• Archives of Pharmacal Research
• /
• v.28 no.7
• /
• pp.848-853
• /
• 2005

Synurus deltoides was previously found to possess significant anti-inflammatory activity especially against chronic inflammation, and strong analgesic activity in vivo. In this study, new anti-inflammatory formulation containing S. deltoides extract as a major ingredient was prepared and in vivo activity was evaluated. The plausible action mechanism was also investigated. The new formulation (SAG) contains 1 part of S. deltoides extract, 0.9 part of Angelica gigas extract and 0.9 part of glucosamine sulfate (w/w). SAG inhibited dose-dependently edematic response of arachidonic acid (AA)- and 12-O-tetradecanoyl 13-acetate (TPA)-induced ear edema in mice, which is an animal model of acute inflammation. SAG showed 44.1 % inhibition of AA-induced ear edema at an oral dose of 50 mg/kg. In an animal model of chronic inflammation, SAG clearly reduced the edematic response of 7 -day model of multiple treatment of TPA (38.1 % inhibition at 200 mg/kg/day). Furthermore, SAG (50-800 mg/kg/day) as well as S. deltoides extract (285 mg/kg/day) significantly inhibited prostaglandin $E_2$ production from the skin lesion of the animals of 7-day model. These results were well correlated with in vitro finding that SAG as well as S. deltoides extract reduced cyclooxygenase (COX)-1- and COX-2-induced prostanoid production, measured in mouse bone marrow-derived mast cells. Therefore, these results suggest that SAG possesses anti-inflammatory activity in vivo against acute as well as chronic inflammatory animal models at least in part by inhibition of prostaglandin production through COX-1/COX-2 inhibition. And COX inhibition of SAG is possibly contributed by S. deltoides extract among the ingredients. Although the anti-inflammatory potencies of SAG were less than those of currently used anti-inflammatory drugs, this formulation may have beneficial effect on inflammatory disorders as a neutraceutical.

• Proceedings of the Plant Resources Society of Korea Conference
• /
• 2019.10a
• /
• pp.66-66
• /
• 2019

Heracleum moellendorffii roots (HM-R) have been long treated for inflammatory diseases such as arthritis, backache and fever. However, an anti-inflammatory effect and the specific mechanism of HM-R were not yet clear. In this study, we for the first time explored the anti-inflammatory of HM-R. Results: HM-R dose-dependently blocked LPS-induced NO and PGE2 production. In addition, HM-R inhibited LPS-induced overexpression of iNOS, COX-2, $IL-1{\beta}$ and IL-6 in RAW264.7 cells. HM-R inhibited LPS-induced $NF-{\kappa}B$ signaling activation through blocking $I{\kappa}B-{\alpha}$ degradation and p65 nuclear accumulation. Furthermore, HM-R inhibited MAPK signaling activation by attenuating the phosphorylation of ERK1/2, p38 and JNK. HM-R increased nuclear accumulation of Nrf2 and HO-1 expression. However, NAC reduced the increased nuclear accumulation of Nrf2 and HO-1 expression by HM-R. In HPLC analysis, falcarinol was detected from HM-R as an anti-inflammatory compound. These results indicate that HM-R may exert anti-inflammatory activity by inhibiting $NF-{\kappa}B$ and MAPK signaling, and activating ROS/Nrf2/HO-1 signaling. From these findings, HM-R may have potential to be a candidate for the development of anti-inflammatory drugs.

• Journal of Applied Biological Chemistry
• /
• v.66
• /
• pp.29-38
• /
• 2023

Recent studies have highlighted the link between diseases and inflammation across our lifespan. Our sedentary lifestyle, high-calorie diet, chronic stress, chronic infections, and exposure to pollutants and xenobiotics, collectively intensify the course and recurrence of infections and inflammation in our bodies, promoting the prevalence of chronic diseases and aging. Given such phenomena and considering additional factors such as the frequency of prescription, and easy access to over-the-counter drugs, the need for anti-inflammatory therapeutics is ever-increasing. However, the readily available anti-inflammatory treatment option comes with a greater risk of side effects or high cost (biologics). Therefore in this growing competition of discovering and developing new potent anti-inflammatory drugs, we focused on utilizing the established knowledge of traditional medicine to find lead compounds. Since lead optimization is an indispensable step toward drug development, we applied this concept for the production of potent anti-inflammatory compounds achieved by structural modification of flavonoids. The derivative obtained through acetylation of myricetin, 3,3',4',5,5',7-hexaacetate myricetin, showed a greater inhibitory effect in the production of pro-inflammatory mediators such as nitric oxide, Prostaglandin E₂, and pro-inflammatory cytokines like interleukin-6, interleukin1β, in lipopolysaccharide-stimulated RAW264.7 mouse macrophage cells compared to myricetin. The increased potency of inhibition was in conjunction with an increased inhibitory effect on inducible nitric oxide synthase and cyclooxygenase-2 proteins. Through such measures, this study supports lead optimization for well-established lead compounds from traditional medicine using a simpler and greener chemistry approach for the purpose of designing and developing potent anti-inflammatory therapeutics with possibly fewer side effects and increased bioavailability.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
• /
• v.21 no.2
• /
• pp.46-53
• /
• 2008

Background and Objectives : The aim of this study was to investigate the anti-oxidant, anti-allergic and anti-inflammatory ability of the Taglisodog-eum(SHE) extract on the RAW 264.7 and EL4 cells Materials and Methods : Three types of experiments were implemented for this study: first, the experiment to study the anti-oxidant effect of SHE using Riboflavin; second, in vitro experiment to investigate the inhibition of Th 2 cell differentiation by SHE using EL4 cells (IL-4 mRNA expression); third, the suppression of $NF-{\kappa}B$ activation using RAW 264.7 cells (iNOS and COX-2 mRNA expression). Results : The anti-oxidant ability of SHE were dose-dependantly increased. From in vitro, the LPS-induced iNOS and COX-2 mRNA expression were dose-dependantly decreased in the RAW264.7 cells treated with SHE and the PMA-induced IL-4 mRNA expression were also dose-dependantly decreased in EL4 cells. $NF-{\kappa}B$ activation was suppressed, and iNOS & COX-2 production were inhibited by SHE Conclusion : The results suggest that SHE has dose-dependant anti-oxidant ability, and has anti-allergic and anti-inflammatory effects through the suppression of $NF-{\kappa}B$ activation and the inhibition of Th 2 cell differentiation.

• Biomolecules & Therapeutics
• /
• v.3 no.1
• /
• pp.34-37
• /
• 1995

Non-steroidal anti-inflammatory drugs (NSAIDs) have been known as inhibitors of the folate-requiring enzymes. In the present work, we have expanded on these observations and have investigated the inhibitory effects of NSAIDs on Lactobacillus casei thymidylate synthase expressed in E. coli. NSAIDs including sulphasalizine, salicylic acid, indomethacin and mefenamic acid were found to be competitive inhibitors with respect to folate of Lactobacillus casei thymidylate synthase. In contrast, aspirin and the antipyretic-analgesic drugs acetaminophen and antipyrine were weak inhibitors of the enzyme. Structure-activity correlation suggests that an aromatic ring with a side chain containing a carboxylic acid is a requirement for competitive inhibition of the thymidylate synthase. The results are consistent with the hypothesis that the antifolate activity of NSAIDs, and hence cytostatic consequences, are important factors in producing anti-inflammatory activity and aspirin exerts its anti-inflammatory effects after its conversion into salicylic acid, which possesses greater antifolate activity than its parent compound.

• Natural Product Sciences
• /
• v.8 no.3
• /
• pp.97-99
• /
• 2002

In the present study, Pisonia grandis leaves were extracted with chloroform and methanol. The extracts were vacuum dried to yield the respective chloroform (CE) and methanol extract (ME). CE and ME were evaluated for analgesic, anti-inflammatory (acute and chronic) and diuretic activity at 2 dose levels (250 and 500 mg/kg). Significant analgesic and anti-inflammatory activities were associated with CE and ME. CE at the dose level of 500 mg/kg was found to exhibit equivalent chronic anti-inflammatory activity as diclofenac at 50 mg/kg dose level. Significant diuretic activity was exhibited by ME. Graded dose response for all the activities were observed for the extracts.

• Advances in Traditional Medicine
• /
• v.9 no.4
• /
• pp.320-325
• /
• 2009

The pharmacological interest coupled with traditional uses (antidiarrhoeal, antiseptic, analgesic etc) prompted us to test for anti-inflammatory, antinociceptive and diuretic activitities of Trema (T.) orientalis Linn. The crude methanolic leaves extract of T. orientalis was investigated for its possible anti-inflammatory activities using carrageenin induced rat paw edema model and cotton pellet implantation method in mice. Then the extract analyzed for its antinociceptive activities by acetic acid induced writhing model in mice. The extract possessed significant anti-inflammatory activity in both models at the doses of 200 and 400 mg/kg body weight of mice. Moreover, the extract showed significantly reduced the number of acetic acid-induced abdominal constriction in mice of 200 and 400 mg/kg body weight. The extract also showed positive diuretic activity in albino mice.

• Korean Journal of Pharmacognosy
• /
• v.27 no.3
• /
• pp.184-189
• /
• 1996

Ohyaksungisan, combined preparation of crude drugs, has been used for hemiplegia, arthralgia and paralysis in traditional Korean medicine. The anti-inflammatory activity of the aqueous extract from Ohyaksungisan(OSSE) was investigated on acetic acid-induced edema and adjuvant arthritis in rats. Acute toxicity and analgesic action in mice were also examined. Its anti-inflammatory activity on 5% acetic acid-induced edema and adjuvant arthritis was observed with oral administration. The acute toxicity showed 10% mortality at 2400 mg/kg (p.o), but was not showed at 1200 mg/kg (i.p). OSSE was showed to have significant analgesic action (P<0.05) at 150 mg/kg and this action was strengthened at 300, 600 mg/kg. The anti-inflammatory effect was showed significant preventive effect on the hind paw edema from 90 min. and the adjuvant arthritis, when orally administered for 19 days. showed significant inhibitory effect on the hind paw edema from the 5th day.

• Korean Journal of Plant Resources
• /
• v.28 no.3
• /
• pp.305-311
• /
• 2015

This study investigated in vitro antioxidant, anti-inflammatory and cytotoxicity on human lung epithelial A549 cells of different solvent extracts from Jerusalem artichoke (Helianthus tuberosus L.) tuber. The EtOH extract contained amounts of phenolics (22.20 tannic acid equivalent ㎎/ɡ) and exhibited the highest antioxidant activity and anti-inflammatory activity. Several methods were employed for measure the antioxidant activity: 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity (IC₅₀ = 206.79 ㎍/㎖), reducing power activity (21.26 ascorbic acid equivalent ㎎/ɡ) and total antioxidant activity (19.05 ascorbic acid equivalent ㎎/ɡ). Meantime, the EtOH extract inhibited the NO production completely with a concentration of 800 ㎍/㎖. Besides, the H₂O extract exhibited more potent effect on human lung epithelial A549 cells. This study suggested that Jerusalem artichoke tuber had antioxidant, anti-inflammatory and cytotoxicity on human lung epithelial A549 cells.

• Archives of Pharmacal Research
• /
• v.28 no.5
• /
• pp.509-517
• /
• 2005

A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4- chloro-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analygesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.