Eight previously undescribed lanostane triterpenoids, including five nortriterpenoids with 26 carbons, ganothenoids A-E (1-5), and three lanostanoids, ganothenoids F-H (6-8), along with 24 known ones (9-32), were isolated from the fruiting bodies of Ganodrma theaecolum. The structures of the novel compounds were elucidated using comprehensive spectroscopic methods, including electronic circular dichroism (ECD) and nuclear magnetic resonance (NMR) calculations. Compounds 1-32 were assessed for their neuroprotective effects against H₂O₂-induced damage in human neuroblastoma SH-SY5Y cells, as well as their inhibitory activities against protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase. Compound 4 demonstrated the most potent neuroprotective activity against H₂O₂-induced oxidative stress by suppressing G₀/G₁ phase cell cycle arrest, reducing reactive oxygen species (ROS) levels, and inhibiting cell apoptosis through modulation of B-cell lymphoma 2 protein (Bcl-2) and Bcl-2 associated X-protein (Bax) protein expression. Compounds 26, 12, and 28 exhibited PTP1B inhibitory activities with IC₅₀ values ranging from 13.92 to 56.94 μmol·L^-1, while compound 12 alone displayed significant inhibitory effects on α-glucosidase with an IC₅₀ value of 43.56 μmol·L^-1. Additionally, enzyme kinetic analyses and molecular docking simulations were conducted for compounds 26 and 12 with PTP1B and α-glucosidase, respectively.
Humans ; Fruiting Bodies, Fungal/chemistry* ; Triterpenes/isolation & purification* ; Neuroprotective Agents/isolation & purification* ; Protein Tyrosine Phosphatase, Non-Receptor Type 1/metabolism* ; Ganoderma/chemistry* ; Apoptosis/drug effects* ; Hypoglycemic Agents/isolation & purification* ; Molecular Structure ; alpha-Glucosidases/metabolism* ; Cell Line, Tumor ; Reactive Oxygen Species/metabolism* ; Oxidative Stress/drug effects* ; Hydrogen Peroxide/toxicity* ; Molecular Docking Simulation

Chemical constituents were isolated from the fruiting bodies of Ganoderma australe by various column chromatographic techniques and HPLC method, and their chemical structures were identified through the combined analysis of physicochemical properties and spectral data. Meanwhile, their α-glucosidase inhibitory activity and anti-oxidative ability were evaluated. Seven compounds were isolated from G. australe and were identified as 6-methoxyl-cyclo-(Phe-Ile)(1), applanoxidic acid A methyl ester(2), ergosta-7,22 E-dien-3β-ol(3), cinnamic acid(4), 5α,8α-epidioxy-(20S,22E,24R)-ergosta-6,22-diene-3β-ol(5), 1-(3, 4-dihydroxyphenyl) ethanone(6), salicylic acid(7) and benzoic acid(8). Among the compounds, compound 1 was a new cyclic dipeptide. Compound 2 was a new lanosta natural product, and compounds 4, 6, 7 and 8 were obtained from G. australe for the first time. Moreover, compounds 4 and 8 exhibited α-glucosidase inhibitory activity with inhibition rates of 36.8% and 34.7%, and compounds 4, 7 and 8 had a certain activity in DPPH free radical scavenging activity with IC_(50) values of 0.168, 0.458 and 0.170 g·L~(-1), respectively. The DPPH radical scavenging rate of compound 1 was 41.1%.
Free Radical Scavengers ; isolation & purification ; Fruiting Bodies, Fungal ; chemistry ; Ganoderma ; chemistry ; Glycoside Hydrolase Inhibitors ; isolation & purification ; Molecular Structure

OBJECTIVETo study the inhibitory effect and mechanism of Ganoderma lipsiense extract (GLE) on the growth of triple-negative breast cancer (TNBC) cell line MDA-MB-231-HM in a mouse model.

METHODSThe mouse model of TNBC was established by subcutaneous injection of 1.5 x 10(6) of MDA-MB-231-HM cells into BALB/c-nu mouse. Twenty successfully modeled mice were divided into the GLE group and the negative control group according to random digit table, 10 in each group. GLE (0.2 mL 100 mg/mL) was peritoneally injected to mice in the GLE group, while equal dose of normal saline was peritoneally injected to mice in the negative control group. The medication was administered once per 3 days and discontinued after 45 days. The CD34 expression was detected using immunohistochemical assay for counting microvessels. Meanwhile, expressions of thrombospondin 1 (TSP-1) and cyclin D1 were detected using immunohistochemical assay.

RESULTSThe average weight was obviously lower in the GLE group than in the negative control group [(0.33 ± 0.16) g vs (0.68 ± 0.37)g, P < 0.05]. The tumor inhibition rate was 51.4% in the GLE group. The volume of transplanted tumor was obviously lesser in the GLE group than in the negative control group (P < 0.05). Results of immunohistochemical staining showed, the microvessel density (MVD) under every field was (20.7 ± 2.1), TSP-1 positive cell count was (66.2 ± 9.2), cyclin D1 positive cell count was (33.8 ± 16.4) in the GLE group, and they were 34.0 ± 2.0, 24.0 ± 6.6, and 168.2 ± 32.6, respectively in the negative control group. There was statistical difference in all indices between the two groups (P < 0.05).

CONCLUSIONGLE could inhibit malignant proliferation of tumor cells by suppressing angiogenesis of blood vessels in tumor tissues and regulating cell cycles, thereby inhibiting TNBC.

Animals ; Biological Products ; pharmacology ; Cell Line, Tumor ; Cyclin D1 ; metabolism ; Disease Models, Animal ; Ganoderma ; chemistry ; Humans ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Microvessels ; Neoplasm Transplantation ; Neovascularization, Pathologic ; prevention & control ; Random Allocation ; Thrombospondin 1 ; metabolism ; Triple Negative Breast Neoplasms ; drug therapy

The objective of this study was to prepare nanostructured lipid carrier (NLC)-based topical gel of Ganoderma Triterpenoids (GTs) and evaluate their effects on frostbite treatment. GT-NLCs was prepared by the high pressure homogenization method and then characterized by morphology and analyses of particle size, zeta potential, entrapment efficiency (EE), and drug loading (DL). The NLCs was suitably gelled for skin permeation studies in vitro and pharmacodynamic evaluation in vivo, compared with the GT emulgel. The GT-NLC remained within the colloidal range and was uniformly dispersed after suitably gelled by carbopol preparation. Transmission electron microscopy (TEM) study showed GT-NLCs was spherical in shape. The EE (%) and DL (%) could reach up to (81.84 ± 0.60)% and (2.13 ± 0.12)%, respectively. The result of X-ray diffractograms (XRD) showed that GTs were in an amorphous state in the NLC-gel. In vitro permeation studies through rat skin indicated that the amount of GTs permeated through skin of GT-NLCs after 24 h was higher than that of GT emulsion, and GT-NLCs increased the accumulative amounts of GTs in epidermis 7.76 times greater than GT emulsion. GT-NLC-gel was found to possess superior therapeutic effect for frostbite, compared with the GT emulgel. The NLC based topical gel of GTs could improve -their therapeutic effect for frostbite.
Animals ; Drug Carriers ; chemistry ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Frostbite ; drug therapy ; Ganoderma ; chemistry ; Gels ; administration & dosage ; chemistry ; Humans ; Lipids ; chemistry ; Male ; Nanostructures ; administration & dosage ; chemistry ; Rats ; Rats, Sprague-Dawley

The chemical investigation on Ganoderma philippii led to the isolation of sixteen compounds by silica gel and Sephadex LH-20 column chromatography. On the basis of spectroscopic data analyses, their structures were elucidated as 2, 5-dihydroxyacetophenone (1), methyl gentisate (2), (S) -dimethyl malate (3), muurola-4, 10 (14) -dien-11beta-ol (4), dihydroepicubenol (5), 5-hydroxymethylfuran carboxaldehyde (6), ergosta-7, 22E-dien-3beta-ol (7), ergosta-7, 22E-dien-3-one (8), ergosta-7, 22E-diene-2beta, 3alpha, 9alpha-triol (9), 6/beta-methoxyergo-sta-7, 22E-dien-3beta, 5alpha-diol (10), ergosta-4, 6, 8(14), 22E-tetraen-3-one (11), ergosta4, 6, 8-(14), 22E-etetraen-3beta-ol (12), 5alpha, 8alpha-epidioxy-ergosta-6, 22E-dien-3beta-ol (13), 7alpha-methoxy-5alpha, 6alpha-epoxyergosta-8-(14), 22E-dien-3beta-ol (14), ergosta-8, 22E-diene-3beta, 5alpha, 6beta, 7alpha-tetraol (15), and ergosta-5, 23-dien-3beta-ol, acetate (16). All the compounds were obtained from this fungus for the first time, and compounds 4 and 5 were isolated from the Ganoderma genus for the first time.
Ganoderma ; chemistry ; Medicine, Chinese Traditional ; Organic Chemicals ; analysis ; isolation & purification

A new terpenoid, lucidone D (1), has been isolated from Ganoderma lucidum. Its structure was determined to be 7beta, 15alpha-dihydroxy-4, 4, 14alpha-trimethyl-3, 11, 20-trioxo-5alpha-pregn-8-en on the basis of 1D and 2D-NMR spectral analysis.
Ganoderma ; chemistry ; Molecular Structure ; Terpenes ; chemistry ; isolation & purification

OBJECTIVETo investigate the effects of glossy ganoderma spore oil on the proliferation, apoptosis, expression of miR-21 and its target genes of human lung adenocarcinoma SPC-A1 cell line, and to explore its possible mechanism.

METHODThe SPC-A1 cells were treated with glossy ganoderma spore oil for 24 and 48 hours. The inhibition growth efficacy was determined using cell count kit (CCK-8). Cell morphological changes were observed by light microscopy. Cell apoptosis was analyzed by flow cytometry. The expression of miR-21, PTEN and PDCD4 were determined by Real-time PCR.

RESULTGlossy ganoderma spore oil concentration-dependently inhibited the SPC-A1 cell's proliferation. When the concentration of glossy ganoderma spore oil attained to 0.2%, the cells' morphology changed obviously. Glossy ganoderma spore oil could induce the apoptosis of SPC-A1 cells at low concentration. Glossy ganoderma spore oil down-regulated the expression of miR-21 and up-regulated the expression of PTEN and PDCD4 significantly.

CONCLUSIONglossy ganoderma spore oil could inhibit the proliferation obviously and cause the changes of cell morphology. Furthermore, glossy ganoderma spore oil induced apoptosis of SPC-A1 cell through down-regulating the expression of miR-21 and up-regulating tumor suppressors.

Adenocarcinoma ; metabolism ; Antineoplastic Agents ; pharmacology ; Apoptosis ; drug effects ; Cell Line, Tumor ; Ganoderma ; chemistry ; Humans ; Lung Neoplasms ; metabolism ; MicroRNAs ; genetics ; Polymerase Chain Reaction ; Spores, Fungal ; chemistry

To study the cultural characteristics of mycelia of Ganoderma gibbosum, a medicinal fungus used in China. The growth rate and biomass of G. gibbosum mycelia were measured under different temperature, lightning carbon and nitrogen sources conditions. It showed that the optimal growth temperature for mycelia was 25 degrees C. Darkness was beneficial for mycelium growth. The initial pH 5.5 was suitable. The sucrose was the best carbon source and yeast extract the best nitrogen source, the optimal carbon-nitrogen ratio 60:2. These conclusions will offer references for further artificial cultivation and liquid fermentation.
Carbon ; metabolism ; China ; Culture Techniques ; Ganoderma ; chemistry ; growth & development ; Light ; Mycelium ; chemistry ; growth & development ; metabolism ; radiation effects ; Nitrogen ; metabolism

OBJECTIVETo investigate the alteration of the adiponectin signal pathway in hypertrophic myocardium of spontaneous hypertensive rats (SHR) and to observe the effects of Gadol (GD) and Ganoderma spores (GS) on the hemodynamic parameters and the adiponectin signal pathway of SHR.

METHODSSHRs, 8 weeks old, were randomly divided into four groups: the untreated group, and the three treated groups treated with GD, GS, and GD + GS respectively by gastrogavage for 4 weeks. Controlled with 8-week-old WKY rats, the hemodynamic parameters in all rats were recorded through the carotid artery intubation; the serum level of adiponectin was determined with ELISA; the mRNA expressions of adiponectin receptors (AdipoRs) and carnitine palmitoyl transferase (CPT-1) were determined by RT-PCR; and the protein expression of adenosine monophosphate activated protein kinase (AMPK), both phosphorylated and un-phosphorylated, was detected by Western blot.

RESULTSCompared with the WKY rats, the systolic blood pressure (SBP), diastolic blood pressure (DBP) and myocardial hypertrophy index (MHI) in SHR were significantly higher; the serum levels of adiponectin and phosphorylated AMPK, mRNA expressions of AdipoR1 and CPT-1 in SHR heart tissue were lower (P < 0.05). Compared with the SHR, medication of GD and GS, either alone or in combination, could reduce SBP, DBP and MHI significantly (P < 0.01, P < 0.05), and elevate the mRNA expression of CPT-1 (P < 0.05) in heart, but levels of adiponectin, AdipoR1 and phosphorylated AMPK could only be raised by combined use of the two (P < 0.05).

CONCLUSIONSAdiponectin signal transduction pathway alteration presents in the myocardium of SHR, which might be one of the molecular mechanisms that cause hypertrophic metabolic abnormality. GD and GS could improve the hemodynamic index in SHR, and enhance the level of adiponectin and the expression of its related signal transduction molecules.

Adiponectin ; metabolism ; physiology ; Animals ; Cardiomyopathy, Hypertrophic ; etiology ; metabolism ; Drugs, Chinese Herbal ; pharmacology ; Ganoderma ; chemistry ; Hemodynamics ; drug effects ; Hypertension ; complications ; Male ; Random Allocation ; Rats ; Rats, Inbred SHR ; Rats, Inbred WKY ; Rhodiola ; chemistry ; Signal Transduction ; drug effects ; Spores

OBJECTIVETo investigate the changes of serum inteferon-gamma (IFN-gamma) in mice bearing S-180 tumor and explore the role of the endogenous IFN-gamma in confining the transplanted tumor by intervention with immunomodulators.

METHODSMouse models bearing S-180 solid tumor were established and subjected to intragastric administration of Ganoderma lucidum polysaccharides (GLP) or cyclosporine A (CsA) at different daily doses for 9 consecutive days. Serum IFN-gamma levels were measured in untreated tumor-bearing mice and in those after completion of GLP or CsA treatments by enzyme-linked immunosorbent assay (ELISA), and the changes of the tumor weight in the treated mice were evaluated.

RESULTSIt was found for the first time that serum IFN-gamma levels in the tumor-bearing mice increased progressively within the initial 20 days after tumor implantation. The serum IFN-gamma levels in the 3 GLP-treated groups (at daily doses of 400, 200, and 100 mg/kg) all increased, which was the most obvious in 400 mg/kg GLP-treated group, and the tumor weight decreased significantly in response to GLP treatment, but the most conspicuous effect occurred with the daily dose of 200 mg/kg, and no significant statistical correlation was found between the two parameters. CsA treatment (at 20, 10, and 5 mg/kg, respectively) resulted in reduced serum IFN-gamma levels but produced virtually no effect on the tumor weight, and no obvious correlation was found between serum IFN-gamma level and the tumor weight.

CONCLUSIONIncreased serum IFN-gamma levels following GLP treatment are not significantly correlated to tumor growth inhibition in mice, and CsA reduces serum IFN-gamma levels without affecting the tumor weight, suggesting that endogenous IFN-gamma is not a major immunomodulating factor in growth inhibition of transplanted S-180 tumor.

Animals ; Cyclosporine ; pharmacology ; Female ; Ganoderma ; chemistry ; Immunologic Factors ; pharmacology ; Interferon-gamma ; blood ; Male ; Mice ; Polysaccharides ; pharmacology ; Sarcoma 180 ; blood ; pathology ; prevention & control ; Tumor Burden ; drug effects