• 제목/요약/키워드: product inhibition

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Ethnopharmacological Evaluation of Peristrophe bicalyculata Nees. for Anti-inflammatory and Analgesic Activity

  • Rathi, Anshu;Rao, Ch.V.;Khatoon, S.;Mehrotra, S.
    • Natural Product Sciences
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    • v.9 no.3
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    • pp.195-199
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    • 2003
  • The ethanolic (50% v/v) extracts of Peristrophe bicalyculata Nees. (Acanthaceae) were examined for anti-inflammatory and analgesic activities in experimental animals. P. bicalyculata in doses of 50, 100 and 200 mg/kg caused a dose dependent inhibition of swelling caused by carrageenin equivalent to 12.25-24.49% protection and 16.62-39.44% in cotton pellet induced granuloma in rats. There was a significant increase in the tail-flick reaction time in mice (18.05-76.43% protection) and analgesy-meter induced pain in rats (14.49-56.85%) protection). The extract of P. bicalyculata resulted in an inhibition of stretching episodes and the protection range of 14.49-56.85% respectively in acetic acid induced writhing.

Lignan Derivatives from Fraxinus rhynchophylla and Inhibitory Activity on Pancreatic Lipase

  • Ahn, Jong-Hoon;Shin, Eun-Jin;Liu, Qing;Kim, Seon-Beom;Choi, Kyeong-Mi;Yoo, Hwan-Soo;Hwang, Bang-Yeon;Lee, Mi-Kyeong
    • Natural Product Sciences
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    • v.18 no.2
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    • pp.116-120
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    • 2012
  • Pancreatic lipase digests dietary fats by hydrolysis, which is a key enzyme for lipid absorption. Therefore, reduction of fat absorption by the inhibition of pancreatic lipase is suggested to be a therapeutic strategy for obesity. We previously reported coumarins and secoiridoids of Fraxinus rhynchophylla as inhibitory constituents on adipocyte differentiation. Further investigation on F. rhynchophylla led to the isolation of lignan derivatives such as lignans (1 - 10), sesquilignans (11 - 14) and coumarinolignans (15 - 17). Among them, coumarinolignans and sesquilignans were first reported from Fraxinus species. Among the constituents isolated, sesquilignans showed the significant inhibition on pancreatic lipase, whereas lignans and coumarinolignans exerted weak effects.

Influence of Food Ingredients on the Formation of Heterocyclic Aromatic Amine in Cooked Pork Patties

  • Shin, Han-Seung
    • Food Science and Biotechnology
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    • v.14 no.5
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    • pp.572-575
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    • 2005
  • The effects of cooking method, cooking time and various food ingredients on the formation/ inhibition of heterocyclic aromatic amines (HAAs) in pork products were investigated. Three HAAs, 2-amino-3,8-dimethylimidazo [4,5-f] quinoxaline ($MeIQ_x$), 2-amino-3,4,8-trimethylimidazo [4,5-f] quinoxaline ($DiMeIQ_x$) and 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP) were measured in pork products using solid-phase extraction and HPLC. Pork patties were boiled, oven-broiled and pan-fried to internal temperatures of 71, 77 and $88^{\circ}C$. Generally, HAA concentrations increased with increasing internal temperature, and HAA formation was greatest with pan-fried. Selected food ingredients (vitamin E, sodium nitrite, sodium tripolyphosphate, sodium ascorbate, Nanking cherry tissue and cherry tissue extract) inhibited HAA formation in pork patties fried at $225^{\circ}C$ for 10 min/side, with the greater inhibition provided by cherry tissue and its methanolic extract.

Effects of Amino Acids on the Inhibition of Polyphenol Oxidase Activity from Perillae Folium (아미노산류가 들깨잎 폴리페놀 옥시다제 활성저해에 미치는 영향)

  • Park, Soo-Sun;Kim, An-Keun;Sohn, Eun-Soo
    • YAKHAK HOEJI
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    • v.40 no.1
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    • pp.65-71
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    • 1996
  • Characterization of Polyphenol oxidase (PPO) in Perillae Folium, particullarly inhibitor studies were investigated. This enzyme was stable at pH 5.0 and the residual activity of PPO at ${\geq}$ ph 5.5 was estimated to be very low. PPO activity was decreased slightly by adding amino acid with catechol as a substrate, particullary PPO activity was inhibited markedly by cystein, histidine, lysine and arginine. In the absorption spectra of the product formed when catechol was oxidized by PPO, with a ${\lambda}_{max}$ at 410nm, the peak shifted toward ${\lambda}_{max}$ 520nm by addition of L-proline. At relatively low concentrations($10^{-3}M$), sulfite and dithiothreithol completely inhibited PPO activity. Inhibition of PPO activity by amino acids and inhibitors increased or decreased depending on the pH used to measure it.

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Synthesis of Flavokawain Analogues and their Anti-neoplastic Effects on Drug-resistant Cancer Cells Through Hsp90 Inhibition

  • Seo, Young Ho;Park, Sun You
    • Bulletin of the Korean Chemical Society
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    • v.35 no.4
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    • pp.1154-1158
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    • 2014
  • Hsp90 is an ubiquitous molecular chaperone protein, which plays an important role in regulating maturation and stabilization of many oncogenic proteins. Due to its potential to simultaneously disable multiple signaling pathways, Hsp90 represents great promise as a therapeutic target of cancer. In this study, we synthesized flavokawain analogues and evaluated their biological activities against drug-resistant cancer cells. The study indicated that compound 1i impaired the growth of gefitinib-resistant non-small cell lung cancer (H1975), down-regulated the expression of Hsp90 client proteins including EGFR, Her2, Met, Akt and Cdk4, and upregulated the expression of Hsp70. The result strongly suggested that compound 1i inhibited the proliferation of cancer cells through Hsp90 inhibition. Overall, compound 1i could serve as a potential lead compound to overcome the drug resistance in cancer chemotherapy.

Cytotoxic and Antibacterial Activities of Gossypin

  • Chamundeeswari, D.;Sukumar, Ethirajan;Amar, K.;Reddy, N. Brahmananda;Kumar, I. Anil;Chowdry, B.V.;Samatha, K.
    • Natural Product Sciences
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    • v.13 no.4
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    • pp.300-303
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    • 2007
  • Gossypin, a naturally occurring polyhydroxy flavonoid, when subjected to in vitro cytotoxic screening against vero cell lines exhibited 68.75% inhibition at a concentration of $1000{\mu}g$. When tested against five bacteria and five fungi, the flavone derivative showed a moderate activity against Staphylococcus aureus and Escherichia coli, mild inhibition against Pseudomonas aerugenosa and Salmonella typhi and no activity against any of the tested fungi, in the concentrations studied.

Effects of Divalent Cations on the Self-splicing Inhibition of Group I Intron by the Coen-zyme Thiamine Pyrophosphate (2가 양이온이 Thiamine Pyrophosphate에 의한 Group I Intron Ribozyme의 Splicing 억제에 미치는 영향)

  • 안성준;박인국
    • Korean Journal of Microbiology
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    • v.38 no.1
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    • pp.13-18
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    • 2002
  • Effects of divalent cations such as $Mg^{2+}$, $Mn^{2+}$ and $Zn^{2+}$ on the self-splicing inhibition of the T4 phage thymidylate synthase (td) intron by the coenzyme thiamine pyrophosphate have been investigated. The splicing activity increased in proportion to the concentration of $Mg^{2+}$ up to 30 mM. Without $Mg^{2+}$in the splicing reaction the $Zn^{2+}$ ion tested in the range of 0.1-6 mM concentration only produced the splicing activity about 20% that of the normal splicing rate. A majority of the splicing products were I-E2 and E2 but El-E2 ligation product, Cl and Ll were not detected. Similar patterns of splicing products were also observed with $Mn^{2+}$. At 6 mM $Zn^{2+}$the intron RNA was hydrolyzed. $Mn^{2+}$produced a little higher splicing activity than that of $Zn^{2+}$over the range of concentrations used and at 8 mM about 28% splicing activity was observed. In contrast, $Mn^{2+}\;and\;Zn^{2+}$ ions promoted the splicing activity about 35-40% on an average in the presence of 10 mM $Mg^{2+}$. Of all divalent cations tested, $Mg^{2+}$exhibited the maximum activation effect to counteract the splicing inhibition by thiamine pyrophosphate. This appears to be due to the stabilizing effect of td intron ribozyme structure essential for the catalytic function by $Mg^{2+}$.

Hypolipidemic effect of Salicornia herbacea in animal model of type 2 diabetes mellitus

  • Hwang, Ji-Yeon;Lee, Soo-Kyung;Jo, Ja-Rim;Kim, Mi-Eun;So, Hyun-Ah;Cho, Chang-Woo;Seo, Young-Wan;Kim, Jung-In
    • Nutrition Research and Practice
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    • v.1 no.4
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    • pp.371-375
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    • 2007
  • To control blood glucose level as close to normal is a major goal of treatment of diabetes mellitus. Hyperglycemia and hyperlipidemia are the major risk factors for cardiovascular complications, the major cause of immature death among the patients with type 2 diabetes. The purpose of this study is to determine the hypoglycemic and hypolipidemic effects of Salicornia herbacea in animal model of type 2 diabetes and to investigate the possible mechanisms for the beneficial effects of S. herbacea. S. herbacea was extracted with 70% ethanol and desalted with 100% ethanol. Three week-old db/db mice (C57BL/KsJ, n=16) were fed AIN-93G semipurified diet or diet containing 1% desalted ethanol extract of S. herbacea for 6 weeks after 1 week of adaptation. Fasting plasma glucose, triglyceride, and total cholesterol were measured by enzymatic methods and blood glycated hemoglobin ($HbA_{1C}$) by the chromatographic method. Body weight and food intake of S. herbacea group were not significantly different from those of the control group. Fasting plasma glucose and blood glycated hemoglobin levels tended to be lowered by S. herbacea treatment. Consumption of S. herbacea extract significantly decreased plasma triglyceride and cholesterol levels (p<0.05). The inhibition of S. herbacea extract against yeast ${\alpha}$-glucosidase was 31.9% of that of acarbose at the concentration of 0.5 mg/mL in vitro. The inhibitory activity of ethanol extract of S. herbacea against porcine pancreatic lipase was 59.0% of that of orlistat at the concentration of 0.25 mg/mL in vitro. Thus, these results suggest that S. herbacea could be effective in controlling hyperlipidemia by inhibition of pancreatic lipase in animal model of type 2 diabetes.

Anti-wrinkle Effect of Chestnut Leaf (밤나무잎의 항주름 효과)

  • Jang, Min Jung;Jun, Dong Ha;Kim, Sea Hyun;Han, Sang Ik;Lee, Jin Tae
    • Journal of Life Science
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    • v.23 no.6
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    • pp.751-756
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    • 2013
  • This research old age chestnut tree that loss function chestnut leaf renewal efficiency enlargement and development of cosmeceutical product by purpose. Chestnut leaf (CL) exhibits numerous pharmacological effect including anti-allergy and anti-microbial properties. However, the anti-wrinkle effect of CL is not completely understood. In this study, to find a possible explanation for the anti-wrinkle effects of CL, we evaluated the effects of CL on radical scavenging activity, elastase inhibition activity and collagenase inhibition activity. CL was extracted with various solvents including water (CLW), 70% ethanol (CLE) and 70% acetone (CLA). The results showed that CLW, CLE, and CLA have the radical scavenging activity. In addition, we showed that CLW, CLE, and CLA have the elastase inhibition activity and collagenase inhibition activity. Consequently, the CL has a potent anti-wrinkle effect and it could be a useful cosmeceutical product for anti-aging purposes.

Biotransformation of benzyle trans-2-phenylcyclopropanecarbamate to tranylcypromine in rats

  • Il, Kang-Gun;Chung, Soon-Young
    • Archives of Pharmacal Research
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    • v.7 no.2
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    • pp.141-143
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    • 1984
  • A metabolic study was performed in order to characterize the in vivo MAO-inhibitory activity of benzyl trans-2-phenylcylopropanecarbamate which was reported to be twice as potent as the tranylcypromine. In the rat urine which was obtained after the administration of the benzyl trans-2-pheny-lcyclopropanecarbamate (40mg/kg) through oral route, a metabolic product, tranylcypromine as well as the intact drug was detected by GC/MS.

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