• 약학회지
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• 제42권4호
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• pp.414-421
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• 1998

In order to compare the suppressive effect of quercetin and its glycosides, such as quercitrin (quercetin-3-rhamnoside), isoquercitrin (quercetin-3-glucoside), hyperin (querceti n-3-galactoside)and rutin (quercetin-3-rhamnosyl glucoside), on the genotocicity by benzo(a)pyrene(B(a)P), in vitro sister chromatid exchange(SCE) test using mouse spleen lymphocytes and in vivo micronucleus test using mouse peripheral blood were performed. B(a)P-induced SCEs in vitro were slightly decreased by the simultaneous treatment of quercetin and its glycosides, although there was no significant decrease. On the other hand, MNU induced micronucleated reticulocytes(MNRL7s) in vivo were significantly decreased with a dose-dependent manner in all compounds tested. However, there were no differences between quercetin aglycone and glycosides in the suppressive effects under experimental condition of this study. To elucidate, the action mechanism of quercetin aglycone and its glycosides against B(a)P-induced genotoxicity, the assay of DNA binding with B(a)P was studied. Quercetin aglycone and its glycosides inhibited B(a)P metabolism in the presence of S-9 mix and decreased the B(a)P/DNA binding in the calf thymus DNA with S-9 mix. These results suggest that antigenotoxicity of quercetin antiglycosides on B(a)P-induced genotoxicity is due to decrease of DNA binding with B(a)P through the inhibition of metabolism with B(a)P in the calf thymus DNA. Therefore, quercetin and its glycosides may act as an antigenotoxicity agent and may be useful as a chemopreventive agent of polycyclic aromaic hydrocarbons like B(a)P.

• Journal of Pharmaceutical Investigation
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• 제18권4호
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• pp.187-195
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• 1988

Poorly permeable $Eudragit^{\circledR}$ RS 100 polymer was used as a wall material for the microencapsulation of zipeprol dihydrochloride by a phase separation method from chloroform-cyclohexane system with 5% polyisobutylene in cyclohexane, and microcapsules obtained were evaluated in vitro by particle size analysis, scanning electron microscopy, drug release test and in vivo bioavailability test in rats. The mechanism of drug release from microcapsules appeared to fit Higuchi matrix model kinetics. The area under the first moment of plasma concentration-time curve of the microcapsules obtained was considerably increased (p<0.05) as compared with that from zipeprol dihydrochloride oral solution. Therefore, it may be suggested that $Eudragit^{\cirledR}$ RS 100 coated zipeprol dihydrochloride microcapsules can be used as a sustained release medication.

• Asian Pacific Journal of Cancer Prevention
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• 제14권9호
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• pp.5243-5248
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• 2013

Background: Triptolide, extracted from the herb Tripteryglum wilfordii Hook.f that has long been used as a natural medicine in China, has attracted much interest for its anti-cancer effects against some kinds of tumours in recent years. Artesunate, extracted from the Chinese herb Artemisia annua, has proven to be effective and safe as an anti-malarial drug that possesses anticancer potential. The present study attempted to clarify if triptolide enhances artesunate-induced cytotoxicity in pancreatic cancer cell lines in vitro and in vivo. Methods: In vitro, to test synergic actions, cell viability and apoptosis were analyzed after treatment of pancreatic cancer cell lines with the two agents singly or in combination. The molecular mechanisms of apoptotic effects were also explored using qRT-PCR and Western blotting. In vivo, a tumor xenograft model was established in nude mice, for assessment of inhibitory effects of triptolide and artesunate. Results: We could show that the combination of triptolide and artesunate could inhibit pancreatic cancer cell line growth, and induce apoptosis, accompanied by expression of HSP 20 and HSP 27, indicating important roles in the synergic effects. Moreover, tumor growth was decreased with triptolide and artesunate synergy. Conclusion: Our result indicated that triptolide and artesunate in combination at low concentrations can exert synergistic anti-tumor effects in pancreatic cancer cells with potential clinical applications.

• Bulletin of the Korean Chemical Society
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• 제34권6호
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• pp.1857-1863
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• 2013

Most of biomaterials come in direct contact with the body, making standardized methods of evaluation and validation of biocompatibility an important aspect to biomaterial development. However, biomaterial validation guidelines have not been fully established, until now. This study was to compare the in vitro behavior of osteoblasts cultured on nanomaterial $TiO_2$ surfaces to osteoblast behavior on culture plates. Comparisons were also made to cells grown in conditioned media (CM) that creates an environment similar to the in vivo environment. Comparisons were made between the different growth conditions for osteoblast adhesion, proliferation, differentiation, and functionality. We found that the in vivo-like system of growing cells in concentrated CM provided a good validation method for biomaterial development and in vivo implant therapy. The $TiO_2$ materials were biocompatible, showing similar behavior to that observed in vivo. This study provided valuable information that would aid in the creation of guidelines into standardization and evaluation of biocompatibility in $TiO_2$ biomaterials.

• 동의생리병리학회지
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• 제24권1호
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• pp.143-151
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• 2010

In Vivo and In vitro antispasmodic effects of Jun-Si-Baek-Chul-San, a Traditional Korean Polyherbal Medicineconsisted of 7 types of herbs were observed in the present study. To clarify the effects of Jun-Si-Baek-Chul-San, on accelerating small intestinal movement induced by the stimulation of cholinergic neurotransmission, we evaluated the effects of Jun-Si-Baek-Chul-San on In vivo carbachol (an acetylcholinergic agent)-accelerated mice small intestinal transit and on In vitro contractions induced by low-frequency electrostimulation, KCl, histamine or acetylcholine using isolated guinea pig ileum. To induce the acceleration of mice small intestinal transit, Carbachol 1 mg/kg was once subcutaneously dosed 15min before last administration of the test drugs. In the present study, Jun-Si-Baek-Chul-San 500, 250 and 125 mg/kg or domperidone 20 mg/kg were orally pretreated on the carbachol-accelerated mice small intestinal transit once a day for 7 days and the small intestinal transit rateof activated charcoal powder were monitored. In vitro assays, Jun-Si-Baek-Chul-San1, 0.1, 0.01 and 0.001 mg/ml or domperidone $2{\times}10^{-5}M$ were treated 10min before ileal contraction was induced by filed stimulation, acetylcholine, KCl and histamine, and the % changes of contractions were observed compared to the treatment of inducer alone. In spontaneous contraction, the % changes of contractions were observed compared to treatment of vehicle alone at 10min after Jun-Si-Baek-Chul-San or domperidone treatment. The efficacy of Jun-Si-Baek-Chul-San was compared to those of domperidone. High concentration, 1 mg/ml of Jun-Si-Baek-Chul-San was found to decrease the spontaneous contraction of the isolated guinea-pig ileum. In addition, Jun-Si-Baek-Chul-San decrease contractions induced by electrostimulation, acetylcholine, histamine and KCl in the isolated guinea-pig ileum. In addition, Jun-Si-Baek-Chul-San effectively inhibited the accelerated small intestinal movement induced by carbachol stimulation of cholinergic neurotransmission in In vivo. Based on the results, although the exact molecular or action mechanism and which herbs or compound in Jun-Si-Baek-Chul-San are responsible for actions, it was concluded that Jun-Si-Baek-Chul-San normalization in the accelerated intestinal motility might be interfere with a variety of muscarinic, adrenergic and histaminic receptor activities or with the mobilization of calcium ions required for smooth muscle contraction non-specificly. Therefore, it is expected that Jun-Si-Baek-Chul-San will be promising as a prescription of clinical treatment of digestive tract disorders such as accelerated the motility of intestine, diarrhea or intestinal painful contractions.

• Toxicological Research
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• 제33권3호
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• pp.191-203
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• 2017

Human eyes and skin are frequently exposed to chemicals accidentally or on purpose due to their external location. Therefore, chemicals are required to undergo the evaluation of the ocular and dermal irritancy for their safe handling and use before release into the market. Draize rabbit eye and skin irritation test developed in 1944, has been a gold standard test which was enlisted as OECD TG 404 and OECD TG 405 but it has been criticized with respect to animal welfare due to invasive and cruel procedure. To replace it, diverse alternatives have been developed: (i) For Draize eye irritation test, organotypic assay, in vitro cytotoxicity-based method, in chemico tests, in silico prediction model, and 3D reconstructed human cornealike epithelium (RhCE); (ii) For Draize skin irritation test, in vitro cytotoxicity-based cell model, and 3D reconstructed human epidermis models (RhE). Of these, RhCE and RhE models are getting spotlight as a promising alternative with a wide applicability domain covering cosmetics and personal care products. In this review, we overviewed the current alternatives to Draize test with a focus on 3D human epithelium models to provide an insight into advancing and widening their utility.

• 한국잠사곤충학회지
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• 제46권1호
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• pp.23-27
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• 2004

견 피브로인 가수분해물의 몇 가지 특성과 in vitro 및 in vivo에 의한 동물 인지 기능 향상효과를 알아본 결과, 다음과 같은 결과를 얻을 수 있었다. 1) 효소 가수분해 실크 피브로인 펩타이드의 분획에 있어 3가지의 분자량이 다른 분획을 제조할 수 있었다. 2) 분획 별 실크 피브로인 펩타이드의 유리 아미노산 조성은 분획간의 유의차가 나타났으며, 분획 2 및 3의 경우 활성부분을 가진 Cys, Tyr 및 Phe부분이 상당한 양을 차지하였다. 3) 대표적으로 산 및 효소 가수분해물의 핵자기공명(NMR) 법에 의한 구조적 차이는 산으로 가수분해한 저분자와 그렇치 않은 샘풀 간에는 확실한 구조적 차이에 기인한 상이한 스펙트럼을 관측할 수 있었다. 4) 분자량 별 실크 피브로인의 인지기능 향상 효과를 세포배양(in vitro)및 동물투여(in vivo)에 의해 알아본 결과, 세포배양에 의한 활성 효과는 분자량에 따라 다소 차이가 나타났으며, 그 중 분자량 500미만의 샘플군(LF)이 대조인 유발군에 비해 23.5%의 세포보호 효과가 있었다. 또한 동물(in vivo)에 의한 인지기능 향상 효과에 있어서는 보다 확실한 차이가 나타났는데, 그 중 분자량 500-1000정도의 분자량 범위의 분획물질을 10 mg/kg을 투여하였을 경우, 대조군(scopolamine)에 비하여 최고 50%까지 기억회복 효과를 나타내었다.

• 대한화장품학회지
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• 제33권4호
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• pp.219-225
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• 2007

비스에칠헥실옥시페놀메톡시페닐트리아진(Bis-ethylhexyloxyphenolmeth oxyphenyltrizine; BEMT)은 식품의약품안전청 고시 기능성 원료로 자외선 차단 제품에 널리 사용되는 UVA와 UVB의 화학적 자외선 흡수제이다. 그러나 BEMT는 실제 적용에 있어 여러 가지 결점이 있어 사용이 제한되고 있다. 본 연구의 목적은 BEMT가 적용된 고형지질나노입자(BEMT- SLN)의 자외선차단제품 응용에 있다. 제조된 고형지질나노입자의 입도는 약 330 nm, 봉입율은 93.3 %, 결정화지표는 4.3 %였다. In vitro 방출 및 투과 실험 결과에서, BEMT는 SLN보다 O/W 에멀젼이 대체로 높았다. In vivo 실험에서 SLN의 BEMT 방출비는 80 % 감소하였다. 또한 in vitro UV 방어 효과 실험에서 SLN이 적용된 처방의 자외선방어지수(SPF) 값은 약 2.5배 증가하였다. 결국 SLN은 BEMT를 효과적으로 봉입하고 있었으며, 자외선 차단 상승 효과를 나타낸다.

• 생약학회지
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• 제43권3호
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• pp.239-242
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• 2012

This study was carried out to investigate the anti-malarial activity of Juniperus chinensis by in vitro and in vivo system using Plasmodium falciparum chloroquine-sensitive(3D7) and P. falciparum chloroquine-resistant(S20) strains. According to cytotoxicty test on NIH 3T3 cell, the ethanol extract(EtOH), ethylacetate(EtOAc) fraction and aqueous fraction possessed significant anti-malarial activity against both 3D7 and S20 strains at non-toxic concentrations(<100 /). In vitro assay, EtOAc fraction showed notable activity against 3D7 and S20 strains of P. falciparum with $IC_{50}$ values of $37{\pm}2{\mu}g/ml$ and $36{\pm}6{\mu}g/ml$. In animal test using P. falciparum infected human erythrocytes, the treatment of EtOAc fraction significantly inhibited parasitaemia in mice in a dose-dependent manner that is parasitaemia of 42%, 34% and 31% in doses of 10 mg/kg, 20 mg/kg and 40 mg/kg, respectively. The study provides data to support the medicinal importance of the J. chinensis.

• 한국미생물·생명공학회지
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• 제19권3호
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• pp.235-241
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• 1991

Streptomyces melanosporofaciens로 동정된 strain 88-GT-161 균주는, 그람양성세균 및 식물병원성 곰팡이에 각각 항균활성을 나타내는 phthalate 유도체 및 염기성 마크로라이드의 새로운 항생물질을 생산하는 것으로 밝혀졌다. 이들 활성물질들의 분리. 정제과정에서 in vitro 및 in vivo(포트 시험) 항균활성을 조사하였으며, phtahalate 유도체 항생물질은 IR, NMR, 질량분석 스펙트럼 조사를 통하여 bis(2-ethylexyl) phthalate(dioctyl phthalate)로 동정하였다. Dioctyl phthalate가 Streptomyces sp.에 의하여 생산되며 생합성된 이 화합물이 항균활성을 가진다는 사실이 보고된 것은 이것이 처음이다.