scholarly journals In vivo antinociceptive and anti-inflammatory potential of hesperidin and its cyclodextrin inclusion compounds

2021 ◽  
Vol 12 (Vol.12, no.1) ◽  
pp. 40-45
Author(s):  
Andreia CORCIOVĂ ◽  
Bianca IVĂNESCU ◽  
Daniela Carmen ABABEI ◽  
Ana Flavia BURLEC ◽  
Cornelia MIRCEA ◽  
...  

Introduction. This study aims to evaluate the antinociceptive activity on inflammatory and non-inflammatory nociception models, as well as the anti-inflammatory action of hesperidin and its inclusion compounds with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin. Material and method. For these experiments, we employed nociception models using thermal, chemical and pressure stimuli and an inflammation model for the evaluation of inflammatory edema by plethysmometer test. Results and discussions. The obtained results demonstrate that the HES-βCD inclusion compounds exhibited antinociceptive action predominantly on experimental non-inflammatory nociception models, while HES-HP-βCD exhibited anti-inflammatory and antinociceptive activities predominantly in inflammatory nociception models. Conclusions. This research may be the starting point for future studies regarding the improvement of biopharmaceutical qualities of HES by encapsulation in cyclodextrins. Keywords: hesperidin, cyclodextrin inclusion compunds, antinociceptive, anti-inflammatory activity,

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Deok-Sang Hwang ◽  
Hyo Geun Kim ◽  
Jun-Bock Jang ◽  
Myung Sook Oh

Dangguijakyak-san (DJS), a famous traditional Korean multiherbal medicine, has been used to treat gynecological and neuro-associated disease. Recent studies demonstrated that DJS has multiple bioactivities including neuroprotection. In the present study, we were to investigate the effect of DJS and its mechanism in anin vitroandin vivomodel of Parkinson’s disease (PD). In primary mesencephalic culture system, DJS attenuated the dopaminergic cell damage induced by 1-methyl-4-phenylpyridine toxicity, and it inhibited production of inflammatory factors such as tumor necrosis factorα(TNF-α), nitric oxide (NO), and activation of microglial cells. Then, we confirmed the effect of DJS in a mouse PD model induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). In the pole test, DJS at 50 mg/kg/day for 5 days showed increase of motor activity showing shortened time to turn and locomotor activity compared with the MPTP only treated mice. In addition, DJS significantly protected nigrostriatal dopaminergic neuron from MPTP stress. Moreover, DJS showed inhibition of gliosis in the substantia nigra pars compacta. These results have therapeutic implications for DJS in the treatment of PD via anti-inflammatory effects.


2007 ◽  
Vol 59 (1) ◽  
pp. 123-130 ◽  
Author(s):  
Mu Hong Lee ◽  
Jeong Min Lee ◽  
Sung Hoon Jun ◽  
Chul Gyu Ha ◽  
Seung-Ha Lee ◽  
...  

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Olumayokun A. Olajide ◽  
Mutalib A. Aderogba ◽  
Uchechukwu P. Okorji ◽  
Bernd L. Fiebich

Bridelia ferrugineais commonly used in traditional African medicine (TAM) for treating various inflammatory conditions. Extracts from the plant have been shown to exhibit anti-inflammatory property in a number ofin vivomodels. In this study the influence ofB. ferruginea(BFE) on the production of PGE2, nitrite, and proinflammatory cytokines from LPS-stimulated BV-2 microglia was investigated. The effects of BFE on cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) protein expressions were evaluated in LPS-activated rat primary microglia. The roles of NF-κB and MAPK signalling in the actions of BFE were also investigated. BFE (25–200 μg) inhibited the production of PGE2, nitrite, tumour necrosis factor-α(TNFα), and interleukin-6 (IL-6) as well as COX-2 and iNOS protein expressions in LPS-activated microglial cells. Further studies to elucidate the mechanism of anti-inflammatory action of BFE revealed interference with nuclear translocation of NF-κBp65 through mechanisms involving inhibition of IκB degradation. BFE prevented phosphorylation of p38, but not p42/44 or JNK MAPK. It is suggested thatBridelia ferrugineaproduces anti-inflammatory action through mechanisms involving p38 MAPK and NF-κB signalling.


2016 ◽  
Vol 46 ◽  
pp. 15-15
Author(s):  
Michiko Mori ◽  
Prajakta Jogdand ◽  
Caroline Sanden ◽  
Jimmie Jönsson ◽  
Ravi Krishnan ◽  
...  

2018 ◽  
Vol 29 (6) ◽  
pp. 659-669 ◽  
Author(s):  
Newman Osafo ◽  
David D. Obiri ◽  
Aaron O. Antwi ◽  
Oduro K. Yeboah

AbstractBackgroundOur earlier studies had given evidence of the traditional application ofXylopia aethiopicain the management of inflammation. The principal constituent obtained from its bio-fractionation is xylopic acid. It is a crystalline diterpene that belongs to the class of kauranes. This work sets out to investigate the anti-inflammatory potential of the xylopic acid isolated from the dried fruit ofX. aethiopica.MethodsA preliminary anti-inflammatory study, using the protein denaturation model, andin vivoanti-inflammatory assay were employed in the investigation of acute inflammation. The modulation of the effect of the pro-inflammatory markers histamine, serotonin, bradykinin, and prostaglandin E2by xylopic acid was investigated byin vivomice paw oedema models.ResultsXylopic acid showed a concentration-dependent inhibition of albumen denaturation with an IC50of 15.55 μg mL−1. Xylopic acid (10, 30, 100 mg kg−1) inhibited the maximal oedema and the average paw thickness (oedema) over the period of each study considerably for all phlogistic agents employed (i.e. carrageenan, histamine, serotonin, bradykinin, and prostaglandin E2) in the inflammation induction for both prophylactic and therapeutic protocols.ConclusionThis study establishes that xylopic acid has anti-inflammatory action in acute inflammation.


2019 ◽  
Vol 15 (5) ◽  
pp. 521-536 ◽  
Author(s):  
Natalya Agafonova ◽  
Evgeny Shchegolkov ◽  
Yanina Burgart ◽  
Victor Saloutin ◽  
Alexandra Trefilova ◽  
...  

Background: Formally belonging to the non-steroidal anti-inflammatory drug class pyrazolones have long been used in medical practices. Objective: Our goal is to synthesize N-methylated 1-aryl-3-polyfluoroalkylpyrazolones as fluorinated analogs of antipyrine, their isomeric O-methylated derivatives resembling celecoxib structure and evaluate biological activities of obtained compounds. Methods: In vitro (permeability) and in vivo (anti-inflammatory and analgesic activities, acute toxicity, hyperalgesia, antipyretic activity, “open field” test) experiments. To suggest the mechanism of biological activity, molecular docking of the synthesized compounds was carried out into the tyrosine site of COX-1/2. Conclusion: The trifluoromethyl antipyrine represents a valuable starting point in design of the lead series for discovery new antipyretic analgesics with anti-inflammatory properties.


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