• Title/Summary/Keyword: ${\alpha}-Glucosidase$ inhibition

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마황 추출물의 항바이러스 활성 (Antiviral activity of methanol extract from Ephedra sinica Stapf)

  • 이도승;이동선
    • 한국식품저장유통학회지
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    • 제21권5호
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    • pp.735-739
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    • 2014
  • Newcastle disease virus(NDV) 감염된 baby hamster kidney(BHK) 세포에서 syncytium(합포체) 형성은 세포막 표면으로의 수송된 바이러스 당단백질 hemagglutinin-neuramidase(HN)에 의해 일어난다. HAU 값은 추출물의 농도가 25과 3.2 ug/mL 사이에서는 현저하게 감소하였으나, NDV 감염된 HAD(%)는 25 ug/mL 농도에서 광범위한 흡착능의 감소를 나타내 바이러스 당단백질의 세포내 생합성은 저해되지 않았다. 그러므로, 약용식물인 마황 메탄올 추출물이 바이러스 당단백질의 세포막으로의 수송과 함께 합포체 형성을 저해하여 항바이러스 작용을 하였다. 또한 마황 추출물의 저해활성을 조사한 결과 ${\alpha}$-glucosidase에 대한 추출물의 $IC_{50}$$18{\mu}g/mL$이었으며, ${\beta}$-glucosidase, ${\alpha}$-mannosidase, ${\beta}$-mannosidase에 대한 마황 추출물의 $IC_{50}$은 각각 60, 40, $150{\mu}g/mL$로 나타나 ${\beta}$-type glycosidases 보다 ${\alpha}$-type glycosidase에 대한 효소활성 저해능이 우수하였다. 따라서 $IC_{50}$농도에서는 세포내에서 당단백질 생합성은 저해되지 않으며 당단백질의 수송을 저해하는 것으로 판단되었으며 향후 항바이러스 관련 작용기작의 연구가 필요하다고 판단된다.

오갈피나무 속(屬) 식물의 항당뇨 및 혈당강하 효과 (Anti-diabetic and Hypoglycemic Effect of Eleutherococcus spp.)

  • 임상현;박유화;권창주;함헌주;정햇님;김경희;안영섭
    • 한국식품영양과학회지
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    • 제39권12호
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    • pp.1761-1768
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    • 2010
  • 오갈피나무 속의 가시오갈피(Eleutherococcus senticosu), 섬오갈피나무(Eleutherococcus gracilistylus), 오가나무(Eleutherococcus sieboldianus), 오갈피나무(Eleutherococcus sessiliflorus)의 잎 부위를 이용하여 $\alpha$-glucosidase와 $\alpha$-amylase 활성 저해 효과를 통한 혈당강하 효과를 평가 하였다. $\alpha$-Glucosidase 활성 저해 효과를 비교한 결과 섬오갈피 잎 추출물이 acarbose 대비 약 43.38%의 활성 저해 효과를 나타내었고, 가시오갈피 잎 추출물이 41.24%의 저해 효과를 보였다. $\alpha$-Amylase 활성 저해 효과를 측정한 결과 acarbose가 10 mg/mL의 농도에서 73.25%의 활성 저해 효과를 보였으며, 가시오갈피 잎 추출물이 acarbose 대비 91.90%의 높은 활성 저해 효과를 나타내었다. 또한 streptozotocin (STZ)으로 당뇨를 유도한 모델에 2주간 오갈피나무 속 식물 추출물을 섭취시킨 후 혈당과 지질 개선 효과를 탐색한 결과 STZ 투여로 인하여 모든 당뇨 유발군은 정상군에 비하여 혈당 수준이 유의적으로 증가하였다. 당뇨 유발 대조군(C)과 대비하여 시료 투여군인 가시오갈피(T1), 섬오갈피나무(T2), 오가나무(T3), 오갈피나무(T4)군 모두 혈당이 크게 감소하였다. 혈중 지질 농도 변화 실험 중 총 콜레스테롤의 함량은 정상군에 비하여 당뇨 유발 대조군은 증가하는 경향을 나타내는 반면 약물 투여군인 가시오갈피(T1), 오가나무 (T3), 오갈피나무(T4)군에서는 대조군에 비하여 유의적으로 감소하였다. HDL-cholesterol은 오가나무군에서 대조군에 비하여 55.61% 가장 크게 유의적으로 증가하였다. LDLcholesterol의 경우 정상군과 대조군과의 큰 차이가 관찰되지 않았으나 섬오갈피나무, 오가나무에서는 유의적으로 증가하였고, 가시오갈피와 오갈피나무 투여군에서는 대조군에 비하여 유의적으로 감소하였다. 혈중 중성지방의 경우 또한 총 콜레스테롤과 유사하게 대조군의 경우 혈중 농도가 증가하였다. 약물 투여군인 오가나무군은 60.16%, 오갈피군은 60.80%, 가시오갈피군은 50.16% 대조군 대비 유의적으로 감소하였다. 적출한 간 내의 중성지방의 농도를 측정한 결과 대조군의 경우 정상군에 비교하여 유의적인 증가를 보였으며, 가시오갈피군, 섬오갈피나무군은 각각 대조군 대비 유의적으로 감소하였다. 이상의 결과들에서 오갈피나무 속 추출물들은 혈당강하 및 당뇨대사 이상으로 인한 지질대사의 개선에 효과적인 것으로 나타났다.

오디와인의 생리활성 및 α-glucosidase 저해제의 분석 (Biological activity and analysis of α-glucosidase inhibitor from mulberry (Morus alba L.) wine)

  • 손우림;최상원
    • 한국식품저장유통학회지
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    • 제20권6호
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    • pp.877-885
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    • 2013
  • 본 연구는 오디를 이용한 고부가가치의 기능성와인을 개발하기 위한 연구의 일환으로 먼저 4가지 베리류과실(오디, 블루베리, 딸기, 복분자)와인의 항당뇨, 항노화 및 항산화활성을 ${\alpha}$-glucosidase, tyrosinase 및 DPPH radical를 사용하여 측정한 후 ${\alpha}$-glucosidase 저해활성이 가장 강한 오디와인으로부터 저해제를 분리 및 동정하였다. 또한, 3 가지 뽕나무 품종(익수뽕, 대성뽕, 청일뽕) 오디를 이용하여 오디와인을 제조하여 품종과 발효에 따른 ${\alpha}$-glucosidase 저해제의 함량 변화를 측정한 결과는 다음과 같다. 4가지 베리류과실 와인의 항산화, 항당뇨 및 항노화 활성을 측정한 결과, 오디와인이 가장 높은 ${\alpha}$-glucosidase 저해활성을(69.37%) 나타내었으며, DPPH 라디컬 소거능은 블루베리(64.57%) 및 오디와인(62.48%)이 유사하게 높았으며, 딸기와인이 가장 높은 tyrosinase 저해활성(59.63%)을 나타내었다. 이 중 ${\alpha}$-glucosidase 저해활성이 가장 높은 오디와인으로부터 효소저해제를 분리 및 동정하기 위해 오디와인을 먼저 감압농축하여 에틸아세테이트로 분획한 다음 Diaion HP-20, ODS-A 및 Sephadex LH-20 column chromatography를 순차적으로 실시하여 4가지 분획을 얻었으며, 이 중 ${\alpha}$-glucosidase 저해활성이 가장 강한 Fr. 4로부터 UV 및 NMR 분석을 통해 quercetin를 동정하였다. 마지막으로 뽕나무 품종 및 발효에 따른 오디와인의 ${\alpha}$-glucosidase 저해제의 함량을 측정한 결과, 대성뽕 오디와인의 quercetin 함량(16.83 ppm)이 가장 높았으나, 익수뽕 및 청일뽕 오디와인의 quercetin 함량은 각각 14.85 및 8.92 ppm으로 낮았다. 그리고 발효 및 숙성에 따라 오디와인의 quercetin 함량은 크게 감소하였다. 이상의 연구 결과로부터 4가지 베리류 과실와인 중 오디와인이 가장 높은 ${\alpha}$-glucosidase 저해활성을 나타내었으며, 주된 저해물질은 quercetin임을 기기분석을 통해 확인할 수 있었기에 향후 오디와인은 당뇨예방용 기능성와인으로서 크게 각광을 받을 것으로 사료된다.

Antioxidant and α-Glucosidase Inhibitory Activities of the Extract from Sparganium stoloniferum Buch.-Ham. Root and Its Constituent Compounds

  • Xu, Ming Lu;Wang, Lan;Hu, Jian He;Wang, Myeong-Hyeon
    • Preventive Nutrition and Food Science
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    • 제14권4호
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    • pp.354-357
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    • 2009
  • Three compounds, vanillic acid, p-hydroxylcinnamic acid, p-hydroxybenzaldehyde have been isolated from the ethylacetate extract of Sparganium stoloniferum Buch.-Ham roots using silica gel open column chromatography, preparative thin-layer chromatography (pTLC) and reverse phase high performance liquid chromatography. The structures of the compounds were established on the basis of IR, extensive 1D NMR, and MS analyses. The ethylacetate (EtOAc) extract, vanillic acid, and p-hydroxybenzaldehyde showed $\alpha$-glucosidase inhibition activity of 72.71%, 20.13%, and 30.42%, at the concentration of 10 ${\mu}g/mL$, respectively. The EtOAc extract exhibited strong antioxidant activity with an $IC_50$ value of 24.37 ${\mu}g/mL$ against DPPH radical scavenging activity, the vanillic acid, p-hydroxylcinnamic acid, and p-hydroxybenzaldehyde with an $IC_50$ value of 2.10 ${\mu}M$, 1.59 ${\mu}M$, and 2.72 ${\mu}M$ against DPPH, respectively.

ISOLATION OF A NEW $\alpha$-GLUCOSIDASE INHIBITOR FROM A FUNGUS, PENICILLIUM SP. F70614

  • Kwon, Oh-Sung;Park, Sang-Ho;Lee, Sang-Hwa;Park, Dong-Jin;Yun, Bong-Sik;Kim, Chang-Jin
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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    • pp.134-134
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    • 1998
  • The modulation of glycosidase activity by inhibitors is of great interest. Such compounds have been shown to be important tools in mechanistic studies on glycohydrolase as well as having promising therapeutic application. An ${\alpha}$-glucosidase inhibitor was isolated from culture filterates of Penicillium sp. The inhibitor was active against ${\alpha}$-glucosidase isolated from yeast and porcine small intestine. However, it showed no inhibition to Aspergillus ${\alpha}$-galactosidase, Escherichia coli ${\beta}$-galactosidase, and jack bean ${\alpha}$-mannosidase. The inhibitor was highly soluble in ether, methanol and chloroform. The inhibitor was purified using silica gel, Sephadex LH-20 column chromatography and reverse-phase HPLC. The inhibitory compound designated PA-7(IC$\sub$50/=35$\mu\textrm{g}$) was obtained as white powder. The structure of PA-7 was determined with spectroscopic data of EI-MS, FAB-MS, $^1$H, and $\^$13/C NMR. The inhibitor has a diketopiperazine moiety.

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Comparative analysis of Bombyx batryticatus and Bombyx mori on α-glucosidase inhibition and their bioactive compositions

  • Hwa Lee;Jong-Hoon Kim
    • International Journal of Industrial Entomology and Biomaterials
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    • 제48권3호
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    • pp.156-162
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    • 2024
  • This study aimed to evaluate and compare the inhibitory effects of extracts from Bombyx batryticatus (BBE) and Bombyx mori (BME) on α-glucosidase, DPP-4, and LDL oxidation activities, focusing on their potential applications in managing postprandial hyperglycemia and metabolic syndrome. The results demonstrated that both BBE and BME effectively inhibited α-glucosidase and LDL oxidation, with BBE exhibiting higher inhibitory activity than BME. HPLC analysis identified linolenic acid, linoleic acid, linolenic acid ethyl ester, pheophorbide a, and pyropheophorbide a as key compounds contributing to these effects. Notably, the identified unsaturated fatty acids and pheophorbides showed strong α-glucosidase inhibitory activity, surpassing that of acarbose, a standard diabetic drug. These results suggest that, in addition to the previously reported 1-DNJ and fibroin proteins, unsaturated fatty acids and chlorophyll-derived pheophorbides may play significant roles in glycemic control. Compounds, particularly those from BBE, present promising opportunities for the development of natural therapeutic agents for diabetes management. The study concludes that BBE and BME have strong potential as functional ingredients in future diabetes treatment strategies, possibly offering enhanced efficacy over conventional inhibitors.

Antioxidant and Anti-diabetes Activities of Methanolic Extract and Fractions of Astragalus membranaceus Roots

  • Park, Jae-Hyo;Yin, Yu;Wang, Myeong-Hyeon
    • Preventive Nutrition and Food Science
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    • 제15권1호
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    • pp.30-35
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    • 2010
  • The potential biological activities of methanol extract and 5 fractions (hexane, $CH_2Cl_2$, EtOAc, BuOH and water) from roots of Astragalus membranaceus were examined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, hydroxyl radical (${\cdot}OH$) scavenging activity, reducing power assays, lipid peroxidation inhibitory activity, $\alpha$-amylase and $\alpha$-glucosidase inhibition assays. The EtOAc fraction showed high DPPH free radical scavenging activity ($EC_{50}=170.34\;{\mu}g/mL$), hydroxyl radical scavenging activity ($EC_{50}=32.14\;{\mu}g/mL$), lipid peroxidation inhibitory activity ($EC_{50}=52.46\;{\mu}g/mL$) and a concentration dependence, with OD value ranging from 0.234 to 0.345 (0.1 to 0.5 mg/mL), for reducing power. The EtOAc fraction has the highest total phenolic content ($142.13\;Gal\;{\mu}g/mg$) and the $CH_2Cl_2$ fraction has the highest flavonoid content ($71.63\;Que\;{\mu}g/mg$). Meanwhile, hexane and EtOAc showed certain $\alpha$-amylase and $\alpha$-glucosidase inhibition activities. These results suggest that the methanol extract and fractions from Astragalus membranaceus root have significant antioxidant and anti-diabetes activities, which could be used as a potential source of pharmaceutical materials.

Biological Activities of Water and Ethanol Extracts from Two Varieties of Rubus coreanus Miquel Fruits

  • Yin, Yu;Wang, Myeong-Hyeon
    • Preventive Nutrition and Food Science
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    • 제16권1호
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    • pp.89-94
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    • 2011
  • The potential biological activities of water and ethanol extracts from two varieties of Rubus coreanus Miquel fruits produced in the Gochang-gun (GR) and Hoengseong-gun (HR) regions of Korea were examined. The hydroxyl radical ($\cdot$OH) scavenging activity, reducing power, lipid peroxidation inhibitory activity, and antiproliferative activity on cancer cells by these extracts were examined, and $\alpha$-amylase and $\alpha$-glucosidase inhibition assays were also performed. The EtOH extract from GR showed high hydroxyl radical scavenging activity ($EC_{50}=119.47{\pm}5.13\;{\mu}g/mL$), lipid peroxidation inhibitory activity ($EC_{50}=213.45{\pm}3.14\;{\mu}g/mL$) and a concentration dependence, with OD values ranging from 0.15 to 0.56 (50 to 200 ${\mu}g/mL$), for reducing power. The EtOH extract from GR has the highest antiproliferative activities on MDA-MB-231 and HepG2 cancer cells among four extracts. Meanwhile, all extracts showed certain $\alpha$-amylase and $\alpha$-glucosidase inhibition activities. These results indicate that extracts from two varieties of R. coreanus fruits have significant antioxidant, anti-diabetic and anti-tumorigenic activities, which suggest these extracts could be a potential source for pharmaceutical.

약용식물 물 추출물의 항산화 활성 및 α-Glucosidase 저해효과 (Antioxidant Activities and α-Glucosidase Inhibitory Effect of Water Extracts from Medicinal Plants)

  • 김현숙;김태우;김대중;이재성;김경곤;최면
    • 한국약용작물학회지
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    • 제21권3호
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    • pp.197-203
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    • 2013
  • We studied the total polyphenol content, DPPH radical scavenging activity, hydroxyl radical scavenging activity and ${\alpha}$-glucosidase inhibition of water extracts from 17 medicinal plants. Total polyphenol contents ranged from 10.0 (Coix lachryma-jobi L, CL) ~ 279.7 (Perilla sikokiana, PS)mg/g. The water extract from medicinal plants were evaluated for its free radical scavenging activities and compared with a commercial antioxidant, ascorbic acid. DPPH radical scavenging activity of Pyrus pyrifolia (PP), Chamaecyparis obtusa L. (COL), Chamaecyparis obtusa F. (COF), and PS were higher than positive control. Higher hydroxyl radical scavenging activity were shown in Acanthopanax senticosus (AS) and Cordyceps militaris (CM) than the other plants. The highest anti-${\alpha}$-glucosidase activity was observed in Cornus officinalis (CO) and Paeonia suffruticosa Andrews (PSA) water extracts. PSA showed not only the higher DPPH radical scavenging activity but also the anti-${\alpha}$-glucosidase activity. The results of our study that PP, COL, COF, PS, AS, CM, CO and PSA could be potential candidates for natural antioxidants.

Screening for Anti-diabetic Effects of Prescribed Korean Traditional Medicines

  • Shin, Seon Mi;Jeong, Yong Joon;Park, Dae Won;Ko, Heung;Kim, Gi Tae;Kim, Ee-Hwa;Kim, Taeseong;Sohn, Eun-Hwa;Kwon, Jung-Eun;Koo, Hyun Jung;Kang, Se Chan
    • 한국자원식물학회지
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    • 제25권6호
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    • pp.670-681
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    • 2012
  • Herb extracts commercially used in Korea were screened for PPAR-${\gamma}$ agonist test and ${\alpha}$-glucosidase inhibition assay. Total 16 herb plants had a PPAR-${\gamma}$ agonist activity. Specially, Alisma orientale Juz (108.41%), Ephedra sinica (98.22%), Sasa japonica Makino var. purpurascens Nakai (140.68%), Astragalus membranaceus Bunge (106.79%) and Cnidium officinale Makino (113.00%) showed high PPAR-${\gamma}$ agonist activity rate compared with rosiglitazone's (167.46%). And Cornus officinalis S. et Z. (90.3%), Cinnamomum cassia Blume (89.2%), Psoralea corylifolia L. (89.8%), Paeonia japonica (Makino) Miyabe (92.4%) and Paeonia suffruticosa Andr (93.2%), showed high ${\alpha}$-glucosidase inhibition rates. These results support previous reports of the efficacy of Oriental medicinal plants used for diabetes mellitus.