Anti-androgenic activities of the triterpenoids fraction of Ganoderma lucidum

Liu, Jie; Shimizu, Kuniyoshi; Konishi, Fumiko; Noda, Kiyoshi; Kumamoto, Shoichiro; Kurashiki, Kenji; Kondo, Ryuichiro

doi:10.1016/j.foodchem.2006.01.003

Cited by 63 publications

(31 citation statements)

References 28 publications

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“…17,18,22) However, the use of radiolabeled compounds is inconvenient for routine assays. In addition, it is necessary to separate testosterone and radiolabeled DHT using HPLC or TLC.…”

Section: Effects Onmentioning

confidence: 99%

“…Thus, we developed a method that utilizes electrospray ionization (ESI)-LC/MS without radiolabeled testosterone by modifying Liu's method. 17,18) 5a-Reductase activity was evaluated by measuring the ratio of DHT area to internal standard area. Figure 2 shows selected ion chromatograms of DHT and dexamethasone as an internal standard.…”

Section: Effects Onmentioning

confidence: 99%

“…Protein concentrations were measured by the method of Lowry et al 16) Microsomal Preparation, 5a a-Reductase Activity, and LC/MS Analysis The liver microsomes of rats were prepared as reported by Liu et al with some modifications. 17,18) The liver was removed from female rats and homogenized in 4 volumes of medium A (0.32 M sucrose, 1 mM dithiothreitol, and 20 mM sodium phosphate, pH 6.5). The homogenate was then centrifuged at 10000ϫg for 10 min.…”

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confidence: 99%

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Pharmacologically Relevant Receptor Binding Characteristics and 5.ALPHA.-Reductase Inhibitory Activity of Free Fatty Acids Contained in Saw Palmetto Extract

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Oyunzul

et al. 2009

Biological & Pharmaceutical Bulletin

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Benign prostatic hyperplasia (BPH) and related lower urinary tract symptoms (LUTS) are common disorders in aging men. Plant extracts are widely used in the treatment of BPH and related LUTS. In fact, phytotherapeutic agents, including saw palmetto extract (SPE), are very popular in many European countries as herbal remedies, representing up to 80% of all drugs prescribed for these disorders.1,2) An analysis of many clinical trials showed mild to moderate improvements in symptom scores and urinary flow in patients with BPH.3)The most widely known effect of SPE is the inhibition of type 1 and 2 isozymes of 5a-reductase. 4,5) Other pharmacodynamic mechanisms of SPE have also been proposed, including anti-androgenic effects, anti-proliferative effects and anti-inflammatory effects. [6][7][8] Our recent study has shown that the intraduodenal administration of SPE in the rat cystometry resulted in a significant and dose-related increase in micturition interval as well as a decrease in micturition volume and bladder capacity caused by the infusion of 0.1% acetic acid.9) Furthermore, we have reported that SPE inhibited the specific binding of radioligands to a 1 -adrenergic, muscarinic and 1,4-dihydropyridine (1,4-DHP) calcium channel antagonist receptors in the lower urinary tract of rats.9-11) However, the exact active constituents of SPE remain to be identified. SPE contains mainly saturated and unsaturated fatty acids (90%). Among these fatty acids, the major constituents are oleic acid and lauric acid, which together compose more than 50% of SPE.12) The aim of this study is to investigate binding activities for pharmacologically relevant (a 1 -adrenergic, muscarinic, 1,4-DHP calcium channel antagonist) receptors of major fatty acids contained in SPE. In addition, with a newly developed method using LC/MS, the effects of SPE and its fatty acids on 5a-reductase activity in the rat liver were also examined. MATERIALS AND METHODSMaterials SPE (Serenoa repens purified extract) was kindly provided by Indena Japan (Tokyo, Japan). SPE was obtained with hypercritical CO 2 (SABAL SELECT, Indena S.p.A., Milan, Italy). The constituents contained in SPE are presented elsewhere.12) Oleic acid, lauric acid, myristic acid, palmitic acid and linoleic acid were purchased from Tokyo Chemical Industry (Tokyo, Japan), Nacalai Tesque (Kyoto, Japan), Sigma-Aldrich (St. Louis, MO, U.S.A.) and Wako Pure Chemicals (Osaka, Japan), respectively. [ Animals Male and female Sprague-Dawley rats at 8-10 weeks of age (Japan SLC Inc., Shizuoka, Japan) were housed in the laboratory with free access to a normal diet (CE-2, CREA Japan Inc., Tokyo, Japan) and water, and maintained on a 12-h light-dark cycle in a room with controlled temperature and humidity. The study was conducted in accordance with the guidelines of the Experimental Ani- to bind a a 1 -adrenergic, muscarinic and 1,4-dihydropyridine (1,4-DHP The results suggest that lauric acid and oleic acid bind noncompetitively to a a 1 -adrenergic, muscarinic and 1,4-DHP calcium channel antagonist...

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“…17,18,22) However, the use of radiolabeled compounds is inconvenient for routine assays. In addition, it is necessary to separate testosterone and radiolabeled DHT using HPLC or TLC.…”

Section: Effects Onmentioning

confidence: 99%

Section: Effects Onmentioning

confidence: 99%

mentioning

confidence: 99%

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Pharmacologically Relevant Receptor Binding Characteristics and 5.ALPHA.-Reductase Inhibitory Activity of Free Fatty Acids Contained in Saw Palmetto Extract

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Oyunzul

et al. 2009

Biological & Pharmaceutical Bulletin

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“…Over 130 triterpenoids have been isolated from the fruiting bodies, cultured mycelia, and spores during the past two decades [8,9]. Some of the triterpenoids showed antiandrogenic [10], antihepatitis B [11], antioxidant [12,17], antitumor [13,15], anticomplement [14], antimicrobial [16], anti-HIV-1 [18], selectively inhibit eukaryotic DNA polymerase [19], and angiotensin converting enzyme-inhibitory activities [20]. Thus, a valuable and convincing method for characterization of triterpenoids of G. lucidum is necessary for quality control of the herbal medicine.…”

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confidence: 99%

Analysis of triterpenoids in Ganoderma lucidum using liquid chromatography coupled with electrospray ionization mass spectrometry

Yang

Wang

Guan

et al. 2007

J. Am. Soc. Mass Spectrom.

132

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Triterpenoids extracted from Ganoderma lucidum (Leyss. ex Fr.) Karst were separated and characterized using optimized reversed-phase liquid chromatography with diode array detection and electrospray ion trap tandem mass spectrometry (HPLC-DAD-ESI-MS n ). They could be classified into five types depending on the fragmentation behavior. second alcohol at C-15 were oxidized to ketone, the prominent cleavage would occur at C-ring and produce a group of ions of a; if C-7 were oxidized to ketone, transference of two hydrogen atoms would occur during the cleavage of rings and a list of ions about a ϩ 2 and/or b ϩ 2 would appear instead. The above fragmentations and regularities in fragmentation pathways were reported for the first time, and were implemented for the analysis of triterpenoids in G. lucidum. The chloroform extract was separated on a Zorbax SB-C 18 column, eluting with an acetonitrile-0.2% acetic acid gradient. A total of 32 triterpenoids, including six new ones, were identified or tentatively characterized based on the tandem mass spectra of the HPLC peaks. (J Am Soc Mass Spectrom 2007, 18, 927-939)

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“…[6À11] Liu et al [8] reported that the triterpenoid fraction of G. lucidum might be beneficial for curing benign prostatic hyperplasia. The experiments of Fatmawatia et al [11] indicated that triterpenoid isolated from the fruiting body of G. lucidum was found to inhibit a-glucosidase in vitro.…”

Section: Introductionmentioning

confidence: 99%

Improvement of polysaccharide and triterpenoid production ofGanoderma lucidumthrough mutagenesis of protoplasts

Ren

Zou

et al. 2016

Biotechnology & Biotechnological Equipment

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Ganoderma lucidum is a traditional medicinal macrofungus in China, which has two kinds of key bioactive compounds -polysaccharides and triterpenoids. To improve the polysaccharide and triterpenoid production from G. lucidum, the preparation and regeneration conditions of protoplasts were optimized. This was done by systematic trials with various parameters, and protoplast mutation was subsequently performed. A mycelium that was cultivated for seven days and treated with 0.33 mL of 1% snailase and 0.66 mL of 0.5% cellulase solution for 2.5 h at 30 C in the presence of osmotic pressure stabilizer mannitol (0.5 mol/L), had the best conditions, in which the resultant protoplasts were 6.40 £ 10 5 /mL and the regeneration rate was 6.25%. The resultant protoplasts were subjected to subsequent mutation by lithium chloride or by the combination of lithium chloride and Triton X-100. The highest yields of intracellular polysaccharide and triterpenoid in two mutant strains were 37.50 and 40.81 mg/g, which were increased with 568.45% and 373.43%, respectively, as compared to the original strain. Furthermore, the yields of intracellular polysaccharides and triterpenoids in the second generation and the third generation of the mutants were comparable to that of the first generation, which showed genetic stability of the mutants for the production of polysaccharides and triterpenoids.

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Anti-androgenic activities of the triterpenoids fraction of Ganoderma lucidum

Cited by 63 publications

References 28 publications

Pharmacologically Relevant Receptor Binding Characteristics and 5.ALPHA.-Reductase Inhibitory Activity of Free Fatty Acids Contained in Saw Palmetto Extract

Pharmacologically Relevant Receptor Binding Characteristics and 5.ALPHA.-Reductase Inhibitory Activity of Free Fatty Acids Contained in Saw Palmetto Extract

Analysis of triterpenoids in Ganoderma lucidum using liquid chromatography coupled with electrospray ionization mass spectrometry

Improvement of polysaccharide and triterpenoid production ofGanoderma lucidumthrough mutagenesis of protoplasts

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