• 폴리머
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• 제36권6호
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• pp.699-704
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• 2012

경구투여를 통한 친수성 약물의 방출조절을 위하여 이중층으로 된 고분자 담체를 설계하였다. 생체고분자인 alginate와 chitosan은 각각 극성 흡수성분으로, poly(D,L-lactide)는 소수성 피막으로, 그리고 theophylline과 diclofenac sodium은 모델 약물로 사용하였다. 담체는 지연방출과 이어지는 지속방출을 위하여 외부 껍질은 poly(D,L-lactide)로, 내부중심은 약물과 함께 알지네이트 또는 키토산으로 구성되어진 이중층의 미립구 담체로 성형하였다. 담체와 약물간의 극성 조합으로 인한 담체의 모폴로지와 약물방출 거동을 조사하였다. 담체와 약물 그리고 pH 환경의 상대적 극성이 약물방출 특성에 상당한 영향이 있음을 확인하였다.

• Journal of Microbiology and Biotechnology
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• 제22권2호
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• pp.274-282
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• 2012

The object of this study was to assess the efficacy of Polycan from Aureobasidium pullulans SM-2001, which is composed mostly of beta-1,3-1,6-glucan, on osteoarthritis (OA)-induced by anterior cruciate ligament transection and partial medial meniscectomy (ACLT&PMM). Three different dosages of Polycan (85, 42.5, and 21.25 mg/kg) were orally administered once a day for 84 days to male rats a week after ACLT&PMM surgery. Changes in the circumference and maximum extension angle of each knee, and in cartilage histopathology were assessed using Mankin scores 12 weeks after Polycan administration. In addition, cartilage proliferation was evaluated using bromodeoxyuridine (BrdU). As the result of ACLT&PMM, classic OA was induced with increases in maximum extension angles, edematous knees changes, and capsule thickness, as well as decreases in chondrocyte proliferation, cartilages degenerative changes, and loss of articular cartilage. However, these changes (except for capsule thickness) were markedly inhibited in all Polycan- and diclofenac sodium-treated groups compared with OA control. Although diclofenac sodium did not influence BrdU uptake, BrdU-immunoreactive cells were increased with all dosages of Polycan, which means that Polycan treatment induced proliferation of chondrocytes in the surface articular cartilage of the tibia and femur. The results obtained in this study suggest that 84 days of continuous oral treatment of three different dosages of Polycan led to lesser degrees of articular stiffness and histological cartilage damage compared with OA controls 91 days after OA inducement, suggesting that the optimal Polycan dosage to treat OA is 42.5 mg/kg based on the present study.

• The Korean Journal of Pain
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• 제34권3호
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• pp.262-270
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• 2021

Background: Transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel implicated in pain sensation in response to heat, protons, and capsaicin (CAPS). It is well established that TRPV1 is involved in mechanical allodynia. This study investigates the effect of Ononis spinosa (Fabaceae) in CAPS-induced mechanical allodynia and its mechanism of action. Methods: Mechanical allodynia was induced by the intraplantar (ipl) injection of 40 ㎍ CAPS into the left hind paw of male Wistar rats. Animals received an ipl injection of 100 ㎍ O. spinosa methanolic leaf extract or 2.5% diclofenac sodium 20 minutes before CAPS injection. Paw withdrawal threshold (PWT) was measured using von Frey filament 30, 90, and 150 minutes after CAPS injection. A molecular docking tool, AutoDock 4.2, was used to study the binding energies and intermolecular interactions between O. spinosa constituents and TRPV1 receptor. Results: The ipsilateral ipl injection of O. spinosa before CAPS injection increased PWT in rats at all time points. O. spinosa decreased mechanical allodynia by 5.35-fold compared to a 3.59-fold decrease produced by diclofenac sodium. The ipsilateral pretreatment with TRPV1 antagonist (300 ㎍ 4-[3-Chloro-2-pyridinyl]-N-[4-[1,1-dimethylethyl] phenyl]-1-piperazinecarboxamide [BCTC]) as well as the β2-adrenoreceptor antagonist (150 ㎍ butoxamine) attenuated the action of O. spinosa. Depending on molecular docking results, the activity of the extract could be attributed to the bindings of campesterol, stigmasterol, and ononin compounds to TRPV1. Conclusions: O. spinosa alleviated CAPS-induced mechanical allodynia through 2 mechanisms: the direct modulation of TRPV1 and the involvement of β2 adrenoreceptor signaling.

• 공업화학
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• 제5권3호
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• pp.413-418
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• 1994

(2-(2, 6-디클로로페닐)아미노)페닐 아세트산나트륨의 합성단계를 줄이고 각 단계별 합성수율을 향상시켰다. 합성은 4단계로 하였으며 출발물질은 2,6-디클로로아닐린과 모노브로모벤젠을 사용하였다. 첫단계인 Ullmann반응은 구리촉매를 3회 분할 첨가하여 80%의 수율로 진행시켰고, 아실화와 프리델-크라프트 반응도 효율적으로 단순화하였다. 최종 반응생성물인 디클로페낙은 클라이젠 용액을 사용하여 제3단계에서 얻은 1-(2, 6-디클로로페닐)-2-인돌리논을 가수분해함으로써 97%의 수율로 얻었다.

• Journal of Pharmaceutical Investigation
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• 제37권3호
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• pp.187-192
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• 2007

A reversed phase HPLC analysis of atorvastatin (AS) standard solution was performed using diclofenac (DF) as internal standard. Column oven temperature, flow rate and the composition of the mobile phase were varied in order to determine a practical system setup using a C18 column and UV detector. Two C18 columns of different length were compared regarding their influence on the AS peak shape. Based on these preliminary experiments a validation study was performed utilizing a C18 column at $62^{\circ}C$ with a mobile phase consisting of sodium phosphate buffer (0.05 M, pH 4.0), methanol and acetonitrile (40:50:10, v/v/v). The detection limit for AS was $0.1{\mu}g/ml$ and inter- and intra-day calibration curves were linear over a concentration range of $0.2-50{\mu}g/ml$. Accuracy and precision were satisfactory in the AS concentration range of $0.5-50{\mu}g/ml$.

• 대한화학회지
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• 제47권3호
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• pp.237-240
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• 2003

소염작용을 가진 일련의 싸이아졸리딘아세트산 유도체들을 싸이오유레아와 말레산무수물로부터 합성하고 분광학적인 방법으로 구조를 확립하였다. 또한 이 화합물들의 소염작용을 표준시약인 디클로펜악 소듐과 비교한 결과 어느정도의 효과를 가지고 있음을 검정하였다.

• Bulletin of the Korean Chemical Society
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• 제32권7호
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• pp.2274-2278
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• 2011

Verapamil is a calcium channel blocker and is classified as a class IV anti-arrhythmic agent. It is used in the control of supra ventricular tachyarrhythmias, and in the management of classical and variant angina pectoris. It is also used in the treatment of hypertension and used as an important therapeutic agent for angina pectoris, ischemic heart disease, hypertension and hypertrophic cardiomyopathy. Verapamil commonly co-administered with NSAIDs (non-steroidal anti-inflammatory drugs) i.e. diclofenac sodium, flurbiprofen, Ibuprofen, mefanamic acid and meloxicam. A simple and rapid RP-HPLC method for simultaneous determination and quantification of verapamil and NSAIDs was developed and validated. The mobile phase constituted of acetonitrile: water (55:45) whose pH was adjusted at 2.7 and pumped at a flow rate of 2.0 mL $min^{-1}$ at 230 nm. The proposed method is simple, precise, accurate, low cost and least time consuming for the simultaneous determination of verapamil and NSAIDs which can be effectively applied for the analysis of human serum.

• Advances in Traditional Medicine
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• 제7권3호
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• pp.274-279
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• 2007

The crude ethanol extract of leaves of Sonneratia caseolaris Linn. (Sonneratiaceae) was screened for its antinociceptive and antidiarrhoeal activities. The extract produced significant writhing inhibition in acetic acid induced writhing in mice at dose of 250 and 500 mg/kg body weight (P<0.01) comparable to the standard drug diclofenac sodium at the dose of 25 mg/kg of body weight. When tested for its antidiarrhoeal effects on castor oil induced diarrhea in mice, it increased mean latent period and decreased the frequency of defecation significantly at the dose of 500 mg/kg body weight (P < 0.05) comparable to the standard drug loperamide at the dose of 50 mg/kg of body weight. The overall results tend to suggest the antinociceptive and antidiarrhoeal activities of the extract.

• Advances in Traditional Medicine
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• 제7권3호
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• pp.280-285
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• 2007

The methanol extract of leaves of Bruguiera gymnorrhiza (L.) Lam. (Rhizophoraceae) was screened for its antinociceptive and antidiarrhoeal activities. The extract produced significant inhibition in acetic acid-induced writhing in mice at dose of 250 and 500 mg/kg body weight (P < 0.001), comparable to the standard drug diclofenac sodium at the dose of 25 mg/kg of body weight (P < 0.001). When tested for its antidiarrhoeal effects on castor oil-induced diarrhea in mice, it increased mean latent period (P < 0.02) and decreased the frequency of defecation (P < 0.01) significantly at the dose of 500 mg/kg body weight, comparable to the standard drug loperamide at the dose of 50 mg/kg of body weight. The overall results tend to suggest the antinociceptive and antidiarrhoeal activities of the extract.

• Advances in Traditional Medicine
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• 제3권3호
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• pp.123-128
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• 2003

Stephania hernandifolia belonging to the family Menispermaceae is the biggest storehouse of diphenylbisbenzylisoquinoline (DBBI) alkaloids. Exhaustive chemical processing of the bulb of S. hernandifolia by the application of modern separation techniques yielded a DBBI alkaloid which was identified as cycleanine using spectroscopic methods (UV, IR, $^1HNMR$. $^{13}CNMR$, Mass). Cycleanine showed significant anti-inflammatory activity against carrageenin induced paw oedema, comparable to that produced by diclofenac sodium, used as standard drug. It exhibited potent analgesic effects against chemical and thermal noxious stimuli. It was also found to possess anticonvulsive activity in the strychnine induced convulsion model.