017433:Protein Structure, Secondary; D011753:Pyrones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D012756:Sheep
chemical_list: D000893:Anti-Inflammatory Agents; D007155:Immunologic Factors; D018836:Inflammation Mediators; D057888:Iridoid Glucosides; D010936:Plant Extracts; D011753:Pyrones; C013270:swertiamarin
references.citation: J Mol Graph Model. 1999 Feb;17(1):57-61
references.pmid: 10660911
references.citation: J Ethnopharmacol. 2009 Sep 7;125(2):252-6
references.pmid: 19607900
references.citation: Int Immunopharmacol. 2010 Feb;10(2):155-62
references.pmid: 19879381
references.citation: Curr Protoc Pharmacol. 2005 Jan 1;Chapter 10:Unit 10.10
references.pmid: 22294127
references.citation: Phytother Res. 2013 Apr;27(4):624-7
references.pmid: 22718571
references.citation: Phytother Res. 2012 Aug;26(8):1259-61
references.pmid: 22228612
references.citation: Bioinformatics. 2005 May 1;21(9):1908-16
references.pmid: 15701681
references.citation: J Biol Chem. 1987 Sep 25;262(27):13107-10
references.pmid: 3654604
references.citation: J Ethnopharmacol. 2010 Jul 6;130(1):103-6
references.pmid: 20420896
references.citation: J Ethnopharmacol. 2001 Feb;74(2):181-7
references.pmid: 11167036
references.citation: J Ethnopharmacol. 2009 Jan 21;121(2):241-7
references.pmid: 19038322
references.citation: Planta Med. 2009 Jan;75(1):12-7
references.pmid: 19006050
references.citation: Eur J Cancer Prev. 2013 May;22(3):215-28
references.pmid: 23514809
references.citation: J Ethnopharmacol. 2012 Mar 27;140(2):239-46
references.pmid: 22285523
references.citation: Med J Aust. 2006 Aug 21;185(S4):S1-S24
references.pmid: 17022438
references.citation: Anal Biochem. 1990 Mar;185(2):238-42
references.pmid: 2160202
references.citation: Pharmacology. 2007;79(2):86-92
references.pmid: 17159380
references.citation: Science. 1963 Apr 26;140(3565):405
references.pmid: 17815805
references.citation: Nat Prod Commun. 2010 Oct;5(10):1525-30
references.pmid: 21121240
references.citation: J Ethnopharmacol. 2000 Jul;71(1-2):349-52
references.pmid: 10904185
references.citation: J Ethnopharmacol. 2000 Jul;71(1-2):193-200
references.pmid: 10904163
references.citation: J Vet Med A Physiol Pathol Clin Med. 2000 Feb;47(1):1-8
references.pmid: 10841457
references.citation: J Immunol Methods. 1978;21(1-2):159-65
references.pmid: 659900
references.citation: Immunology. 1998 Feb;93(2):296-305
references.pmid: 9616382
references.citation: Pak J Pharm Sci. 1996 Jan;9(1):29-35
references.pmid: 16414773
references.citation: Phytomedicine. 2009 Mar;16(2-3):227-32
references.pmid: 19019644
references.citation: Interdiscip Toxicol. 2012 Jun;5(2):81-3
references.pmid: 23118592
references.citation: Nat Immunol. 2005 Dec;6(12):1191-7
references.pmid: 16369558
references.citation: Atherosclerosis. 2000 Sep;152(1):43-50
references.pmid: 10996338
references.citation: Int Immunopharmacol. 2003 Feb;3(2):257-65
references.pmid: 12586606
references.citation: Fitoterapia. 2011 Sep;82(6):827-33
references.pmid: 21571047
references.citation: Mutagenesis. 2012 Nov;27(6):759-69
references.pmid: 22940646
references.citation: J Nat Med. 2011 Jan;65(1):186-90
references.pmid: 20652643
references.citation: J Exp Med. 1982 Aug 1;156(2):430-42
references.pmid: 7097159
references.citation: Phytother Res. 2012 Feb;26(2):168-73
references.pmid: 21584870
references.citation: J Ethnopharmacol. 2008 Feb 12;115(3):515-9
references.pmid: 18063496
references.citation: J Ethnopharmacol. 1991 May-Jun;33(1-2):31-5
references.pmid: 1943170
references.citation: Mol Cell Biochem. 2010 Jul;340(1-2):1-6
references.pmid: 20229291
references.citation: J Inflamm (Lond). 2008 Jun 13;5:9
references.pmid: 18554383
references.citation: Exp Clin Cardiol. 2012 Spring;17(1):12-6
references.pmid: 23204894
references.citation: J Ethnopharmacol. 2010 Sep 15;131(2):268-75
references.pmid: 20600757
references.citation: Methods. 2001 Dec;25(4):402-8
references.pmid: 11846609
references.citation: J Ethnopharmacol. 2010 Mar 24;128(2):490-4
references.pmid: 20079418
references.citation: Evid Based Complement Alternat Med. 2010 Mar;7(1):41-5
references.pmid: 18955286
references.citation: Immunol Lett. 1988 Nov;19(3):183-91
references.pmid: 3069706