• Title/Summary/Keyword: Antiinflammatory

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Inclusion Complex of Analgesic and Antiinflammatory agents with Cyclodextrins (I): Enhancement of Dissolution of Ibuprofen by $2-Hydroxypropyl-{\beta}-cyclodextrin$ (시클로덱스트린과 소염진통제 간의 포접복합체에 관한 연구(I): 2-히드록시프로필-${\beta}$-시클로덱스트린에 의한 이부프로펜의 용출 증가)

  • Oh, In-Joon;Park, Jeong-Gyu;Lee, Yong-Bok;Shin, Sang-Chul
    • Journal of Pharmaceutical Investigation
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    • v.23 no.1
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    • pp.11-18
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    • 1993
  • Inclusion complex of ibuprofen with $2-Hydroxypropyl-{\beta}-cyclodextrin\;(HP-{\beta}-CD)$ in aqueous solution and in the solid state was evaluated by the solubility method and the instrumental analysis such as infrared spectroscopy, thermal analysis and x-ray diffractometry. The aqueous solubility of ibuprofen was increased linearly with the increase in the concentration of $HP-{\beta}-CD$, showing an $A_L$ type phase solubility diagram. The results showed that the dissolution rate of ibuprofen was significantly increased by complexation with $HP-{\beta}-CD$. $Ibuprofen-HP-{\beta}-CD$ complex enhanced the mean plasma concentration levels and the area under plasma concentration-time curve after oral administration compared to those of the drug alone. It is concluded that the complex of ibuprofen with $HP-{\beta}-CD$ increases the dissolution rate and improves the bioavailability of the ibuprofen by the formation of a water-soluble complex.

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Screening of Antioxidative Activities and Antiinflammatory Activities in Local Native Plants (국내자생식물 추출물의 항산화 및 항염 활성 탐색)

  • Kim, Han-Hyuk;Kwon, Joo-Hee;Park, Kwan-Hee;Kim, Manh-Heun;Oh, Myoeng-Hwan;Choe, Kang-In;Park, Sang-Hee;Jin, Hye-Young;Kim, Sung-Sik;Lee, Min-Won
    • Korean Journal of Pharmacognosy
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    • v.43 no.1
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    • pp.85-93
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    • 2012
  • 181 kinds of local native plants were selected by its anti-inflammatorial folk medicinal uses and evaluated it antioxidative and inhibitory activity of nitric oxide (NO) production in lipopolysaccharide (LPS)-induced 264.7 macrophage cells. Among the 181 kinds of plants, 99 species showed potent antioxidative activities and 20 extracts showed inhibitory activity towards nitric oxide production by more than 70% at a concentration of $100{\mu}g/mL$. Therefore, these plants should be considered promising candidates for the treatment of inflammatory diseases accompanying overproduction of NO.

In vitro Antiinflammatory Activity of Amygdalin in Murine Macrophage Raw 264.7 Cells (Amygdalin의 Murine Macrophage Raw 264.7 세포에서 in vitro 항염효과)

  • Shin, Kyung-Min;Park, Young-Mi;Kim, In-Tae;Hong, Seon-Pyo;Hong, Jung-Pyo;Lee, Kyung-Tae
    • Korean Journal of Pharmacognosy
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    • v.34 no.3 s.134
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    • pp.223-227
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    • 2003
  • In the present study, anti-inflammatory activity of amygdalin isolated from persicae Semen have been evaluated on lipopolysaccharide (LPS)-induced release of nitric oxide (NO), prostaglandin $E_2\;(PGE_2)$ and tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$) by the macrophage RAW 264.7 cells. Amygdalin significantly inhibited generation of NO and $TNF-{\alpha}$ on LPS-stimulated RAW264.7 cells in a concentration-dependent manner. Consistent with these observations, the expression of inducible NO synthase (iNOS) enzyme was also inhibited by amygdalin in a concentration-dependent manner. However, amygdalin did not show any influence on the synthesis of $PGE_2$ and the expression of COX-2. Thus, this study suggests that amygdalin-mediated inhibition of iNOS expression, and $TNF-{\alpha}$ release may be one of the mechanisms responsible for the anti-inflammatory effects of Persicae Semen.

Clinical Study on a Case of Cervical Myelopathy with Additional Scolopendrae Corpus Pharmacopuncture (오공 약침을 병행한 경추증성 척수증 환자 1례에 대한 임상적 고찰)

  • Kwon, Ho-Young;Kim, Jeong-Hwan
    • Korean Journal of Acupuncture
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    • v.26 no.4
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    • pp.225-235
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    • 2009
  • Objective : The purpose of this study was to report a case of a treatment with Scolopendrae Corpus Herbal-Acupuncture for one patient suffering from the Cervical Myelopathy. Scolopendrae Corpus Herbal-Acupuncture has been used as a analgesics and antispasmodics in the oriental medicine and reported to have antiinflammatory effect, sedative action and immunity enhancing activity, on one patient suffering from the Cervical Myelopathy. Methods : TThe patient was treated with Scolopendrae Corpus Herbal-Acupuncture, acupuncture, herbal medication. Scolopendrae Corpus Pharmacopuncture was administered two or three times per week and we injected 0.2~1.0 ml of Scolopendrae Corpus Pharmacopuncture to the patient's neck and both arms. The improvement of the symptoms was evaluated by JOA score(Japanese Orthopedic Association score), Nurick grading, VAS(Visual Analog Scale), reflex testing, Finger escape sign, Grip and Release test. Result : After 5 weeks of treatment, the patient's JOA score, Nurick grading and VAS were improved from 12 to 16, from grade III to grade II and from 10 to 3 respectively. The movement and power of upper and lower limbs were restored to nearly normal range.

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The Effects of Zingiber officinale Roscoe Extracts on Mouse $IFN-{\gamma}$ and IL-10 Production (생강 추출물 투여가 전구염증성 사이토카인 $IFN-{\gamma}$와 항염증성 사이토카인 IL-10 분비량에 미치는 영향)

  • Ryu, Hye-Sook
    • The Korean Journal of Food And Nutrition
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    • v.20 no.3
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    • pp.259-264
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    • 2007
  • Ginger(Zingiber officinale Roscoe) has been used as a raw material in many various traditional preparations since the ancient times. As a component of traditional health products, ginger is known to be effective as an appetite enhancer, and has anti-cold and anti-inflammatory activities. This study was performed to investigate the immunomodulative effects of Zingiber officinale Roscoe in mice, using ex vivo experiments. In order to elucidate ginger's immunomodulative effects of Ginger, water extracts were orally administered to mice, and isolated macrophages were used as the experimental model. To identify the ex vivo effects, six to seven week old Balb/c mice were fed a chow diet ad libitum and the ginger water extracts were administered orally every other day for two or four weeks at two different concentrations(50 and 500 mg/kg b.w.). The results show that IL-IO and $IFN-{\gamma}$ were detected in the 500 mg/kg b.w. supplemented group with LPS stimulation in all cases. Also, the $IFN-{\gamma}$ /IL-10 ratio ranged from 3~5 with mitogen stimulation such as Con A and LPS. In conclusion, this study suggests that ginger extracts may enhance the immune function by regulating the cytokine(IL-10 and $IFN-{\gamma}$) production capacity of activated macrophages in mice.

General Pharmacology of DWQ-013, A New Synthetic Quinolone Antibiotics (Effects on the Central Nervous System) (신규 합성 퀴놀론계 항생물질(DWQ-013)의 일반 약리 작용 -중추신경계에 대한 작용-)

  • Lim, Seung-Wook;Kim, Young-Man;Yu, Young-Hyo;Lee, Jae-Wook
    • YAKHAK HOEJI
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    • v.38 no.5
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    • pp.586-594
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    • 1994
  • The general pharmacological effects of DWQ-013, a new synthetic quinolone antibacterial agent, were examined on the central nervous system in experimentral animals and the following results were obtained. Drug interaction of DWQ-013 with theophylline, fenbufen and nonsteroidal antiinflammatory drugs was also examined. DWQ-013 decreased touch escape effect on the general behavior and decreased body temperature at a concentration of 1000 mg/kg in mice. But DWQ 013 had no effect on the locomotor activity, rotarod perfomance and traction test in mice. Furthermore, DWQ-013 increased pentobarbital-induced sleeping time and affected the onset time in acetic acid-induced writhing test in mice. DWQ-013 reduced onset time and death time on strychnine-induced convulsions and death time on pentylenetetrazole-induced convulsions at a concentration of 1000 mg/kg in mice. But, the drug had no effect on the electroshock. DWQ-013 did not interact with fenbufen and any other NSAIDs but it did interact with theophylline. From these results, it could be suggested that DWQ-013 had less pharmacological effect than other quinolones on the central nervous system.

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The Crystal Structure of Acemetacin Monohrdrate $(C_{21}H_{18}NO_6Cl-H_2O)$, A Non-Steroidal Antiinflammatory Agent

  • Kim, Yang-Bae;Kim, Jeong-Ae;Park, Yeong-Il
    • Archives of Pharmacal Research
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    • v.16 no.2
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    • pp.134-139
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    • 1993
  • The molecular structure of acemetacin, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid carboxymethyl ester, was determined by single cystal X-ray diffraction analysis. The compound was recrystallized from a mixture of acetone and water in triclinic, space group P1, with a=7.796(1), b=10.245(2), c=13.542(3)$\AA,\;\alpha=97.35(1),\;\beta=96.34(1),\;\gamma=107.06(1)^\circ$, and Z=2. The calculated density is 1.422; the observed value is $1.42\;g/cm^3$. The structure was solved by the direct method and refined by full matrix least-squares procedure to the final R value of 0,037 for 2960 independent reflections. There are water molecules, which are thought to be co-crystallized during the evaporation procedure, with the ratio of one water per compound molecule in the crystal. The conformation of the compound is found to be very similar to that of indomethacin. The molecules are stabilized by three O-H.....O type intermolecular hydrogen bonds between the oxygen of water molecule and those of the compound.

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Role of ginseng in the neurovascular unit of neuroinflammatory diseases focused on the blood-brain barrier

  • Kim, Minsu;Mok, Hyejung;Yeo, Woon-Seok;Ahn, Joong-Hoon;Choi, Yoon Kyung
    • Journal of Ginseng Research
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    • v.45 no.5
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    • pp.599-609
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    • 2021
  • Ginseng has long been considered as an herbal medicine. Recent data suggest that ginseng has antiinflammatory properties and can improve learning- and memory-related function in the central nervous system (CNS) following the development of CNS neuroinflammatory diseases such as Alzheimer's disease, cerebral ischemia, and other neurological disorders. In this review, we discuss the role of ginseng in the neurovascular unit, which is composed of endothelial cells surrounded by astrocytes, pericytes, microglia, neural stem cells, oligodendrocytes, and neurons, especially their blood-brain barrier maintenance, anti-inflammatory effects and regenerative functions. In addition, cell-cell communication enhanced by ginseng may be attributed to regeneration via induction of neurogenesis and angiogenesis in CNS diseases. Thus, ginseng may have therapeutic potential to exert cognitive improvement in neuroinflammatory diseases such as stroke, traumatic brain injury, multiple sclerosis, Parkinson's disease, and Alzheimer's disease.

Antiinflammatory and Antiangiogenic Activities of Flavonoids Isolated from Belamcandae Rhizoma

  • Jung, Sang-Hoon;Ahn, Kwang-Seok;Lee, Yeon-Sil;Shin, Kuk-Hyun;Kim, Yeong-Shik
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.202.4-203
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    • 2003
  • The present study was carried out to clarify whether isoflavonoids isolated from Belamcandae Rhizoma (Iridaceae) inhibit inflammation and angiogenesis by the experimental methods in vitro and in vivo. Among the isolated isoflavonoids, such as irigenin, irisflorentine, and iristectorene B inhibited nitric oxide (NO) production, as measured by nitrite formation at 3-30 ${\mu}M$. Also these compounds reduced cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) enzyme expression in a concentration dependent manner, when measured by western blotting, at 3-30 ${\mu}M$. Irigenin, irisflorentine and iristectoren B decreased angiogenesis of chick embryos in the chorioallantoic membrane assay. These compounds also reduced the proliferation of calf pulmonary arterial endothelial (CPAE) cells and found to possess relatively weak gelatinase/collagenase inhibitory activity in vitro. These compounds, when administered subcataneously at the dose of 30mg/kg for 20 days to mice implanted with murine Lewis lung carcinoma (LLC), caused a significant inhibition of tumor volume. Therefore, antiangiogenic activities of isoflavonoids from Belamcandae Rhizoma might be due to antiproliferative activities under inhibition the induction of COX-2 and iNOS enzyme.

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Sesamin attenuates neuronal damage through inhibition of microglial activation following global cerebral ischemia in rats

  • Kong, Minjung;Hong, Sung In
    • The Korea Journal of Herbology
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    • v.28 no.2
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    • pp.1-7
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    • 2013
  • Objectives : Sesamin, a major lignan in sesame seeds, has been reported to have neuroprotective effects against in vitro ischemia and in vivo MCAo-reperfusion cerebral ischemia model, however, there is no reports in an in vivo global cerebral ischemia model. The purpose of the study was to investigate the neuroprotective effect of sesamin in global cerebral ischemia induced by four-vessel occlusion (4-VO) in rats through inhibition of microglial activation in this model. Methods : The neuroprotective effects were investigated using a 10 min of 4-VO ischemia rat model by measuring intact pyramidal neurons in the CA1 region of the hippocampus using Nissle staining. The antiinflammatory or reducing neurotoxicity effect was investigated using immunohistochemisty, RT-PCR and western blot analysis of inflammatory or neurotoxic mediators. Results : Intraperitoneal injection of sesamin at doses of 0.3, 1.0, 3.0, and 10.0 mg/kg at 0 min and 90 min after ischemia conferred 26.6%, 30.1%, 42.5%, and 30.5% neuroprotection, respectively, compared to the vehicle-treated control group. A 3.0 mg/kg dose of sesamin inhibited microglia activation and consequently, cyclooxygenase-2, inducible nitric oxide, and interleukine-$1{\beta}$ expressions at 48 h after reperfusion. Conclusions : Sesamin protects neuronal cell death through inhibition of microglial activation or the production of neurotoxic metabolites and proinflammatory mediators by microglia such as COX-2, iNOS and IL-$1{\beta}$ in global cerebral ischemia.