• Archives of Pharmacal Research
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• 제28권2호
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• pp.180-185
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• 2005

In the process of investigating anti-obesity effect of Platycodi Radix, we found that aqueous extract of Platycodi Radix might inhibit intestinal absorption of dietary fat by inhibiting pancreatic lipase (PL) activity. In order to clarify the anti-obesity mechanism of Platycodi Radix, activity-guided isolation was performed to find active components. The total saponin fraction of Platycodi Radix appeared to have a potent inhibitory activity against the hydrolysis of triolein emulsified with phosphatidycholine by pancreatic lipase in vitro. Based on these results, further purification of active components yielded 10 known triterpenoidal saponins, among these compounds, platycodin A, C, D, and deapioplatycodin D exhibited significant inhibitory effects on PL at the concentration of $500\;{\mu}g/mL$ with 3.3, 5.2, 34.8, and $11.67\%$ pancreatic lipase activity vs control, respectively. Platycodin D was found to inhibit the PL activity in a dose-dependent manner. Therefore, the anti-obesity effect of Platycodi Radix might be due to the inhibition of pancreatic lipase by its saponins.

• Journal of Applied Biological Chemistry
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• 제48권2호
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• pp.84-88
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• 2005

To develop functional food and anti-obesity drug through inhibition of dietary lipid absorption, inhibitory effects of herb extracts on pancreatic lipase were investigated. Due to high yield and simplicity of isolation, lipase inhibitor (ELI) was isolated from ethyl acetate extract of Eugenia aromaticum, which showed highest inhibitory activity, and characterized for development of novel functional material. Stability of ELI at high temperature and low pH was investigated. Results showed ELI is relatively stable under thermal and acidic conditions, reversible, and noncompetitive inhibitor of pancreatic lipase.

• 한국식품저장유통학회지
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• 제18권3호
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• pp.390-396
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• 2011

신선한 생강을 80% EtOH로 침지 추출하여 얻어진 추출물을 $CHCl_3$, EtOAc, n-BuOH로 순차 용매 분획하였고, pancreatic lipase 저해활성, DPPH 및 $ABTS^+$ radical 소거능을 평가하였다. Pancreatic lipase 저해활성을 측정한 결과, EtOAc층의 15.6 ${\mu}g$/mL의 실험 농도에서 에서 대조군인 orlistat보다 강한 $98.0{\pm}0.7%$ 저해능을 확인하였으며, 생강의 주성분으로 잘 알려져 있는 6-gingerol의 경우 같은 농도에서 $16.2{\pm}0.5%$의 상대적으로 낮은 저해능을 나타내었다. DPPH 라칼 소거능은 페놀성 화합물의 함량이 상대적으로 높은 EtOAc층의 125 ${\mu}g$/mL의 농도에서 $56.5{\pm}1.4%$, 62.5 ${\mu}g$/mL의 농도에서 $40.5{\pm}1.2%$의 라디칼 소거능을 확인하였고, 이는 생강의 항산화 활성은 생강 추출물에 존재하는 6-gingerol 등과 같은 페놀성 화합물이 관여함을 시사하였다. 또한 총페놀성 함량이 g당 $82.0{\pm}0.3$ mg으로 나타난 $CHCl_3$층에 대해서도 $ABTS^+$ 라디칼 소거 활성물질의 존재가 시사되었으며, pancreatic lipase, DPPH 및 $ABTS^+$ 라디칼 소거활성물질의 동정을 진행 중에 있으며, 향후 이들 활성물질의 활성 기작에 대한 연구가 필요하다고 사료된다. 또한 본 연구결과는 보다 우수한 pancreatic lipase 저해능을 가지는 새로운 선도화합물 발굴을 위한 기초자료로 이용될 수 있을 뿐만 아니라 국내에 자생하는 생강의 식물 화학적 성분에 대한 기초자료로 이용될 수 있을 것으로 사료된다.

• 약학회지
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• 제12권1_2호
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• pp.1-15
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• 1968

The levels of activities of amylase, lipase and trypsin in both the pancreatic tissue and serum of 18 species of vertebrate animals were measured and enzymologically compared with each other. 1) The value of amylase in the pancreas of experimental mammalia has been found decreasing in the order pig, rat, dog, cat, rabbit and cow; that of pancreatic lipase has been found decreasing in the order of pig, dog, cat, rat, rabbit and cow; and that of trypsin has been found decreasing in the order of pig, cow, dog, rat, rabbit. Thus the value of all the above three kinds of enzymes were observed highest in pig, but in cow amylase and lipase were observed lowest while trypsin were observed considerably high. 2) In view of diets, the comparatively high values of pancreatic enzyme were observed in the ommivorous animals such as pig, rat, dog, while the values observed low in the herbivorous animals, such as cow and rabbit. 3) In the bovine, the values were observed moderately high except lipase which were found comparatively low. 4) In the Reptilia and Amphibia such a mud turttle and frog, the values were shown in similar measure with each other, that is, the pancreatic amylase and trypsin were observed considerably high while the lipase was found low. 5) In the species of Reptilia such as a viper and snake, the activities of pancreatic enzymes were not detected. But in the tissue of liver, stomach, activities of the enzymes were found considerably high. Lacertilia animals such as lizard the values of pancreatic enzymes were little observed. 6) In the fish in which the pancreatic tissue is scattered in the liver, the pancreatic enzymes were found in the liver tissue considerably higher than in the other tissues but lower than in the warm-blooded animals, especially the lipase was lower. 7) In generally the values of serum amylase and lipase were observed higher than those of man; and even in the cold-blooded animals in which the values of pancreatic enzymes were shown low or none, the values were also observed high. 8) The above three kinds of pancreatic enzyme values of those experimental animals have shown a tendency of higher degree in higher taxa than in lower taxa according to taxonomical order. 9) In view of tissue, the pancreatic cell was observed large in the mammalian animals such as rat and pig and cytoplasm was also abundantly contained in the acinous cell; and the bovine and the snake haave the pancreatic cells of the similar rosette form the comparatively large acinous cells of long rhombic form in the comparatively large acinous cells of long rhombic form in which the spindle shaped neucleus and the abundant cytoplasm were contained. In the fish the pancreatic cell were found scattered in the liver in which the very large pancreatic islet were found.

• 한국식품과학회지
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• 제22권3호
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• pp.248-254
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• 1990

식용 돼지췌장 리파제를 두 가지 함량으로 치즈제조시 혼합하여 $7^{\circ},\;13^{\circ},\;21^{\circ}C$에서 숙성시켰다. GC 분석결과 효소처리한 치즈에서는 Control에서 보다 훨씬 많은 양의 저급지방산이 생성되었다. 돼지췌장 리파제를 많이 넣어 $21^{\circ}C$에서 숙성시킨 치즈의 경우 1주 후에 medium flavor 치즈, 3주 후에 거의 sharp flavor 치즈가 특별한 결함없이 생산되었다. 또한 이 효소를 조금 넣은 치즈에서는 양호한 질의 치즈가 많았는데, $7^{\circ},\;13^{\circ},\;21^{\circ}C$에서 3주부터 15주의 숙성기간 중 medium과 sharp flavor 치즈가 생산되었다. 통계분석에 의하면 체다풍미와 caproic acid의 함량에서, 또 체다풍미와 butyric acid, caproic acid 혼합함량 상호관계에서 유의성이 있었다. 적합한 조건을 사용한다면 돼지췌장 리파제는 체다치즈의 숙성을 촉진시키는데 사용 가능한 것으로 사료된다.

• 대한본초학회지
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• 제32권4호
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• pp.9-15
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• 2017

Objectives : In this study, the inhibitory activities of Korean Medicine against pancreatic lipase in vitro and biochemical analyses in vivo were measured to determine its possibility as a well-matched sauce material with chicken. Methods : The inhibitory activity on pancreatic lipase enzyme of 11 samples were evaluated in vitro and then 5 samples were selected. The activity of pancreatic lipase was investigated using orlistat as a positive control. Animals were divided into eight groups (n=7). The experimental groups except for normal group were fed 60% high-fat diet for 7 days. 5 samples were orally administered at a dose of 200 mg/kg body weight and orlistat were orally administrated at a dose of 60 mg/kg body weight for 7 days. Biochemical anaylses of 5 samples were executed based on lipid parameters analysis. Results : Korean Medicines with an $IC_{50}$ of below 1 mg/kg were Scutellariae Radix, Gardeniae Fructus, Theae Folium Coptidis Radix, and Mori Cortex Radicis. Body weight change of Mori Cortex Radicis reduced significantly, however fecal triglyceride couldn't regulate effectively. The most excellent inhibitory effect of pancreatic lipase showed in Scutellariae Radix treatment and also regulated significantly serum triglyceride and total cholesterol. Moreover, the supplementation of Coptidis Radix excreted meaningfully triglyceride to fece. Conclusions : In conclusion, Coptidis Radix may exert anti-obesity effect by directly inhibiting pancreatic lipase, which would prevent the absorption of lipid from the small intestine. Besides, Mori Cortex Radicis may led to the decrease of the body weight via the different pathway.

• Asian-Australasian Journal of Animal Sciences
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• 제18권2호
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• pp.282-295
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• 2005

The processing of dietary lipids can be distinguished in several sequential steps, including their emulsification, hydrolysis and micellization, before they are absorbed by the enterocytes. Emulsification of lipids starts in the stomach and is mediated by physical forces and favoured by the partial lipolysis of the dietary lipids due to the activity of gastric lipase. The process of lipid digestion continues in the duodenum where pancreatic triacylglycerol lipase (PTL) releases 50 to 70% of dietary fatty acids. Bile salts at low concentrations stimulate PTL activity, but higher concentrations inhibit PTL activity. Pancreatic triacylglycerol lipase activity is regulated by colipase, that interacts with bile salts and PTL and can release bile salt mediated PTL inhibition. Without colipase, PTL is unable to hydrolyse fatty acids from dietary triacylglycerols, resulting in fat malabsorption with severe consequences on bioavailability of dietary lipids and fat-soluble vitamins. Furthermore, carboxyl ester lipase, a pancreatic enzyme that is bile salt-stimulated and displays wide substrate reactivities, is involved in lipid digestion. The products of lipolysis are removed from the water-oil interface by incorporation into mixed micelles that are formed spontaneously by the interaction of bile salts. Monoacylglycerols and phospholipids enhance the ability of bile salts to form mixed micelles. Formation of mixed micelles is necessary to move the non-polar lipids across the unstirred water layer adjacent to the mucosal cells, thereby facilitating absorption.

• 한국식품저장유통학회지
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• 제18권2호
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• pp.250-255
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• 2011

마디풀을 80% ethanol로 침지 추출하여 얻어진 추출물에 대해 $CHCl_3$, EtOAc 및 n-BuOH로 순차 용매 분획 하였고, 얻어진 결과물에 대하여 DPPH 및 $ABTS^+$ radical 소거능 및 pancreatic lipase 저해활성을 평가하였다. DPPH 라디칼 소거능은 페놀성 화합물의 함량이 상대적으로 높은 EtOAc층의 $100{\mu}g/mL$의 시험농도에서는 $58.1{\pm}2.3%$의 라디칼 소거능을 확인하였고, 마디풀 추출물에 존재하는 페놀성 화합물이 라디칼 소거능과의 연관성을 시사하였다. 또한 $ABTS^+$ 라디칼 소거능은 EtOAc층이 $IC_{50}=2.8{\pm}0.5{\mu}g/mL$. $CHCl_3$층이 $IC_{50}=9.2{\pm}0.5{\mu}g/mL$의 강한 활성이 확인되었고, 강력한 활성물질의 존재가 시사되었다. 또한, pancreatic lipase 저해활성을 측정한 결과, 강한 $ABTS^+$ 라디칼 소거능을 나타낸 EtOAc층과 $CHCl_3$층의 $IC_{50}=1.9{\pm}0.2$. $5.7{\pm}1.3{\mu}g/mL$의 저해율을 나타내었으며 이는 대조군인 orlistat에 비해 다소 약하나 단일물질로 정제할 경우 더욱 강한 효능의 화합물이 존재할 가능성을 시사하였다. 향후 이들 활성물질 동정을 통한 활성 기작에 대한 연구가 필요하며 본 연구결과는 보다 우수한 라디칼 소거능 및 pancreatic lipase 저해능을 가지는 새로운 선도화합물 발굴을 위한 기초자료로 이용될 수 있을 뿐만 아니라 국내에 자생하는 마디풀의 식물 화학적 성분연구에 대한 기초자료로 활용가능하리라 사료된다.

• 한국식품저장유통학회지
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• 제17권5호
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• pp.727-732
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• 2010

신선한 산양삼 잎을 EtOH로 침지 추출하여 얻어진 추출물을 n-hexane, EtOAc, n-BuOH 로 용매 분획하였다. 이중 pancreatic lipase 저해활성이 상대적으로 높은 EtOAc 분획에 대해 silica 및 $C_{18}$ column chromatography를 이용하여 3개의 flavonoid 화합물을 분리하였다. 각 화합물의 화학구조는 NMR 스펙트럼 데이터 해석 및 표품과의 HPLC 직접 비교를 통하여 kaempferol-3-O-sophoroside (I), astragalin (II), kaempferol (III)로 동정하였다. 이들 화합물중 kaempferol (III)는 $IC_{50}$ 값이 $9.1{\pm}1.5$ mM로 가장 강한 효능을 나타내었으며, 다음으로 C-3 번 위치에 1개의 glucose가 결합한 astragalin (II)의 $IC_{50}$ 값이 $17.4{\pm}2.7$ ${\mu}M$, C-3 번 위치에 2개의 glucose가 결합한 kaempferol-3-O-sophoroside (I)의 $IC_{50}$ 값이 $20.3{\pm}2.2$ ${\mu}M$의 저해능을 나타내었다. 산양삼 잎의 EtOAc 가용부에에 존재하는 flavonoid계 pancreatic lipase 저해활성 물질을 동정하였으며, 이들 활성은 kaempferol 타입의 화합물은 C-3위치에 당 결합에 의한 hydrophobicity와 관련됨을 시사하였다. 향후 이들 활성물질의 활성 기작에 대한 연구가 필요하며 본 연구결과는 보다 우수한 pancreatic lipase 저해능을 가지는 새로운 선도화합물 발굴을 위한 기초자료로 이용될 수 있을 뿐만 아니라 산양삼잎의 식물 화학적 성분에 대한 기초자료로 이용될 수 있을 것으로 사료된다.

• Natural Product Sciences
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• 제18권3호
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• pp.153-157
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• 2012

Obesity, which is characterized by excessive fat accumulation in adipose tissues, occurs by fat absorption by lipase and sequential fat accumulation in adipocyte through adipocyte differentiation. Thus, inhibition of pancreatic lipase activity and adipocyte differentiation would be crucial for the prevention and progression of obesity. In the present study, we attempted to evaluate anti-adipogenic activity of several algae extracts employing preadipocytes cell line, 3T3-L1 as an in vitro assay system. The effects on pancreatic lipase activity in vitro were also evaluated. Total methanolic extracts of Cladophora wrightiana and Costaria costata showed significant inhibitory activity on adipocyte differentiation as assessed by measuring fat accumulation using Oil Red O staining. Related to pancreatic lipase, C. wrightiana and Padina arborescens showed significant inhibition. Further fractionation of C. wrightiana, which showed the most potent activity, suggested that $CHCl_3$ and n-BuOH fraction are responsible for adipocyte differentiation inhibition, whereas n-BuOH and $H_2O$ fraction for pancreatic lipase inhibition. Our study also demonstrated that n-BuOH fraction was effective both in early and middle stage of differentiation whereas $CHCl_3$ fraction was effective only in early stage of differentiation. Taken together, algae might be new candidates in the development of obesity treatment.