• Journal of Life Science
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• v.25 no.1
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• pp.93-100
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• 2015

Pachymic acid (PA) is a lanostane-type triterpenoid derived from the Poria cocos mushroom. Several beneficial biological features of PA provide medicine with a wide variety of valuable effects, such as anticancer and anti-inflammatory activity; it also has antioxidant effects against oxidative stress. Nonetheless, the biological properties and mechanisms that produce this anti-cancer action of PA remain largely undetermined. In this study, we investigated the pro-apoptotic effects of PA in T24 human bladder cancer cells. It was found that PA could inhibit the cell growth of T24 cells in a dose-dependent manner, which was associated with the induction of apoptotic cell death, as evidenced by the formation of apoptotic bodies and chromatin condensation and accumulation of cells in the sub-G1 phase. The induction of apoptotic cell death by PA was connected with an up-regulation of pro-apoptotic Bax and Bad protein expression and down-regulation of anti-apoptotic Bcl-2 and Bcl-xL proteins, and inhibition of apoptosis family proteins. In addition, apoptosis-inducing concentrations of PA induced the activation of caspase-9, an initiator caspase of the mitochondrial-mediated intrinsic pathway, and caspase-3, accompanied by proteolytic degradation of poly (ADP-ribose)-polymerase. PA also induced apoptosis via a death receptor-mediated extrinsic pathway by caspase-8 activation, resulting in the truncation of Bid and suggesting the existence of cross-talk between the extrinsic and intrinsic pathways. Taken together, the present results suggest that PA may be a potential chemotherapeutic agent for the control of human bladder cancer cells.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.5
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• pp.1877-1880
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• 2012

Breast cancer metastasis is the most common cause of cancer-related death in women. Thus, seeking targets of breast tumor cells is an attractive goal towards improving clinical treatment. The present study showed that CCL18 from tumor-associated macrophages could promote breast cancer metastasis via PITPNM3. In addition, we found that pachymic acid (PA) could dose-dependently inhibit migration and invasion of MDA-MB-231cells, with or without rCCL18 stimulation. Furthermore, evidence was obtained that PA could suppress the phosphorylation of PITPNM3 and the combination of CCL18 and PITPNM3. Therefore, we speculate that PA could inhibit breast cancer metastasis via PITPNM3.

• Korean Journal of Pharmacognosy
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• v.48 no.4
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• pp.320-328
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• 2017

Yongdamsagan-tang has been used to treat the urinary disorders, acute- and chronic-urethritis, and cystitis in Korea. In this study, an ultra-performance liquid chromatography-electrospray ionization-mass spectrometry (UPLC-ESI-MS/MS) method was established for simultaneous analysis of the 20 bioactive marker compounds, geniposidic acid, chlorogenic acid, geniposide, liquiritin apioside, acteoside, calceolarioside B, liquiritin, nodakenin, baicalin, liquiritigenin, wogonoside, baicalein, glycyrrhizin, wogonin, glycyrrhizin, wogonin, saikosaponin A, decursin, decursinol angelate, alisol B, alisol B acetate, and pachymic acid in traditional herbal formula, Yongdamsagan-tang. Chromatographic separations of all marker compounds were conducted using a Waters Acquity UPLC BEH $C_{18}$ analytical column ($2.1{\times}100mm$, $1.7{\mu}m$) at $45^{\circ}C$ using a mobile phase of 0.1% (v/v) formic acid in water and acetonitrile with gradient elution. The MS analysis was performed using a Waters ACQUITY TQD LC-MS/MS coupled with an electrospray ionization source in the positive and negative modes. The flow rate was 0.3 mL/min and injection volume was $2.0{\mu}L$. The correlation coefficient of 20 marker compounds in the test ranges was 0.9943-1.0000. The limits of detection and quantification values of the all marker components were 0.11-6.66 and 0.34-19.99 ng/mL, respectively. As a result of the analysis using the optimized LC-ESI-MS/MS method, three compounds, geniposidic acid (from Plantaginis Semen), alisol B (from Alismatis Rhizoma), and pachymic acid (from Poria Sclerotium), were not detected in this sample. While the amounts of the 17 compounds except for the geniposidic acid, alisol B, and pachymic acid were $0.04-548.13{\mu}g/g$ in Yongdamsagan-tang sample. Among these compounds, baicalin, bioactive marker compound of Scutellariae Radix, was detected at the highest amount as a $548.13{\mu}g/g$.

• Korean Journal of Pharmacognosy
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• v.36 no.3 s.142
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• pp.177-185
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• 2005

For the purpose of the quality control of Poria cocos, three major compounds were isolated and identified as pachymic acid (1), $3{\beta}-hydroxylanosta-7,9(11),24-trien-21-oic$ acid (2), and dehydroeburicoic acid (3). The optimal extraction conditions for the quantification of pachymic acid its analogues were the 3 hours of reflux with 15g of P. cocos in 100ml 95% ethanol. HPLC conditions were as follows: Column; ZORBAX Eclipse XDB C18 $(4.6{\times}250\;mm,\;Agillent)$, mobile phase; 1% HOAc in 70% $MeOH{\rightarrow}1%$ HOAc in 100% MeOH for 25 min, then 1% HOAc in 100% MeOH for 15 min, detector, ELSD, flow rate; 1ml/min. The mean contents of 1,2, and 3 in Poria cocos cultivated at 18 different site were $0.65{\pm}0.19,\;0.88{\pm}0.72,\;and\;0.84{\pm}0.54\;mg/g$, respectively, and values might be the guide line for the quality control of P. cocos.

• Biomolecules & Therapeutics
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• v.22 no.4
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• pp.314-320
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• 2014

This study was investigated to know whether pachymic acid (PA), one of the predominant triterpenoids in Poria cocos (Hoelen) has the sedative-hypnotic effects, and underlying mechanisms are mediated via ${\gamma}$-aminobutyric acid (GABA)-ergic systems. Oral administration of PA markedly suppressed locomotion activity in mice. This compound also prolonged sleeping time, and reduced sleep latency showing synergic effects with muscimol (0.2 mg/kg) in shortening sleep onset and enhancing sleep time induced by pentobarbital, both at the hypnotic (40 mg/kg) and sub-hypnotic (28 mg/kg) doses. Additionally, PA elevated intracellular chloride levels in hypothalamic primary cultured neuronal cells of rats. Moreover, Western blotting quantitative results showed that PA increased the amount of protein level expression of $GAD_{65/67}$ over a broader range of doses. PA increased ${\alpha}$- and ${\beta}$-subunits protein levels, but decreased ${\gamma}$-subunit protein levels in $GABA_A$ receptors. The present experiment provides evidence for the hypnotic effects as PA enhanced pentobarbital-induced sleeping behaviors via $GABA_A$-ergic mechanisms in rodents. Taken together, it is proposed that PA may be useful for the treatment of sleep disturbed subjects with insomnia.

• Journal of Mushroom
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• v.20 no.4
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• pp.187-192
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• 2022

Wolfiporia cocos is an edible fungus commercially cultivated in Asia. To investigate metabolic changes of W. cocos mycelia under both light and dark culture conditions, gas chromatography mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC) analyses were performed. In terms of the total amount of sugars, alcohols, amino acids, organic acids, fatty acids, and purines, there no significant differences between the W. cocos mycelia cultivated under light (L) or dark (D) conditions (p < 0.05). However, there were some differences with respect to the production of particular sugars and proteins. The levels of trehalose (L: 17.2 ± 0.3% vs. D: 13.9 ± 1.6%), maltose (L: 0.9 ± 0.1% vs. D: 0.3 ± 0.1%), turanose (L: 0.7 ± 0.2% vs. D: 0.1 ± 0.1%), glutamine (L: 1.6 ± 0.3% vs. D: 0.7 ± 0.2%), and proline (L: 0.3 ± 0% vs. D: 0.1 ± 0%) were all significantly higher under light condition (p < 0.05). In contrast, the levels of galactose (L: 13.7 ± 1.2% vs. D: 17.6 ± 2.0%), aspartic acid (L: 0.6 ± 0.1 % vs. D: 0.9 ± 0.1%), cystathionine (L: 0.6 ± 0.1% vs. D: 0.8 ± 0 %), and malic acid (L: 0.7 ± 0.1% vs. D: 1.2 ± 0.1%) were higher under the dark condition. It is worth noting that the amount of pachymic acid, a pharmaceutically active compound of W. cocos, was 1.68 times greater under the light condition (p < 0.05).

• Archives of Pharmacal Research
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• v.27 no.8
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• pp.829-833
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• 2004

The bioactivity-guided fractionation of the methylene chloride extract of the sclerotium of Poria cocos led to the isolation of (S)-(＋)-turmerone (1), ergosterol peroxide (2), polyporenic acid C (3), dehydropachymic acid (4), pachymic acid (5), and tumulosic acid (6). Compounds 4-6 exhibited moderate cytotoxicities, with $IC_{50}$ values of 20.5, 29.1, and $10.4{\;}\mu\textrm{m}$, respectively, against a human colon carcinoma cell line. However, 3-6 not only showed inhibitory activities as potent as etoposide used as a positive control on DNA topoisomerase II (36.1, 36.2, 43.9 and 66.7％ inhibition at a concentration of $20{\;}\mu\textrm{m}$, respectively), but also inhibition of DNA topoisomerase I (55.8, 60.7, 43.5, and 83.3％ inhibition at a concentration of $100{\;}\mu\textrm{m}$, respec-tively).

• Natural Product Sciences
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• v.23 no.2
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• pp.84-91
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• 2017

This study proposes a sensitive and selective liquid chromatography-electrospray ionization tandem mass spectrometry method of efficiently assessing the quality of a traditional herbal medicine called Yeonggyechulgam-tang (YGCGT). The following compounds 1 - 11, namely, liquiritin apioside (1), liquiritin (2), liquiritigene (3), coumarin (4), cinnamic acid (5), cinnamaldehyde (6), glycyrrhizin (7), atractylenolide III (8), atractylenolide II (9), atractylenolide I (10), and pachymic acid (11) were separated on a UPLC BEH $C_{18}$ column ($2.1{\times}100mm$, $1.7{\mu}m$) at a column temperature of $45^{\circ}C$ eluted with a gradient condition of 0.1% (v/v) formic acid in distilled water and acetonitrile. The correlation coefficient of the calibration curve of the eleven constituents was ${\geq}0.9936$. The limits of detection and quantification of the compounds 1 - 11 were 0.06 - 4.73 ng/mL and 0.17-14.20 ng/mL, respectively. Using this analytical method, the compound 11 in lyophilized YGCGT decoction extract was not detected, while the compounds 1 - 10 were detected 0.13-166.43 mg/g.

• Journal of the Korean Society of Food Science and Nutrition
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• v.27 no.6
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• pp.1034-1040
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• 1998

The nutritional quality and physiological activity of cultivated hoelen from 13 months to 24 months were examined to compare with natural hoelen. General compositions of hoelen were as follows re spectively; crude protein 1.80~2.50%, crude fat 0.68~1.23%, crude ash 0.12~0.43%, crude fiber 6.30~7.14%, nitrogen free extract 89.25~90.44%. The major free sugar was glucose, and the content of 13 months cultivated hoelen was higher than any other cultivated hoelen. The major fatty acids of hoelen were linoleic acid, palmitic acid, stearic acid and oleic acid. The ratio of unsaturated fatty acids was 62.62~77.96% and the content was higher in cultivated hoelen than in natural hoelen. The contents of amino acid were high in the order of tyrosine, aspartic acid, glutamic acid and serine, and increased as the day of cultivation became longer. The contents of mineral components were higher in the order of Ca, K, Mg and the contents of Na and Ca were higher in natural hoelen than in cultivated hoelen. The contents of pachymic acid and dehydropachymic acid was similar in the natural and cultivated hoelen. On the results of antimicrobial test the ethanol extract showed a stronger effect than water extract, and had an excellent antimicrobial activity on Micrococcus luteus and Escherichia coli. The ethanol extract of hoelen showed comparatively strong electron donating ability. The ethanol extract of hoelen showed a high inhibition activity on the growth of lung cancer, ovary cancer, skin cancer, central nerve cancer and rectum cancer, especially the activity of 19 months cultivated hoelen was the highest. On the above results of nutritional quality and physiological activity of hoelen, it is supposed that the picking date of cultivated hoelen was suitable over than 19 months.

• Journal of Korean Society of Forest Science
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• v.113 no.1
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• pp.73-87
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• 2024

Wolfiporia hoelen (Fr.) Y.C.Dai & V. Papp, commonly known as Poria cocos, is a significant traditional herb used for medicinal and culinary purposes Asian and European countries. Many studies have confirmed that the main components of W. hoelen have pharmacological activities and thatits extract has been shown to affect bone metabolism. This study aimed to the potential of a 50% ethanol extract of the sclerotium of W. hoelen for preventing and treating bone diseases. The ethanol extract was systematically fractionated using n-hexane, dichloromethane, and ethyl acetate. The dichloromethane fraction caused an approximately 29% increase in alkaline phosphatase (ALP) differentiation activity in C2C12 cells compared to the control. Four compounds isolated from this active dichloromethane fraction were identified through instrumental analysis and literature references as 3α-dehydrotrametenolic acid, ergosterol, pachymic acid, and dehydrotumulosic acid. All four compounds were evaluated at increasing concentrations (1, 3, 10, 30, and 100 μM) to determine their effects on ALP differentiation activity in C2C12 cells and RANKL-induced inhibition activity in bone marrow macrophages (BMMs), with a concurrent assessment of cytotoxicity at these concentrations. At a concentration of 3 μM, dehydrotumulosic acid caused a 160% increase in ALP activity, 24% higher than in the BMP-2 control. BMMs treated with dehydrotumulosic acid at concentrations between 10 and 100 μM showed a substantial 15-86% decrease in RANKL-induced inhibition activity compared to the control, with distinct patterns of RANKL inhibition and cytotoxicity observed at 10 μM. These findings suggest that the ethanol extract from the sclerotium of W. hoelen has potential to modulate bone-cell differentiation, while highlighting the possible benefits of dehydrotumulosic acid isolated from the dichloromethane fraction of W. hoelen for preventing and treating osteoporosis.