• 한국독성학회:학술대회논문집
• /
• 한국독성학회 2001년도 International Symposium on Dietary and Medicinal Antimutgens and Anticarcinogens
• /
• pp.161-161
• /
• 2001

Resveratrol (trans-3, 4', 5-trihydroxystilbene), which is a polyphenolic compound found in a variety of plants such as grapes and wine, has been reported to have a variety of anti-inflammatory, anti-platelet, and anti-carcinogenic effects. Recently resveratrol was reported to serve as an estrogen agonist in MCF-7 cells Based on its structural similarity to diethylstilbestrol, a synthetic estrogen, we examined whether resveratrol and its derivatives might be estrogenic using stable MCF-7-ERE cells. (omitted)

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
• /
• pp.102.2-103
• /
• 2003

It has been previously reported that luteolin and luteolin-7-glucoside displayed the potent anti-oxidant and anti-inflammatory effects, which have also been successful in reducing vascular smooth muscle cells(VSMCs) proliferation. In this study, a possible anti-proliferative effect and its mechanism on rat aortic VSMCs by luteolin and luteolin-7-glucoside were investigated. Luteolin significantly inhibited the platelet-derived growth factor(PDGF)-BB-induced proliferation of rat aortic VSMCs. While luteolin-7-glucoside weakly inhibited the proliferation. (omitted)

• The Korean Journal of Physiology and Pharmacology
• /
• 제19권5호
• /
• pp.421-426
• /
• 2015

The increased potential for vascular smooth muscle cell (VSMC) growth is a key abnormality in the development of atherosclerosis and post-angioplasty restenosis. Abnormally high activity of platelet-derived growth factor (PDGF) is believed to play a central role in the etiology of these pathophysiological situations. Here, we investigated the anti-proliferative effects and possible mechanism(s) of murrayafoline A, a carbazole alkaloid isolated from Glycosmis stenocarpa Guillamin (Rutaceae), on PDGF-BB-stimulated VSMCs. Murrayafoline A inhibited the PDGF-BB-stimulated proliferation of VSMCs in a concentration-dependent manner, as measured using a non-radioactive colorimetric WST-1 assay and direct cell counting. Furthermore, murrayafoline A suppressed the PDGF-BB-stimulated progression through $G_0/G_1$ to S phase of the cell cycle, as measured by [$^3H$]-thymidine incorporation assay and cell cycle progression analysis. This anti-proliferative action of murrayafoline A, arresting cell cycle progression at $G_0/G_1$ phase in PDGF-BB-stimulated VSMCs, was mediated via down-regulation of the expression of cyclin D1, cyclin E, cyclin-dependent kinase (CDK)2, CDK4, and proliferating cell nuclear antigen (PCNA), and the phosphorylation of retinoblastoma protein (pRb). These results indicate that murrayafoline A may be useful in preventing the progression of vascular complications such as restenosis after percutaneous transluminal coronary angioplasty and atherosclerosis.

• 한국임상수의학회지
• /
• 제36권4호
• /
• pp.200-206
• /
• 2019

This study was performed to assess the anti-inflammatory and cartilage regenerative effects of platelet-rich plasma (PRP) on canine chondrocytes. Proliferation and migration assays under both normal and lipopolysaccharide (LPS)-induced inflammatory conditions were performed with various concentrations of PRP (1% to 10%). The expression levels of genes related to osteoarthritis were evaluated in the following groups: PRP group, LPS group and LPS + PRP group. mRNA expression levels were detected using real-time polymerase chain reaction (RT-PCR). Proliferation assays showed significantly enhanced proliferation in all PRP-treated groups compared with the no serum group. Compared with 10% fetal bovine serum (FBS), PRP concentrations above 3% in the normal condition and 1% to 7% PRP in the LPS-induced inflammatory condition were found to significantly promote chondrocyte proliferation. In the normal condition, all PRP-treated groups showed significantly increased cell migration compared with the no serum group. Chondrocyte migration was decreased with LPS-induced inflammation, but PRP treatment resulted in significantly enhanced migration compared with the other groups in this condition. According to RT-PCR, the LPS + PRP group showed significantly higher levels of COL1A1, IL-6, aggrecan and lower levels of $TNF-{\alpha}$, MMP-1, MMP-3 mRNA expression compared to the LPS group. The results of this study suggest that PRP application can enhance the proliferation and migration of canine chondrocytes and improve canine articular cartilage regeneration.

• Journal of Acupuncture Research
• /
• 제23권6호
• /
• pp.61-76
• /
• 2006

To study the effects of anti-cancer, anti-metastasis and immune response improvement effects of herbal-accupunture with Orostachys japhonicus A.Berger, infusion solution put into Kansu(BL18) of mouse induced by Colon26-L5 human colon cancer cells, which are corresponding to humanbody. We observed the change of body weight, surviving number, median surviving time, increase of life span, changes in amount of leukocyte, erythrocyte, platelet, total protein, creatinine, glucose and LDH, weight of spleen and kidney, histological analysis on tissue metastasis of liver, splenic cell proliferation, the expression of cytokine gene, the number of CD4+, CD8+, CD9+ and NK cell, and concluded like this. The results were obtained as follows ; 1. In acute and sub-acute cytotoxicity experiment, significantly signs were not appeared in all groups. 2. Antimetastatic experiment in vitro and in vivo showed that Orostachys Japhonicus A.Berger Herbal-acupuncture at Kansu(BL18) has antimetastatic effects. 3. The spleen cells proliferation of the experimental groups treated with Orostachys Japhonicus A.Berger infusion solution extract has increased significantly compared with that of the control group. 4. As compared with control, the population of total T cell, helper T cell, cytotoxic T cell and macrophage were increased. 5. The production of Th 1 type cytokines from splenocyte and cytokines which is associated with anti-tumor activity form macrophage were increased significantly. Above the results revealed that herbal-accupunture with Orostachys Japhonicus A.Berger infusion solution has effects of anti-cancer, anti-metastasis and immune response improvement.

• 동의생리병리학회지
• /
• 제18권5호
• /
• pp.1494-1504
• /
• 2004

The present paper reports the effects of Hwaotang an atherosclerosis using a spontaneous experimental model, We have also investigated the pharmacological effect of Hwaotang on collagen- and ADP-induced blood platelet aggregation, thrombin-induced conversion of fibrinogen and fibrinolysis in in vitro experiments, and various effects on stimuli-induced superoxide generation in human neutrophils. Hwao-tang was shown to have inhibitory effect on collagen- and ADP-induced blood platelet aggregation, on thrombin-induced conversion of fibrinogen to fibrin and on the activity of plasminogen or plasmin. Hwao-tang also significantly inhibited fMLP-induced superoxide generation in a concentration-dependent manner, but not that induced by arachidonic acid. Hwao-tang inhibited neutrophil functions, including degranulation, superoxide generation, and leukotriene B4 production, without any effect on 5-lipoxygenase activity. In conclusion, the protection of extracts of Hwao-tang on the ischemic infarction induced artificially might be involved to their inhibition of thrombotic action. The results also indicate that Hwao-tang exerts the effects on superoxide generation related to the inhibition of neutrophil functions.

• Journal of Yeungnam Medical Science
• /
• 제17권1호
• /
• pp.1-11
• /
• 2000

Inhibition of cyclooxygenase(COX), and thus prevention of the formation of prostaglandins, provided a unifying explanation of the therapeutic and toxic actions of nonsteroidal anti-inflammatory drugs (NSAIDs). Recently, the discovery of the two isoforms of COX was made by molecular biologists studying neoplastic transformation in chick embryo cells. The constitutive enzyme, COX-1, is obviously responsible for the production of prostaglandins involved in housekeeping functions such as maintenance of integrity of the gastric mucosa, renal blood flow and platelet aggregation. The inducible form of COX (COX-2) is responsible for the formation of prostaglandins that pathologically affects inflammation, pain and fever. Clearly, all the experimental and clinical data support the hypothesis that the beneficial effects of NSAIDs are due to inhibition of the COX-2 enzyme, whereas the gastrotoxicity is due to inhibition of COX-1. The cox-2/COX-1 ratios of the NSAIDs in common use have been measured and compared with epidemiological data on their side effects. There is little evidence to suggest that one NSAID is clearly more effective than another, But substantial individual variability is present with respect to the pharmacology and pharmacokinetics of these drugs: therefore it is essential to adjust the dosage and choose specific drug to the patient's response.

• 생명과학회지
• /
• 제21권10호
• /
• pp.1355-1363
• /
• 2011

많은 임상 실험을 통해 마늘(Allium sativum)이 심혈관 질환에 유효한 효과가 알려져 있다. 흑마늘(AGE)은 항산화, 항염증, 항암 효과 등 다양한 생물학적 효과가 보고되었다. 그러나, 흑마늘의 심혈관계 질환과의 상관관계에 대한 연구는 아직 미흡한 실정이다. 흑마늘과 그 유래 성분이 혈소판에 미치는 영향을 조사하였다. 백서의 혈액을 얻어, 흑마늘과 그 유래 성분의 thrombin에 의해 유도되는 혈소판 응집에 대한 억제 효과를 조사한 결과, 흑마늘과 diallyl sulphides는 농도의존적으로 혈소판 응집을 억제함을 관찰하였다. 또한 in vivo 실험에서도 마늘 오일과 S-Allylmercapto-cystein (SAMC)는 thrombin과 ADP에 의해 유도되는 혈소판 응집을 유의성 있게 억제하는 것을 관찰하였다. 흑마늘 유래 SAMC와 diallyl sulphides가 혈소판 응집 억제 효과를 나타내는 것을 확인할 수 있었다. 이러한 결과는 흑마늘이 심혈관계 질환의 예방을 위한 건강보조식품으로의 새로운 가능성을 제시한다.

• Journal of Acupuncture Research
• /
• 제23권2호
• /
• pp.139-157
• /
• 2006

In the present study, I have investigated the bee venom (BV) and melittin (a major component of BV) -mediated anti-proliferative effects, and defined its mechanisms of action in cultured rat aortic vascular smooth muscle cells (VSMCs). BV and melittin $(0.4{\sim}0.8\;{\mu}g/ml)$ effectively inhibited 50 ng/ml platelet derived growth factor BB (PDGF-BB)-induced VSMCs proliferations. The regulation of apoptosis has attracted much attention as a possible means of eliminating excessively proliferating VSMCs. In the present study, the treatment of BV and melittin strongly induced apoptosis of VSMCs. I examined the effects on $NF-{\kappa}B$ activation to investigate a possible mechanism for anti-proliferative effects of BV and melittin, the PDGF-BB-induced $I{\kappa}B{\alpha}$ phosphorylation and its degradation were potently inhibited by melittin, and DNA binding activity and nuclear translocation of $NF-{\kappa}B$ p50 subunit in response to the action of PDGF-BB were potently attenuated by melittin. In further investigations, melittin markedly inhibited the PDGF-BB-induced phosphorylation of Akt but not ERK1/2, upstream signals of $NF-{\kappa}B$. Treatment of melittin also potently induced pro-apoptotic protein p53, Bax, and caspase-3 expression, but decreased anti-apoptotic protein Bcl-2 expression. These results suggest that the anti-proliferative effects of BV and melittin in VSMCs through induction of apoptosis via suppressions of $NF-{\kappa}B$ and Akt activation, and enhancement of apoptotic signal pathway. Based on these results, BV acupuncture can be a candidate as a therapeutic method for restenosis and atherosclerosis.

• Archives of Pharmacal Research
• /
• 제29권5호
• /
• pp.375-383
• /
• 2006

The anti platelet effects of a novel guanidine derivative, KR-32570 ([5-(2-methoxy-5-chlorophenyl) furan-2-ylcarbonyl]guanidine), were investigated with an emphasis on the mechanisms underlying its inhibition of collagen-induced platelet aggregation. KR-32570 significantly inhibited the aggregation of washed rabbit platelets induced by collagen $(10{\mu}g/mL)$, thrombin (0.05 U/mL), arachidonic acid $(100{\mu}M)$, a thromboxane (TX) $A_2$ mimetic agent U46619 (9,11-dideoxy-9,11-methanoepoxy-prostaglandin $F_2,\;1{\mu}M$) and a $Ca^{2+}$ ATPase inhibitor thapsigargin $(0.5{\mu}M)$ ($IC_{50}$ values: $13.8{\pm}1.8,\;26.3{\pm}1.2,\;8.5{\pm}0.9,\;4.3{\pm}1.7\;and\;49.8{\pm}1.4{\mu}M$, respectively). KR-32570 inhibited the collagen-induced liberation of $[^3H]$arachidonic acid from the platelets in a concentration dependent manner with complete inhibition being observed at $50{\mu}M$. The $TXA_2$ synthase assay showed that KR-32570 also inhibited the conversion of the substrate $PGH_2$ to $TXB_2$ at all concentrations. Furthermore, KR-32570 significantly inhibited the $[Ca^{2+}]_i$ mobilization induced by collagen at $50{\mu}M$, which is the concentration that completely inhibits platelet aggregation. KR-32570 also decreased the level of collagen $(10{\mu}g/mL)$induced secretion of serotonin from the dense-granule contents of platelets, and inhibited the NHE-1-mediated rabbit platelet swelling induced by intracellular acidification. These results suggest that the antiplatelet activity of KR-32570 against collagen-induced platelet aggregation is mediated mainly by inhibiting the release of arachidonic acid, $TXA_2$ synthase, the mobilization of cytosolic $Ca^{2+}$ and NHE-1.