Sri Fatmawati

Ganoderol B: A potent α-glucosidase inhibitor isolated from the fruiting body of Ganoderma lucidum

α-Glucosidase inhibitor has considerable potential as a diabetes mellitus type 2 drug because it prevents the digestion of carbohydrates. The search for the constituents reducing α-glucosidase activity led to the finding of active compounds in the fruiting body of Ganoderma lucidum. The CHCl(3) extract of the fruiting body of G. lucidum was found to show inhibitory activity on α-glucosidase in vitro. The neutral fraction, with an IC(50) of 88.7 μg/ml, had stronger inhibition than a positive control, acarbose, with an IC(50) of 336.7 μg/ml (521.5 μM). The neutral fraction was subjected to silica gel column chromatography and repeated p-HPLC to provide an active compound, (3β,24E)-lanosta-7,9(11),24-trien-3,26-diol (ganoderol B). It was found to have high α-glucosidase inhibition, with an IC(50) of 48.5 μg/ml (119.8 μM).

Ganoderic acid Df, a new triterpenoid with aldose reductase inhibitory activity from the fruiting body of Ganoderma lucidum

Ganoderic acid Df, a new lanostane-type triterpenoid, was isolated from the fruiting body of Ganoderma lucidum. Its structure was characterized as 7β, 11β-dihydroxy-3, 15, 23-trioxo-5α-lanosta-8-en-26-oic acid by 1D- and 2D-NMR spectra. This compound exhibited potent human aldose reductase inhibitory activity, with an IC(50) of 22.8 μM in vitro. A carboxyl group of this compounds side chain is essential for eliciting inhibitory activity because its methyl ester is much less active.

Structure-activity relationships of lanostane-type triterpenoids from Ganoderma lingzhi as α-glucosidase inhibitors

A series of lanostane-type triterpenoids, identified as ganoderma alcohols and ganoderma acids, were isolated from the fruiting body of Ganoderma lingzhi. Some of these compounds were confirmed as active inhibitors of the in vitro human recombinant aldose reductase. This paper aims to explain the structural requirement for α-glucosidase inhibition. Our structure-activity studies of ganoderma alcohols showed that the OH substituent at C-3 and the double-bond moiety at C-24 and C-25 are necessary to increase α-glucosidase inhibitory activity. The structure-activity relationships of ganoderma acids revealed that the OH substituent at C-11 is an important feature and that the carboxylic group in the side chain is essential for the recognition of α-glucosidase inhibitory activity. Moreover, the double-bond moiety at C-20 and C-22 in the side chain and the OH substituent at C-3 of ganoderma acids improve α-glucosidase inhibitory activity. These results provide an approach with which to consider the structural requirements of lanostane-type triterpenoids from G. lingzhi. An understanding of these requirements is considered necessary in order to improve a new type of α-glucosidase inhibitor.

The inhibitory effect on aldose reductase by an extract of Ganoderma lucidum.

The human aldose reductase inhibitory effects of the methanol extracts of 17 medicinal and edible mushrooms were examined. Ganoderma lucidum showed the highest aldose reductase inhibitory activity compared with the other mushrooms. The effect of an ethanol extract of G. lucidum on the galactitol level in the eye lens was studied in a galactosemic rat model in vivo. This mushroom significantly decreased the galactitol accumulation. Copyright

Structure-activity relationships of ganoderma acids from Ganoderma lucidum as aldose reductase inhibitors

A series of lanostane-type triterpenoids, known as ganoderma acids were isolated from the fruiting body of Ganoderma lucidum. Some of these compounds were identified as active inhibitors of the in vitro human recombinant aldose reductase. To clarify the structural requirement for inhibition, some structure-activity relationships were determined. Our structure-activity studies of ganoderma acids revealed that the OH substituent at C-11 is an important feature and the carboxylic group in the side chain is essential for the recognition of aldose reductase inhibitory activity. Moreover, double bond moiety at C-20 and C-22 in the side chain contributes to improving aldose reductase inhibitory activity. In the case of ganoderic acid C2, all of OH substituent at C-3, C-7 and C-15 is important for potent aldose reductase inhibition. These results provide an approach to understanding the structural requirements of ganoderma acids from G. lucidum for aldose reductase inhibitor. This understanding is necessary to design a new-type of aldose reductase inhibitor.

Inhibition of Aldose Reductase In Vitro by Constituents of Ganoderma lucidum

CHCl(3) extract of the fruiting body of Ganoderma lucidum was found to show inhibitory activity on human aldose reductase in vitro. From the acidic fraction, potent human aldose reductase inhibitors, ganoderic acid C2 (1) and ganoderenic acid A (2), were isolated together with three related compounds. It was found that the free carboxyl group of ganoderic acid C2 and ganoderenic acid A is essential in eliciting the inhibitory activity considering the much lower activity of their methyl esters.

20(S)-Ginsenoside Rh2 as aldose reductase inhibitor from Panax ginseng.

The root of Panax ginseng C. A. Meyer (Araliaceae) is a well-known herbal medicine in East Asia. The major bioactive metabolites in this root are commonly identified as ginsenosides. A series of ginsenosides were determined for in vitro human recombinant aldose reductase. This Letter aims to clarify the structural requirement for aldose reductase inhibition. We discovered that only ginsenoside 20(S)-Rh2 showed potent against aldose reductase, with an IC50 of 147.3 μM. These results implied that the stereochemistry of the hydroxyl group at C-20 may play an important role in aldose reductase inhibition. An understanding of these requirements is considered necessary in order to develop a new type of aldose reductase inhibitor. Furthermore, P. ginseng might be an important herbal medicine in preventing diabetic complications.

The inhibitory activity of aldose reductase in vitro by constituents of Garcinia mangostana Linn

We investigated aldose reductase inhibition of Garcinia mangostana Linn. from Indonesia. Dichloromethane extract of the root bark of this tree was found to demonstrate an IC50 value of 11.98 µg/ml for human aldose reductase in vitro. From the dichloromethane fraction, prenylated xanthones were isolated as potent human aldose reductase inhibitors. We discovered 3-isomangostin to be most potent against aldose reductase, with an IC50 of 3.48 µM.

Cylindroxanthones A-C, three new xanthones and their cytotoxicity from the stem bark of Garcinia cylindrocarpa.

Three new xanthones, cylindroxanthones A-C (1-3), were isolated from the stem bark of Garcinia cylindrocarpa. The structures were established on the basis of spectroscopic analysis. The molecular structure of 1 was unequivocally confirmed by single-crystal X-ray diffraction analysis. These three xanthones were evaluated regarding their cytotoxicity against KB, HeLa S-3, HT-29, MCF-7, and Hep G2 cancer cell lines. Compound 1 exhibited good cytotoxicity against KB cell with IC50 value of 2.36 μM.

Thymoquinone: A novel strategy to combat cancer: A review

The higher consumption of fruit, herbs, spices, and vegetables is well known and practical strategy to cure human cancers owing to their presence of bioactive compounds. Among these, Nigella sativa is a promising source of bioactive compounds including thymoquinone, monoterpenes, p-cymene and α-piene etc. Thymoquinone has been found effective to inhibit the different cancer stages such as proliferation, migration and invasion. It also acts as anticancer agent against different human cancers such as breast, pancreatic, prostate, blood, oral, bone, head and neck, cervical, liver and lung. It significantly mediated miR-34a up-regulation, enhanced the levels of miR-34a through p53, and down controlled Rac1 expression. Thymoquinone induces apoptosis, regulates the levels of pro- and anti- apoptotic genes. It also has been known to lower the phosphorylation of NF-κB and IKKα/β and reduces the metastasis as well as also lowered the ERK1/2 and PI3K activities. Thymoquinone inhibits the metastasis through activation of JNK and p38. The present review article highlights the anticancer perspectives of thymoquinone in human by various pathways and use of this compound as diet based therapy has proven new pharmacological agent against several types of cancers.