• Journal of Gastric Cancer
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• 제9권3호
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• pp.78-87
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• 2009

위암 발생률이 높은 우리나라에서는 위암이 발생할 가능성이 높은 고위험군에서 위암 발생 여부를 알 수 있는 생물학적 인자(biological marker)의 개발이 매우 중요한데 가장 많이 연구되는 인자로 혈청 펩시노겐(Pepsinogen)이 있다. 이에 소화기질환을 가지고 있는 환자군과 건강검진센터 수진자를 대상으로 한두 가지 연구에서 혈청 펩시노겐 검사에 영향을 주는 인자를 알아보고 위축성 위염이나 위암 진단에 있어 혈청 펩시노겐 검사의 역할을 알아보았다. 혈청 펩시노겐 검사에 영향을 주는 인자로는 H. pylori 감염이 가장 컸고, 다음으로 성별, 연령이 있었다. 이를 고려한 결과 한국인에서의 내시경적 위축성 위염 진단에 있어서 PG I/II ratio 기준은 H. pylori 감염 여부에 따라 달랐는데 H. pylori 감염이 없는 경우는 PG I/II ratio 6이, H. pylori 감염이 있는 경우는 국제적 기준인 PG I/II ratio 3이 예민도와 민감도에서 우수했다. 또한 한국인에서의 위암이나 위축성 위염 진단에 있어 PG I이나 PG II는 별로 유용하지 않은 반면 PG I/II ratio는 비교적 유용함을 알 수 있었고, 특히 H. pylori 감염이 있는 경우 PG I/II ratio $\leq3$ 이하가 위암 발생위험도 예측에 도움이 되었다. 결과적으로 혈청 펩시노겐을 위암이나 위축성 위염 진단 biomarker로 사용할 때는 기존의 국제적인 기준도 중요하지만 각 나라의 현실에 맞는 기준치 적용을 위해 validation study를 시행하고 사용하는 것이 바람직한 것으로 보인다.

• 방사선산업학회지
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• 제7권2_3호
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• pp.127-134
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• 2013

Bombesin receptors are overexpressed in many kinds of human tumors. In particular, the gastrin releasing peptide receptor (GRPR) which is also called bombesin receptor subtype 2, has been identified in prostate cancer. In the present study, we developed a bombesin antagonist-based $^{177}Lu$-labeled peptide, $^{177}Lu$-DOTA-$Ala(SO_3H)$-Aminooctanoyl-Gln-Trp-Ala-Val-N methyl Gly-His-Statine-Leu-$NH_2$ (DOTA-sBBNA). DOTA-sBBNA was prepared using a solid phase synthesis method. It was labeled with $^{177}Lu$ by a high radiolabeling yield (>98%), and its Log P value was -2.05. The radiolabeled peptide was highly stable in serum incubation at $37^{\circ}C$ for 48 hr. A competitive displacement of $^{125}I-[Tyr^4]$-Bombesin on the PC-3 human prostate carcinoma cells revealed that the $IC_{50}$ value of the peptide was 6.76 nM indicating a highly nanomolar binding affinity for GRPR. These results suggest that $^{177}Lu$-DOTA-sBBNA can be a potential candidate for targeting prostate cancer, and further studies to evaluate its biological characteristics are needed.

• 방사선산업학회지
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• 제7권2_3호
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• pp.191-200
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• 2013

In this study, a novel bombesin (BBN) analogues, DOTA-Ala($SO_3H$)-4 aminobenzoyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met-$NH_2$ (DOTA-sBBN) and DOTA-Lys(glucose)-4 aminobenzoyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met-$NH_2$ (DOTA-gluBBN), were synthesized and radiolabeled, and their binding affinities were evaluated. Peptides were prepared by a solid phase synthesis method and their purities were over 98%. DOTA is the chelating agent for $^{177}Lu$-labeling, and the DOTA-conjugated peptides were radiolabeled with $^{177}Lu$ by a high radiolabeling yield (>98%). The Log P values of DOTA-sBBN and DOTA-gluBBN were -2.20 and -2.79, respectively. 50.41% of $^{177}Lu$-DOTA-sBBN and 72.97% of $^{177}Lu$-DOTA-gluBBN were left undegraded by the serum incubation at $37^{\circ}C$ for 48 hr. A competitive displacement of $^{125}I-[Tyr^4]$-BBN on the PC-3 human prostate carcinoma cells revealed that 50% inhibitory concentration ($IC_{50}$) were 1.46 nM of DOTA-sBBN and 4.67 nM of DOTA-gluBBN indicating a highly nanomolar binding affinity for GRPR. Therefore, it is concluded that $^{177}Lu$-DOTA-sBBN and $^{177}Lu$-DOTA-gluBBN can be potential candidates as a targeting modality for the Gastrin-releasing peptide receptor (GRPR)-over-expressing tumors, and further studies to evaluate their biological and pharmacological characteristics are needed.

• Journal of Digestive Cancer Research
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• 제10권1호
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• pp.1-8
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• 2022

The incidence of gastric neuroendocrine tumors (NET) has been increased with the improvement of endoscopy accessibility. The World Health Organization classified NET of low (G1), intermediate (G2), high (G3) grade and neuroendocrine carcinoma with poor differentiation by mitotic count and Ki-67 labeling index. Gastric NET are divided into three subtypes based on the pathophysiology, and treatment is determined according to the subtype and prognostic factors of tumor. For diagnosis, endoscopy with biopsy, endoscopic ultrasonography, abdominal pelvis computed tomography, and serum gastrin level measure are required. In general, type 3, size > 2 cm, deep submucosal infiltration, high histological grade, lymphovascular invasion and metastasis are poor prognostic factors. Type 1 or 2 without these factors are treated by endoscopic resection, and other tumors needs surgery. Endoscopic resection of early type 3 or type 1 and 2 tumors with poor prognostic factors still remains a challenge.

• The Korean Journal of Physiology
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• 제28권1호
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• pp.91-97
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• 1994

In order to produce a specific bombesin antiserum far very sensitive radioimmunoassay, synthetic $[lys^3]-bombesin$ conjugated to bovine serum albumin was subcutaneously injected into guinea pigs. The conjugation was performed using either carbodiimide or gIutaraldehyde as a coupling agent. The antisera were characterized by analysis of Scatchard and Sips plots. The antiserum LBE 2G/2 raised by repeat injection of the immunogen conjugated with carbodiimide showed the titer of 1 : 188,000, very low cross-reactivity to bombesin-like peptides except bombesin, with high affinity constant $(1.64{\times}10^{11}\;M^{-1})$ and high heterogeneity index (0.91). The antiserum LBG 1G/2 produced by repeat injection of the immunogen conjugated with glutaraldehyde possessed the titer of 1 : 43,000, high cross-reactivity to some bombesin-like peptides, high affinity constant $(1.19{\times}10^{11}\;M^{-1})$ and high heterogeneity index (0.79). These results indicate that the antiserum LBE 2G/2 is specific only to bombesin and that the antiserum LBG IG/2 binds to some bombesin-like peptides such as alytesin, gastrin releasing peptide and neuromedin C. The antiserum LBE 2G/2 is sufficient for the very sensitive radioimmunoassay of bombesin.

• The Korean Journal of Physiology and Pharmacology
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• 제2권5호
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• pp.637-644
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• 1998

Previously, we have isolated authentic bombesin and another bombesin like peptide named bombesin like immunoreactivity (BLI)-K2 from the skin of Korean fire-bellied toad, Bombina orientalis. In the present study, we have newly purified three heterogeneous forms of BLI named BLI-K3, BLI-K4, and BLI-K5 from side fractions obtained in previous isolation of bombesin like peptide. The BLIs were separated into five peaks on a column of $C_{18}$ preparative HPLC. Among them, three minor peaks containing BLI-K3, K4, and K5 were purified by means of sequential chromatography on the columns of SP cation exchange HPLC and $C_{18}$ reverse phase HPLC. The purified BLI-K3 and K4 showed high binding affinity to an anti-bombesin serum (LBE 2G-2) with binding potency of 72 and 95%, respectively, relative to that of bombesin. However, they did not possess any distinctive biological activity of bombesin like peptide. On the contrary, the biological activity of BLI-K5 was similar to that of bombesin but its binding affinity to an anti-bombesin serum was low. The results indicate that three heterogeneous forms of BLI were coexpressed with bombesin and BLI-K2 in the skin of B. orientalis. All forms of the purified BLI in the present study were immunologically active but only BLI-K5 possessed the distinctive biological activity of bombesin like peptide.

• 운동영양학회지
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• 제23권4호
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• pp.6-13
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• 2019

[Purpose] In this study, we examined the in vitro antioxidant activities and laxative effects of taurine-xylose (T-X), a synthetic taurine-carbohydrate derivative, in a rat model of constipation induced by loperamide. [Methods] The animals were divided into four treatment groups: normal untreated rats (NOR group), loperamide-treated control rats (CON group), loperamide and taurine-xylose (15 mg/kg)-treated rats (T-X group), and loperamide and commercial Dulcolax S (5.5 mg/kg)-treated rats (DS group). [Results] In the present study, T-X exhibited potent reducing power and free radical scavenging activities for DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS+ (2,2'-azino-bis (3-ethylbenzothiazoline 6-sulfonic acid ammonium salt) radicals. The laxative effects of T-X were dependent on food, body weight, fecal properties, gastrointestinal transit (GIT) ratio, and serum metabolic parameters. In the T-X group, the number, wet weight, and water content of fecal pellets were noticeably increased compared to those in the loperamide-induced group. T-X treatment significantly increased the activities of hepatic antioxidant enzymes, including those of glutathione peroxidase (GSH-Px), superoxide dismutase (SOD), and catalase (CAT), relative to those in loperamide-induced constipated rats. Furthermore, the GIT ratio and loperamide-induced metabolic parameters in serum, including gastrin (GAS), motilin (MTL), and somatostatin (SS) levels, were significantly improved by T-X treatment. [Conclusion] These results suggest that taurine-xylose exerts antioxidant activities and laxative effects on loperamide-induced constipation by promoting gastrointestinal motility.

• Journal of Digestive Cancer Research
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• 제5권2호
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• pp.86-90
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• 2017

Background: The aim of this study was to investigate clinicopathologic features of type 3 gastric neuroendocrine neoplasm (NEN) by treatment modality. Methods: The Korean Society of Gastrointestinal Cancer conducted the Korean Gastroenteropancreatic Neuroendocrine Tumor Registry, a retrospective registry database of gastroenteropancreatic neuroendocrine tumors from 16 hospitals in Korea. The normal serum gastrin level range was defined as <100 pg/mL, and gastric NEN patients with normal gastrin level were selected for analysis. Results: Among 358 patients with gastric NEN, 21 (5.9%) patients were classified with type 3 gastric NEN. The median age was 53 years (range 30-74). According to the WHO 2010 classification, 13 (61.9%) patients had grade 1, and 8 (38.1%) patients had grade 2 or 3. Endoscopic treatment was performed in 14 (66.7%) patients, and surgery was performed in 7 (33.3%) patients. The tumor size was smaller in the endoscopic treatment group than in the surgery group (0.6 cm vs 1.3 cm, p=0.006). After treatment, there was one recurrence in the surgery group. Conclusion: In small size Type 3 gastric NEN, endoscopic treatment was associated with a good prognosis, compared to surgery. Thus, endoscopic treatment can be used an alternative modality in selected cases of type 3 gastric NEN.

• 대한본초학회지
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• 제24권3호
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• pp.1-12
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• 2009

Objectives : The objective of this study was to compare, the potency of toxicity of Cantharidin containing dried Mylabis phalerata (MP) extract and it's modifier. Methods ： They were monitored at dosage level 2,000, 1,000, 500, 250 and 125 mg/kg, respectively. Changes of body weight, clinical signs, mortality, LD50, macroscopic changes of gastrointestinal tract and liver were observed after single oral dose of test articles with changes of serum Gastrin and Somatostatin levels. Results ： Dosage-dependent decrease of body weight and/or gains were demonstrated in dried MP extract-dosing groups, were also detected in modified and dried MP extract-dosing groups at 2,000 and 1,000 mg/kg-dosing group. However, below 500 mg/kg-dosing group, the body weights were significantly increased compared to that of equal dosage group of dried MP extract-dosing group. Dosage-dependently detected clinical signs in dried MP extract-dosing groups, were also detected in modified and dried MP extract-dosing groups at 2,000 and 1,000 mg/kg-dosing group. However, below 500 mg/kg-dosing group, these clinical signs dramatically were decreased compared to that of equal dosage group of dried MP extract-dosing group. Dosage-dependent increase of mortality rates were observed in dried MP extract-dosing groups, were also detected in modified and dried MP extract-dosing groups at 2,000 and 1,000 mg/kg-dosing group. However, below 500 mg/kg-dosing group, the mortalities were significantly decreased compared to that of equal dosage group of dried MP extract-dosing group. The LD50 of dried MP extract in male mice was dramaticlly increased in their modify, 265.86 vs 426.99 mg/kg. Dosage-dependently increase of number of hemorrhagic and/or erythematous spots detected in the gastrointestinal tracts of dried MP extract-dosing groups, were also detected in modified and dried MP extract-dosing groups at 2,000 and 1,000 mg/kg-dosing group. However, below 500 mg/kg-dosing group, these abnormal spots were dramatically decreased compared to that of equal dosage group of dried MP extract-dosing group. Dosage-dependently increase of degrees of enlargement and congestion detected in the liver of dried MP extract-dosing groups, were also detected in modified and dried MP extract-dosing groups at 2,000 and 1,000 mg/kg-dosing group. However, below 500 mg/kg-dosing group, these abnormal signs were dramatically decreased compared to that of equal dosage group of dried MP extract-dosing group. Dosage-dependently increase of serum gastrin levels of dried MP extract-dosing groups, were also detected in modified and dried MP extract-dosing groups at 2,000 and 1,000 mg/kg-dosing group. However, below 500 mg/kg-dosing group, these abnormal increase were dramatically decreased compared to that of equal dosage group of dried MP extract-dosing group. Dosage-dependently increase of serum somatostatin levels of dried MP extract-dosing groups, were also detected in modified and dried MP extract-dosing groups at 2,000 and 1,000 mg/kg-dosing group. However, below 500 mg/kg-dosing group, these abnormal increase were dramatically decreased compared to that of equal dosage group of dried MP extract-dosing group. Conclusions ： The toxicity of dried MP extract was reduced by their modify.

• 대한한의학방제학회지
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• 제6권1호
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• pp.157-173
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• 1998

The following study looked at the effects of Hyangsayukgunjatang and Hyangsayukgunjatang-ga-kyenegum, moryobun on gastric ulcers in rats. In the 1st experiment, ulcers were induced by method of shay's pylorus-ligated in rats. Subjects were administered 2 kinds of medicine, Hyangsayukgunjatang and Hyangsayukgunjatang-ga-kyenegum, moryobun, which were taken orally. The quantity of gastric juice secretion, total acidity of gastric juice, HCI secretion and serumgastrin content were measured and tissues of gastric mucosa epithelium were observed. 1. The quantity of gastric juice secretion in Hyangsayukgunjatang-treated and Hyangsayukgunjatang-ga-kyenegum, moryobun-treated groups showed significant decrease incomparision with the control group. 2. In relation to total acidity of gastric juice, only Hyangsayukgunjatang -treated groupshowed significant decrease in comparison with the control group. 3. HCI secretion of Hyangsayukgunjatang-treated and Hyangsayukgunjatang-ga-kyenegum, moryobun-treated groups showed significant decrease in comparision with the control group. 4. Content of serum gastrin, which were present in Hyangsayukgunjatang -treated and Hyangsayukgunjatang-ga-kyenegum, moryobun- treated groups showed significant decrease in comparision with the control group. 5. The degree of ulcer occurrence & parietal cell numbers and chief cell numbers of Hyangsayukgunjatang-treated and Hyangsayukgunjatang-ga-kyenegum, moryobun-treatedgroups, which were observed by macrographic & histologic method showed signicant decreasein comparison with the control group. Hyangsayukguniatang-treated group prooved to be increasingly effective. From above the experiment results it can be concluded that Hyangsayukgunjatang will be more clinical effective on curing gastric ulcers induced by method of Shay's pylorus-ligated rather than that of Hyangsayukgunjatang-ga-kyenegum, moryobun.