• 대한의생명과학회지
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• 제17권3호
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• pp.225-230
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• 2011

Indirubin is the active ingredient of Danggui Longhui Wan, a mixture of plants that is used in traditional Chinese medicine to treat chronic diseases. In this study we investigated the anti-inflammatory effects of an indirubin derivative, indirubin-3’-monoxime-5-sulphonic acid (I3M-5S, $C_{16}H_{11}N_3O_5S$). We found that I3M-5S inhibits the production of various inflammatory mediators such as nitric oxide (NO) and prostaglandin $E_2$ ($PGE_2$) as well as inflammatory cytokines, tumor necrosis factor-${\alpha}$ and interleukin-6 in lipopolysaccharide (LPS) stimulated murine macrophage, RAW264.7 cells. In addition, the expression of inducible nitric oxide synthase and cyclooxygenase-2, which are essential enzymes to produce NO and $PGE_2$, respectively, was blocked by I3M-5S treatment in LPS-stimulated RAW264.7 cells. Present data suggest that I3M-5S exhibits potent anti-inflammatory activity in cultured macrophages and merit further study as potential therapeutic agents for inflammatory disorders.

• 한방재활의학과학회지
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• 제30권3호
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• pp.71-87
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• 2020

Objectives Even though the various alternative herbal medicine has applied for osteoarthritis (OA) treatment, its scientific proof remains uncertain. The aim of the present study evaluates the effects of Chulbu-tang on inflammatory responses in a monosodium iodoacetate (MIA)-induced osteoarthritis rat model. Methods OA rat model was established by MIA injection in intra-joint of rats. 7 days after, OA rats except OA control rats were administrated Chulbu-tang (100 or 200 mg/kg) or Indomathacin (5 mg/kg) once a day for 14 days. The weight-bearing ability of hind paws were measured when group isolation 0, 7, and 14 days. Western blotting was performed to examine the knockdown/overexpressing efficiency of Chulbu-tang. In addition, cartilage destruction was measured histologically. Results Chulbu-tang treatment significantly reduced the protein expressions of inflammatory mediators such as inducible nitric oxide synthase and cyclooxygenase 2, and inhibited inflammatory cytokines including tumor necrosis factor alpha, interleukin (IL)-1β, and IL-6 through nuclear factor-kappa B (NF-κB) inactivation. Moreover, anti-oxidant enzymes such as superoxide dismutase and glutathione peroxidase-1/2 through nuclear factor-erythroid 2-related factor 2 (Nrf2) pathway significantly increased. Our findings indicate that Chulbu-tang has the potential therapeutic effect on OA through inhibiting the inflammatory responses via inactivating NF-κB signaling pathway. In addition, upregulation of Nrf2 led to anti-oxidant effects. Conclusions Taken together, Chulbu-tang is believed to have antioxidant, anti-inflammatory effects, and cartilage protection for arthritis-causing rats.

• 한국축산식품학회지
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• 제35권3호
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• pp.293-298
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• 2015

Porcine placenta extract (PPE) is known to possess anti-inflammatory properties owing to its high concentration of bioactive substances. However, the need to eliminate blood-borne infectious agents while maintaining biological efficacy raises concerns about the optimal method for sterilizing PPE. Therefore, the objective of this study was to compare the effects of the standard pressurized heat (autoclaving) method of sterilization with γ-irradiation on the anti-inflammatory effects of PPE. The anti-inflammatory actions of these two preparations of PPE were evaluated by measuring their inhibitory effects on the production of NO, the expression of iNOS protein, and the expression of iNOS, COX2, TNF-α, IL-1β, and IL-6 mRNA in lipopolysaccharide-stimulated RAW 264.7 cells. Compared with autoclaved PPE, γ-irradiated PPE showed significantly greater inhibition of NO production and iNOS protein expression, and produced a greater reduction in the expression of iNOS, COX2, TNF-α, IL-1β, and IL-6 mRNA. These results provide evidence that the sterilization process is crucial in determining the biological activity of PPE, especially its anti-inflammatory activity. Collectively, our data suggest that γ-irradiated PPE acts at the transcriptional level to effectively and potently suppresses the production of NO and the expression of pro-inflammatory cytokines.

• Clinical and Experimental Pediatrics
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• 제53권11호
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• pp.936-941
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• 2010

The systematic approach to pharmacologic treatment is typically to begin with the safest, simplest, and most conservative measures. It has been realized that the more rapidly inflammation is under control, the less likely it is that there will be permanent sequelae. Nonsteroidal anti-inflammatory drugs (NSAIDs) are the mainstay of initial treatment for inflammation. In addition, the slow-acting antirheumatic drugs (SAARDs) and disease-modifying antirheumatic drugs (DMARDs) have efficacy of anti-inflammatory action in children with chronic arthritis. New therapeutic modalities for inflammation, such as etanercept and infliximab, promise even further improvements in the risk/benefit ratio of treatment. It is not typically possible at the onset of the disease to predict which children will recover and which will go on to have unremitting disease with lingering disability or enter adulthood with serious functional impairment. Therefore, the initial therapeutic approach must be vigorous in all children.

• 생약학회지
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• 제38권4호
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• pp.334-338
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• 2007

Roots of Rumex crispus (Rc) (Polygonaceae) has been used as therapeutic agents of acute and chronic cutaneous diseases, cathartics, fever and jaundice in folk medicines. Recently, Seeds of Rc has known as a digestive, an anticancer agent and a remedy of acute hepatitis, among many traditional folk medicines. So far it isn't reported about pharmacological effects of Rumecis Semen. The present study describes the preliminary evaluations of biological activities, anti-inflammatory activity (AA, Carrageenan) analgesic activity (writhing test), and hepatoprotective activities ($CCl_4$), of its methanol extract, ethyl acetate fraction and butanol fraction. Among them butanol fraction showed the highest activity in analgesic acivity.

• 약학회지
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• 제33권2호
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• pp.87-100
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• 1989

Salicylic acids as anti-inflammatory agents were analyzed by ab initio, quantum chemical methods to study the possible modes of binding to the receptor. As the result of multiple regression analysis of reactivity indices and interpretation of normalized frontier orbital charges of drugs, potency seems to be related to energy of HOMO and LUMO at the 5 position of benzene ring, and in the 5-phenyl substituted case, the para position of substituting ring is important. The binding occurs first at the positive site of its receptor. The charge density exhibited by the frontier orbitals suggests that charge moves from receptor site to carboxyl group. The electrostatic orientation effect makes an important contribution to the binding of the active molecules to their receptors. Also the electrostatic potential model may be able to rationalize the source of activity or inactivity of the drugs under investigation.

• Journal of Digestive Cancer Research
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• 제8권2호
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• pp.77-80
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• 2020

Gastric cancer is one of the leading causes of cancer-related deaths worldwide. The increased expression of cyclooxygenase (COX)-2 has been implicated in the development and progression of gastric cancers. A number of recent studies have been published evaluating the chemopreventive effect of aspirin and non steroidal anti inflammatory drungs (NSAIDs) against gastric cancer. Aspirin and NSAIDs use may reduce the risk of gastric cancer incidence and death, whereas other studies have reported contradictory results. Therefore, further study should be needed to clarify the role of aspirin and NSAIDs in the chemoprevention of gastric cancer.

• Archives of Pharmacal Research
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• 제29권10호
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• pp.849-858
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• 2006

Previous screening of the pharmacological action of Gastrodia elata (GE) root (Orchidaceae) showed that methanol (MeOH) extracts have significant anti-inflammatory properties. The antiinflammatory agents of GE, however, remain unclear. In this experiment, MeOH extracts of GE were fractionated with organic solvents for the anti-inflammatory activity-guided separation of GE. Eight phenolic compounds from the ether (EtOEt) and ethyl acetate (EtOAc) fractions were isolated by column chromatography: 4-hydroxybenzaldehyde (I), 4-hydroxybenzyl alcohol (II), benzyl alcohol (III), bis-(4-hydroxyphenyl) methane (IV), 4(4'-hydroxybenzyloxy)benzyl-methylether (V), 4-hydroxy-3-methoxybenzyl alcohol (VI), 4-hydroxy-3-methoxybenzaldehyde (VII), and 4-hydroxy-3-methoxybenzoic acid (VIII). To investigate the anti-inflammatory and anti-oxidant activity of these compounds, their effects on carrageenan-induced paw edema, arachidonic acid (AA)-induced ear edema and analgesic activity in acetic acid (HAc)-induced writhing response were carried out in vivo; cyclooxygenase (COX) activity, reactive oxygen species (ROS) generation in rat basophilic leukemia (RBL 2H3) cells and 1,1-diphenyl-2-picryl-hydroazyl (DPPH) scavenging activity were determined in vitro. These phenolic compounds not only had anti-inflammatory and analgesic properties in vivo, but also inhibited COX activity and silica-induced ROS generation in a dose-dependent manner. Among these phenolic compounds, compound VII was the most potent anti-inflammatory and analgesic. Compound VII significantly inhibited silica-induced ROS generation and compound VI significantly increased DPPH radical scavenging activity. Compounds I, II and III significantly inhibited the activity of COX-I and II. These results indicate that phenolic compounds of GE are anti-inflammatory, which may be related to inhibition of COX activity and to anti-oxidant activity. Consideration of the structure-activity relationship of the phenolic derivatives from GE on the anti-inflammatory action revealed that both C-4 hydroxy and C-3 methoxy radicals of benzyl aldehyde play an important role in anti-inflammatory activities.

• 한국수산과학회지
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• 제47권6호
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• pp.770-775
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• 2014

The green microalga of the genus Nannochloropsis (class Eustigmatophyceae) is a leading candidate for biofuel production due to its ability to accumulate high oil content (28.7% of cellular ash-free dry weight). We investigated the anti-inflammatory and anticancer activities of sterol-rich fraction from nannochloropsis oculata n-hexane (NOH) extract after saponification of the microalga. Among the fractions with n-hexane, chloroform and ethyl acetate, the n-hexane fraction showed the highest anti-inflammatory activity in LPS-stimulated RAW 264.7 macrophage as well as anticancer activity against human leukemia HL-60 cells without the cytotoxity. And the sterol-rich fraction was obtained from the n-hexane fraction by open silica column under the gradient solvent condition with 100% hexane (1L), hexane : ethyl acetate (20 : 1, 10 : 1, 5 : 1, 1 : 1, v/v). Among the four fractions (NOH-1~4), especially NOH-1 contained the highest content of sterols. NOH1 showed the highest HL-60 (about 85%) and NO inhibitory activities at the concentration of $100{\mu}g/mL$. These results demonstrated that the sterol-rich fraction from N. oculata might be a useful candidate as anti-inflammatory and anticancer agents for anti-inflammatory and anticancer activity.

• 한국미생물·생명공학회지
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• 제43권4호
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• pp.391-395
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• 2015

본 연구에서는 번행초의 추출물과 분획물의 항염증 효과 및 항암 활성에 대해 연구하였다. 번행초의 항염증 활성은 $1{\mu}g/ml$ LPS로 유도되는 NO 및 IL-$1{\beta}$의 생성이 억제됨을 통해 확인되었다. IL-6 및 $TNF-{\alpha}$도 $1{\mu}g/ml$ LPS로 자극된 RAW264.7 세포에서 다당류 추출물을 처리한 후 생성이 감소되었다. 나아가 HX 분획물은 GM-CSF의 생성을 강력하게 억제하는 것으로 확인되었다. 또한 Sarcoma 180을 미리 주사한 ICR 마우스에 MeOH과 다당 추출물을 100 mg/kg/day 복강내 투여시 16.67%의 수명 연장 효과가 관찰되었다. 이상의 결과는 번행초를 이용하여 효과적인 항염증 및 항암제 개발을 위한 사전조사로써 중요한 결과를 제공한다.