• Title/Summary/Keyword: antihypercholesterolemic

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Synthesis of 3-Substituted 4,5-Hexamethylenepyrazole Derivatives as Potential Antihypercholesterolemic Agents (고콜레스테롤혈증 치료제로서 3-치환 4,5-헥사메틸렌피라졸 유도체의 합성)

  • Choe, Young-Hee;Kim, Jin-Il;Jahng, Yurng-Dong
    • YAKHAK HOEJI
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    • v.38 no.4
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    • pp.363-365
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    • 1994
  • A series of 6-[2-(3-substituted 4,5-hexamethylenepyrazo-1-yl)ethyl]tetrahydro-4-hydroxy-2H-pyran-2-ones were synthesized from 3-substituted 4,5-hexamethylenepyrazole in 7 steps as potential antihypercholesterolemic agents.

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Radical Scavenging and Antihypercholesterolemic Effects of Red Yeast Rice in Cholesterol Fed Rats

  • Suh, Hyung-Joo;Kim, Young-Soon;Chang, Un-Jae;Oh, Sung-Hoon;Bae, Song-Hwan
    • Preventive Nutrition and Food Science
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    • v.11 no.3
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    • pp.204-209
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    • 2006
  • This study demonstrates that red yeast rice exhibits radical scavenging and antihypercholesterolemic activities in rats fed cholesterol. Sprague-Dawley male rats were divided to five dietary groups (normal, chol-control; and M-1, M-2 & M-3 administered 150, 300, and 500 mg/kg red yeast rice, respectively) and fed their respective diets for 4 weeks. No significant differences in food efficiency ratio (FER) were found among the five groups. The weight of perirenal fat pads decreased with increasing amounts of red yeast rice supplementation. There was a significant decrease in the levels of cholesterol in M-3 group fed red yeast rice with 500 mg/kg compared to those in the chol-control, M-1 and M-2 groups (p<0.05). Among the rats fed the cholesterol-enriched diet, all groups fed red yeast rice showed higher concentration of the HDL cholesterol, but lower concentration of the LDL cholesterol than those of the chol-control group. The scavenging activity of the methanol extract from red yeast rice was increased with increasing amounts of the extract. The glutathione content in the normal group and in the M-3 group were higher than that in the other groups. The M-3 group showed similar hepatic glutathione contents to those of the normal group. These results suggest that red yeast rice may be safe and effective for lowering serum levels of total and LDL-cholesterol, ratio of non-HDL/HDL, and severity of experimental atherosclerosis.

Antinociceptive, Antiinflammtory and Antihypercholesterolemic Effects of Androstane and Cholestane Derivatives (Androstane과 Cholestane 유도체의 진통, 소염 및 항고지혈 효과)

  • Kim, Hak-Soon;Ma, Eun-Sook
    • YAKHAK HOEJI
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    • v.51 no.6
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    • pp.495-499
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    • 2007
  • Seven epoxy- and hydroxyandrostane derivatives ($DH-1{\sim}DH-7$) and nine epoxy- and hydroxycholestane derivatives ($CH-1{\sim}CH-9$) with unsaturation in ring A and ring B were synthesized from DHEA and cholesterol, respectively. The antinociceptive effects of all synthesized compounds were measured by hot plate method. Most of androstane derivatives except $1{\alpha},2{\alpha}$-epoxy-4,6-androstadiene-3,17-dione (DH-3), and CH-6, CH-7 and CH-9 exhibited antinociceptive effect. 1,4-Androstadiene-$3{\beta},17{\beta}$-diol (DH-5, 100 mg/kg, $35.8{\pm}7.39$), $6{\alpha},7{\alpha}$-epoxy-1,4-androstadiene-3,17-dione (DH-4, 100 mg/kg, $32.6{\pm}5.50$) and $5{\alpha},6{\alpha}$-epoxy-17-oxo-androstan-$3{\beta}$-ol (DH-1, 100 mg/kg, $32.5{\pm}2.98$) were more effective than morphine (10 mg/kg, $30.6{\pm}0.5$). The analgesic effects of androstane derivatives on acetic acid writhing in mice were lower than aspirin. The androstane derivatives were less effective than ibuprofen at inhibiting effects on the carrageenin induced paw oedema. 4,6-Cholestadien-$3{\beta}$-ol (CH-5), $1{\alpha},2{\alpha}$-epoxy-4,6-cholestadien-$3{\beta}$-ol (CH-7) and $7{\alpha}$-hydroxy4-cholesten-3-one (CH-9) showed the decrease of serum triglyceride and total cholesterol levels in poloxamer P-407 injected rat.

Alleviation of diabetic complications by ginsenoside Rg3-enriched red ginseng extract in western diet-fed LDL-/- mice

  • Saba, Evelyn;Kim, Seung-Hyung;Kim, Sung-Dae;Park, Sang-Joon;Kwak, Dongmi;Oh, Jun-Hwan;Park, Chae-Kyu;Rhee, Man Hee
    • Journal of Ginseng Research
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    • v.42 no.3
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    • pp.352-355
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    • 2018
  • In this study, we precisely showed how the Rg3-enriched red ginseng extract (Rg3-RGE) lowers glucose, triglyceride, and low-density lipoprotein (LDL) levels in $LDL^{-/-}$ mice. Aspartate aminotransferase/serum glutamic-oxaloacetic transaminase), alanine aminotransferase /serum glutamate-pyruvate transaminase, and steatohepatitis were found to be reduced, and atheroma formation was inhibited by Rg3-enriched red ginseng extract.

Studies on the Antihypercholesterolemic Effects of Gamigwaruhaebaekwhanggum - Tang (가미과루해백황금탕의 항고지혈증 효과)

  • 정은아;김윤경;김남재;김동현;이상인
    • Biomolecules & Therapeutics
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    • v.9 no.2
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    • pp.104-111
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    • 2001
  • Gamigwaruhaebaekwhanggum-Tang (GGHWT) have been evaluated for antihyperlipidemic effects on experimental hyperlipidemic rats and mice induced by Triton WR-1339, com oil and high cholersterol-diet. Especially, GGHWT is formulated with Trichosanthis Fructus, Pinelliae Tuber, Aurantii Immaturus Fructus, Magnoliae Cortex, Allii Macrostemi Bulbuls, Cinnamomi Ramulus and Scutellariae Radix. Oral administration of GGHWT at 500 mg/kg/day for 3 days significantly inhibited the increase of serum triglyceride and LDL-cholesterol, liver triglyceride in hyperlipidemic rats induced by Triton WR-1339. And, GGHWT significantly inhibited the increase of serum triglyceride in hyperlipidemic rats induced by corn oil. Also, administration of GGHWT (500 mg/kg, once daily for 1 week, p.o.) prevented the increase of serum total cholesterol, triglyceride, LDL-cholesterol, liver total cholesterol and triglyceride in 1% cholesterol-diet fed mice. These results suggest that GGHWT is effective for the treatment of hyperlipidemia.

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Effect of the Seaweed Porphya yezoensis Extract on Triton WR-1339 Induced Hypercholesterolemia in Mouse (해조류 김 추출물의 Triton WR-1339유발 고콜레스테롤 혈증 감소효과)

  • HONG Yong-Ki;PARK In-Sick;JUNG Yeongha;SONG Sang-H;HONG Sung-Youl
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.31 no.4
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    • pp.508-515
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    • 1998
  • An antihypercholesterolemic effect was observed by intraperitoneal injection of the seaweed Porphya yezoensis extract. Hypercholesterolemia was induced by intraperitoneal injection of Triton WR-1339 (600 $\mu$g/g-body weight) into a mouse. Maximum level of blood cholesterol was reached at 20 hours after Triton injection. By simultaneous injection of the p. yezoensis extract (30 $\mu$g/g-body weight) with the Triton into each right and left sides of the peritoneal cavity, levels of total cholesterol and low density lipoprotein were decreased to $37\%$ and $24\%$ compared to Triton injection only. For histochemical changes, hepatic tissues obtained at 40 hours after injection of the Triton and the p. yezoensis extract were fixed in fromol-calcium solution. Numbers of lipid drops and cholesterol particles decreased in the portal space of the hepatic cytoplasm. This indicates that the accumulation of lipid, including cholesterol, caused by Triton was prevented by the antihypercholesterolemic effect of extract from the seaweed p. yezoensis.

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Screening of Fungal Strains Producing Lovastatin, an Antihypercholesterolemic Agent (콜레스테롤합성저해제 lovastatin을 생산하는 곰팡이 균주의 탐색)

  • Bang, In-Young;Whang, Seung-Whan;Kim, Jung-Wan;Kim, Sang-Yong;Park, Cheon-Seok
    • Korean Journal of Food Science and Technology
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    • v.35 no.3
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    • pp.442-446
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    • 2003
  • Over two hundred fungal strains from Korean soil were tested for the production of cholesterol-lowering agent, lovastatin. Each fungal strain was cultivated in the rapeseedmeal production medium (RPM). After growing for 7 days, the presence of lovastatin in the culture was examined by TLC analysis and HPLC. Nine different fungal strains were determined to produce detectable amounts of lovastatin, among which one fungal strain isolated from barnyard manure of Kanghwa island produced 25.58 mg/L of lovastatin in the production medium. The morphological observation combined with the determination of 18S-rRNA sequence suggested that the selected strain belongs to a member of Aspergillus sp..

Hypocholestrolemic Effect of CJ90002 in Hamsters: A Potent Inhibitor for Squalene Synthase from Paeonia moutan

  • Park, Jong-Koo;Cho, Hi-Jae;Lim, Yoon-Gho;Cho, Youl-Hee;Lee, Chul-Hoon
    • Journal of Microbiology and Biotechnology
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    • v.12 no.2
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    • pp.222-227
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    • 2002
  • Squalene synthase catalyzes the reductive dimerization of two molecules of farnesyl diphosphate to form squalene at the final branch point of the cholesterol biosynthetic pathway. Due to the unique position of this enzyme in the pathway, its inhibitors may have advantages as antihypercholesterolemic agents. Therefore, selective inhibitors of squalene synthase do not prevent the formation of the essential branch products of the isoprene pathway, such as dolichol, coenzyme-Q, and prenylated proteins, as might be expected for inhibitors of enzymes earlier in the pathway; for example, lovastatin and mevalotin. The current study reports that CJ90002, a pentagalloylglucose isolated from Paeonia moutan SIM (Paeoniaceae), which is an important Chinese crude drug used in many traditional prescriptions, was a potent inhibitor of rat microsomal squalene synthase, and also a potent inhibitor of cholesterol biosynthesis in vitro. In addition, the intraperitoneal and oral administration of CJ90002 had a significant lowering effect on plasma cholesterol levels in hamsters.