• 제목/요약/키워드: Bioactive agents

검색결과 158건 처리시간 0.032초

야생 복숭아나무 추출물의 항산화 및 항염증 효과 (Antioxidant and Antiinflammation Activities of Prunus persica Tree Extracts)

  • 차배천;이은희
    • 한국약용작물학회지
    • /
    • 제12권4호
    • /
    • pp.289-294
    • /
    • 2004
  • 인류의 수명이 연장되고 노령화 사회로 발전됨에 따라 다양한 성인병이 야기되고 있고, 이들 성인병의 원인이 활성산소에 의한 것으로 밝혀짐에 따라 다양한 성인병을 예방 치료할 수 있는 안전하고 우수한 항산화 및 항염증 물질을 천연물로부터 개발하기 위한 연구의 일환으로 자생식물의 하나인 야생복숭아 가지에 대하여 그들의 MeOH 엑스를 필두로 한 분획물 엑스를 대상으로 항산화 및 항염증 효과를 조사하였다. DPPH 법을 사용하여 야생복숭아 가지의 분획물 엑스에 대한 1차 라디칼 소거작용 검색 시험을 한 결과 야생복숭아 가지 의 n-BuOH 엑스와 EtOAc 엑스가 가장 강한 항산화 활성을 나타내었다. 1차 실험에서 얻어진 결과를 토대로 야생복숭아에 대하여 보다 상세한 항산화 효과를 검토하기 위하여 Ferric-Thiocyanate 법을 이용한 지질 과산화 억제작용 시험한 결과 야생복숭아 가지 의 EtOAc 엑스가 천연 항산화제인 tocopherol 및 합성 항산화제인 BHA 보다 우수한 탁월한 항산화 효과를 나타내었고, Rancimat법에 의한 지질 산패 억제 실험을 실시한 결과 또한 야생복숭아 가지의 EtOAc 엑스가 tocopherol보다 우수하고 BHA보다는 약간 우수한 강력한 지질 산패 억제 효과를 보였다. Hyaluronidase 저해에 의한 항염증 효과 시험에서는 항산화 실험에서 전반적으로 우수한 항산화 효과를 보인 야생복숭아 가지의 EtOAc 엑스가 ketoprofen보다는 약하나 ibuprofen과 indomethacin보다는 우수한 항염증 효과를 나타내었다. 이상의 실험 결과는 야생복숭아의 항산화 및 항염증 효과의 활성 주성분 분획은 EtOAc 엑스임을 시사하였다.

한국 자생식물로부터 아라키돈산 대사계 효소 저해제 검색(1) (Screening of Arachidonic acid Cascade Related Enzymes Inhibitors from Korean Indigenous Plants(1))

  • 문태철;정혜진;이은경;박해영;전수진;손건호;김현표;배기환;강삼식;권동렬;장현욱
    • 생약학회지
    • /
    • 제34권1호통권132호
    • /
    • pp.109-117
    • /
    • 2003
  • Arachidonic acid(AA), which is stored in membrane glycerophospholipids, is liberated by phospholipase $A_2(PLA_2)$ enzymes and is sequentially converted to cyclooxygenase (COX) and lipoxygenase (LOX) then to various bioactive prostaglandins (PGs,) and leukotrienes (LTs). In order to find the specific inhibitors of AA metabolism enzymes such as $PLA_2$, COX-2, 5-LO and lyso PAF acetyltransferase. 195 Korean indigenous plant extracts were evaluated for their inhibitory activity on $PGD_2,\;LTC_4$ production from cytokine-induced mouse bone marrow-derived mast cells (BMMC) and arachidonic acid released from phospholipid and PAF production from lyso PAF. From this screening procedure, methanol extract of eight plants such as Saururus chinensis, Aster tataricus, Chrysanthemum cinerariaefolium, Reynoutria japonica, Disocorea nipponica, Epimedium koreanum, impatiens textori, Veronica rotunda var. subintegra were found to inhibit production of inflammatory mediators in vitro assay system.

Role of fumarates in adaptogenics like efficacies of traditionally used Fumaria indica extracts

  • Shakya, Anshul;Chatterjee, Shyam Sunder;Kumar, Vikas
    • 셀메드
    • /
    • 제5권1호
    • /
    • pp.6.1-6.10
    • /
    • 2015
  • Fumaria indica Linn. (Syn: Fumaria parviflora, Fumariaceae) is a wildly grown weed, mentioned and recommended in classical Ayurvedic texts for treatments of variety of ailments including dermatological diseases, topical diseases, cardiovascular complaints, circulatory disease, fever and headache etc. The present pilot study was designed to experimentally verify the possibility that fumarates are the major bioactive principles of Fumaria indica extracts involved in their stress response modulating activities, and to estimate pharmacologicallyactive dose ranges of fumarates and standardized methanolic extract of Fumaria indica (MFI). Effect of single, 5 and 10 daily oral doses of pure fumaric acid (FA), monomethyl fumarate (MMF), dimethyl fumarate (DMF) and MFI was quantified in well validated rodent models viz. apomorphine induced cage climbing, stress induced hyperthermia, and elevated plus-maze tests. Obtained results reveal high efficacy of MFI and pure fumarates possess qualitatively analogous activity profiles in all the three tests. There were no significant difference in the potencies of pure FA, MMF and DMF in the three tests, whereas efficacy of MFI in the elevated plus maze test for anxiolytics was higher than in the other two tests. Efficacies of all the four test agents in all the three tests increased with increasing number of days of oral treatments. Results of these pilot experiments should be helpful for more rational selections of pharmacologically interesting dose ranges and treatment regimens of fumarates and Fumaria indica extracts for further more holistic explorations of their diverse therapeutic potentials.

Antifungal Effect of Triglycerol Monolaurate Synthesized by Lipozyme 435-Mediated Esterification

  • Zhang, Song;Xiong, Jian;Lou, Wenyong;Ning, Zhengxiang;Zhang, Denghui;Yang, Jiguo
    • Journal of Microbiology and Biotechnology
    • /
    • 제30권4호
    • /
    • pp.561-570
    • /
    • 2020
  • This study was designed to synthesize triglycerol monolaurate (TGML) with Lipozyme 435 as the catalyst, and explore its effects on the growth of Aspergillus parasiticus (A. parasiticus) and Aspergillus flavus (A. flavus) and the secretion of aflatoxin b1. The highest content of TGML (49.76%) was obtained at a molar ratio of triglycerol to lauric acid of 1.08, a reaction temperature of 84.93℃, a reaction time of 6 h and an enzyme dosage of 1.32%. After purification by molecular distillation combined with the washes with ethyl acetate and water, the purity of TGML reached 98.3%. Through characterization by electrospray-ionization mass spectrometry, infrared spectrum and nuclear magnetic resonance, the structure of TGML was identified as a linear triglycerol combined with lauroyl at the end. Finally, the inhibitory effects of TGML on the growths of A. parasiticus and A. flavus and the secretion of aflatoxin b1 were evaluated by measuring the colony diameter, the inhibition rate of mycelial growth and the content of mycotoxin in the media. The results indicated that TGML had a stronger inhibitory effects on colony growth and mycelial development of both toxic molds compared to sodium benzoate and potassium sorbate, and the secretions of toxins from A. parasiticus and A. flavus were completely suppressed when adding TGML at 10 and 5 mM, respectively. Based on the above results, TGML may be used as a substitute for traditional antifungal agents in the food industry.

현초에서 분리된 페놀성 화합물들의 흰쥐 수정체 유래 알도즈 환원효소 및 갈락티톨 생성 억제 효과 (Inhibitory Effect of the Phenolic Compounds from Geranium thunbergii on Rat Lens Aldose Reductase and Galactitol Formation)

  • 최세진;김진규;장재만;임순성
    • 한국약용작물학회지
    • /
    • 제20권4호
    • /
    • pp.222-230
    • /
    • 2012
  • We evaluated the inhibitory effects of extracts and components of Geranium thunbergii on aldose reductase (AR) and galactitol formation in rat lenses with high levels of galactose as a part of our ongoing search of natural sources for therapeutic and preventive agents for diabetic complications. The inhibitory effects of water, methanol and ethanol extracts of G. thunbergii on rat lens AR (RLAR) were determined. Comparing inhibitory effects of various solvent extracts, ethanol extract showed RLAR inhibitory activity ($IC_{50}$ values, 5.24 and $6.39{\mu}g/m{\ell}$, respectively). The ethanol extract was fractionated to chloroform, ethyl acetate and water. Of these, the ethyl acetate fraction from ethanol extract of G. thunbergii exhibited RLAR inhibitory activity ($IC_{50}$ value, $2.64{\mu}g/m{\ell}$). In order to identify the bioactive components of ethyl acetate soluble fraction of ethanol extract from G. thunbergii, eight compounds, namely gallic acid (1), protocatechuic acid (2), p-hydroxybenzoic acid (3), brevifolin carboxylic acid (4), geraniin (5), ellagic acid (6), kaempferol-3-O-arabinofuranosyl-7-O-rhamnopyranoside (7), kaempferitrin (8) were isolated. The isolates were subjected to in vitro bioassays to evaluate their inhibitory activity on RLAR and galactitol formation in rat lenses. The ellagic tannins (5, 6) and flavonoid (7) exhibited strong inhibitory effects on RLAR. Also, these three compounds (5, 6 and 7) suppressed galactitol accumulation in rat lens under high galactose conditions, demonstrating the potential to prevent galactitol accumulation exo vivo. These results suggest that the extracts and components of G. thunbergii are a promising agent in the prevention or treatment of diabetic complications.

황정(黃精)과 증숙 황정(蒸熟 黃精)의 항산화, 항피로 효능 비교 연구 (Antioxidant and Anti-physical fatigue Effects of Polygonati Rhizoma and steamed Polygonati Rhizoma)

  • 김정수;이아름;노성수;권오준;서영배
    • 대한본초학회지
    • /
    • 제31권3호
    • /
    • pp.49-57
    • /
    • 2016
  • Objectives: Polygonati Rhizoma (PR) has containing the bioactive compounds such as poly sccharide A,B,C, oligosaccharide, amino acid, it has reported to anti-diabetes and hypertension, atherosclerosis. In this study, we were evaluates antioxidant and anti-physical fatigue effects of PR and steamed PR.Methods : The sample was divided into 5 groups-PR0 (PR without steaming process), PR1 (PR with once steaming process), PR3 (PR with third steaming process), PR6 (PR with sixth steaming process), PR9 (PR with ninth steaming process). We measured anti-oxidant activity through contents of polyphenol, flavonoid and DPPH, ABTS free radical scavenging capacity. And, anti-physical fatigue effect was evaluated using the swimming test, and the AMPK protein expressions in soleus muscle.Results : As a result, polyphenol, flavonoid, DPPH, ABTS free radical scavenging capacity of PR were increased as steaming times. Anti-physical fatigue effects by swimming test, PR0 have significantly increased, but steamed PR groups were decreased. The AMPK protein expressions of PR0 and PR1 groups were increased comparing with PR3, PR6 and PR9. All groups had effects on decreasing TG, creatine in blood serum, but had no effects on TC in blood serum.Conclusions : In conclusion, PR with 9 steaming process was more excellent than not-processed PR in anti-oxidant effect such as DPPH, ABTS radical scavenging activity and contents of polyphenol, flavonoid, but, not-processed PR increased swimming times than processed PR. These results suggest that processed PR has anti-oxidant effect as steaming times, and not-processed PR may be a novel potential anti-physical fatigue agents than processed PR.

산수유 퓨레로 제조한 젤리의 품질 특성 (Quality Characteristics of Jelly Using Fresh Puree of Sansuyu (Corni Fructus))

  • 정지숙;박수진;손병길
    • 한국식품영양과학회지
    • /
    • 제46권1호
    • /
    • pp.83-91
    • /
    • 2017
  • 본 연구는 산수유 퓨레를 첨가하여 젤리를 제조하였으며, 젤화제 종류 및 함량, 가열시간에 따른 젤리의 이화학적 품질 특성을 조사하였다. 산수유 퓨레는 수분 함량 89.39%, pH 2.92, 당도 $10.28^{\circ}Brix$, 총폴리페놀 함량 1,791.71 mg GAE/100 g이었다. 산수유 퓨레 첨가량이 증가할수록 pH는 3.04~2.97로 소폭 감소하였으나 부착성은 큰 폭으로 감소하였다. 또한, 가열시간이 증가할수록 붉은색이 불안정하여 황색으로 변하였으며, 5분 이상 가열 시에는 젤리가 되지 않았다. 산수유 젤리의 pH는 3.04~2.97, 당도는 $64.31{\sim}66.96^{\circ}Brix$ 범위였다. 산수유 퓨레 10%, 한천 1.5%, 카라기난 1.0% 첨가한 젤리의 기호도가 5.15로 가장 높게 평가 되었다. 산수유 과육을 이용함으로써 과육에 포함된 다양한 생리활성 물질을 효과적으로 섭취할 수 있는 젤리 제조가 가능할 것으로 본다.

Enhanced Anti-inflammatory Effects of γ-irradiated Pig Placenta Extracts

  • Kim, Kang Chang;Heo, Jae Hyeok;Yoon, Jong Kwang;Jang, Yuyeon;Kim, Youn Kyu;Kim, Chang-Kyu;Oh, Yu-Kyung;Kim, Young Bong
    • 한국축산식품학회지
    • /
    • 제35권3호
    • /
    • pp.293-298
    • /
    • 2015
  • Porcine placenta extract (PPE) is known to possess anti-inflammatory properties owing to its high concentration of bioactive substances. However, the need to eliminate blood-borne infectious agents while maintaining biological efficacy raises concerns about the optimal method for sterilizing PPE. Therefore, the objective of this study was to compare the effects of the standard pressurized heat (autoclaving) method of sterilization with γ-irradiation on the anti-inflammatory effects of PPE. The anti-inflammatory actions of these two preparations of PPE were evaluated by measuring their inhibitory effects on the production of NO, the expression of iNOS protein, and the expression of iNOS, COX2, TNF-α, IL-1β, and IL-6 mRNA in lipopolysaccharide-stimulated RAW 264.7 cells. Compared with autoclaved PPE, γ-irradiated PPE showed significantly greater inhibition of NO production and iNOS protein expression, and produced a greater reduction in the expression of iNOS, COX2, TNF-α, IL-1β, and IL-6 mRNA. These results provide evidence that the sterilization process is crucial in determining the biological activity of PPE, especially its anti-inflammatory activity. Collectively, our data suggest that γ-irradiated PPE acts at the transcriptional level to effectively and potently suppresses the production of NO and the expression of pro-inflammatory cytokines.

Virtual Screening Approaches in Identification of Bioactive Compounds Akin to Delphinidin as Potential HER2 Inhibitors for the Treatment of Breast Cancer

  • Patidar, Kavisha;Deshmukh, Aruna;Bandaru, Srinivas;Lakkaraju, Chandana;Girdhar, Amandeep;Gutlapalli, VR;Banerjee, Tushar;Nayarisseri, Anuraj;Singh, Sanjeev Kumar
    • Asian Pacific Journal of Cancer Prevention
    • /
    • 제17권4호
    • /
    • pp.2291-2295
    • /
    • 2016
  • Small molecule tyrosine kinase inhibitors targeting HER 2 receptors have emerged as an important therapeutic approach in inhibition of downstream proliferation and survival signals for the treatment of breast cancers. Recent drug discovery efforts have demonstrated that naturally occurring polyphenolic compounds like delphinidin have potential to inhibit proliferation and promote apoptosis of breast cancer cells by targeting HER2 receptors. While delphinidin may thus reduce tumour size, it is associated with serious side effects like dysphonia. Owing to the narrow therapeutic window of delphinidin, the present study aimed to identify high affinity compounds targeting HER2 with safer pharmacological profiles than delphinidin through virtual screening approaches. Delphinidin served as the query parent for identification of structurally similar compounds by Tanimoto-based similarity searching with a threshold of 95% against the PubChem database. The compounds retrieved were further subjected to Lipinski and Verber's filters to obtain drug like agents, then further filtered by diversity based screens with a cut off of 0.6. The compound with Pubchem ID: 91596862 was identified to have higher affinity than its parent. In addition it also proved to be non-toxic with a better ADMET profile and higher kinase activity. The compound identified in the study can be put to further in vitro drug testing to complement the present study.

Protective Effects of [6]-Paradol on Histological Lesions and Immunohistochemical Gene Expression in DMBA Induced Hamster Buccal Pouch Carcinogenesis

  • Mariadoss, Arokia Vijayaanand;Kathiresan, Suresh;Muthusamy, Rajasekar;Kathiresan, Sivakumar
    • Asian Pacific Journal of Cancer Prevention
    • /
    • 제14권5호
    • /
    • pp.3123-3129
    • /
    • 2013
  • Background: The search for naturally occurring agents in routinely consumed foods that may inhibit cancer development is of high priority. [6]-Paradol is a pungent phenolic bioactive component from ginger with welldocumented health promoting antioxidant, antimutagenic, antigenotoxic and anti-inflammatory properties. However, anticarcinogenic effects have yet to be fully explored. The objectives of the present study were therefore to assess protective effects against 7,12-dimethylbenz(a)anthracene (DMBA) induced buccal pouch carcinogenesis in male golden Syrian hamsters. Methods: Oral squamous cell carcinomas developed in the left buccal pouch of hamsters on painting with 0.5% of DMBA, three times in a week. To assess the apoptotic associated gene expressing potential of [6]-paradol, it was orally administered to DMBA treated hamsters on alternate days from DMBA painting for 14 weeks. Results: We observed 100% tumor formation with marked levels of neoplastic changes and altered the expression of apoptotic associated gene (p53, bcl-2, caspase-3 and TNF-${\alpha}$) was observed in the DMBA alone painted hamsters as compared to control hamsters. Oral administration of [6]-paradol at a dose of 30 mg/kg b.wt to DMBA treated animals on alternative days for 14 weeks significantly reduced the neoplastic changes and improved the status of apoptosis associated gene expression. Conclusion: These observations confirmed that [6]-paradol acts as a tumor suppressing agent against DMBA induced oral carcinogenesis. We also conclude that [6]-paradol also effectively enhances apoptosis- associated gene expression in DMBA treated animals.