OBJECTIVES: To elucidate the anti-aging effect of β-sitosterol (BS), an important component in the fruits of Alpinia oxyphylla Miq., in C. elegans and its regulatory effect on ETS-5 gene to modulate ferroptosis. METHODS: C. elegans treated with 10 µg/mL BS were monitored for survival time and changes in body length, motility, and reproductive function. The effect of ETS-5 gene knockdown on survival time of C. elegans was observed, and the changes in fat accumulation and lipid redox homeostasis in the transfected C. elegans were assessed using Oil Red O staining and by detecting MDA levels and the GSH/GSSG ratio. The mRNA expression levels of ferroptosis-related genes (FTN-1, GPX-1 and AAT-9) were detected using qPCR. The effects of BS treatment and ETS-5 knockdown on AAT-9 enzyme activity in C. elegans were examined. The effect of BS on nuclear localization of FEV (the human homolog of ETS-5) was validated in cultured human umbilical venous endothelial cells (HUVECs). RESULTS: Both BS treatment and ETS-5 knockdown significantly prolonged the lifespan, promoted lipid accumulation and reduced lipid peroxidation in C. elegans. ETS-5 knockdown resulted in upregulated expressions of the ferroptosis repressors GPX-1, AAT-9 and FTN-1 and increased the GSH/GSSG ratio in C. elegans. CONCLUSIONS BS inhibits ferroptosis in C. elegans by suppressing the expression of ETS-5 transcription factor and hence the activity of AAT-9 enzyme, a key gene for ferroptosis, which in turn prolongs the lifespan of C. elegans.
Animals ; Caenorhabditis elegans/physiology* ; Ferroptosis/drug effects* ; Alpinia/chemistry* ; Sitosterols/pharmacology* ; Longevity/drug effects* ; Fruit/chemistry* ; Humans

Twenty-one non-anthraquinones constituents were isolated for the first time from an ethanol extract of the roots of Knoxia valerianoides by using a combination of various chromatographic techniques including column chromatography over silica gel, Sephadex LH-20, and reversed-phase HPLC. Their structures were identified by their physical-chemical properties and spectroscopic analysis including NMR and MS. The compounds include ten triterpenoids: ursolic acid (1), oleanolic acid (2), 2-oxo pomolic acid (3), pomolic acid (4), maslinic acid (5), rotungenic acid (6), tormentic accid (7), rotundic acid 3,23-acetonide (8), arjungenin (9), and 2alpha, 3beta, 19alpha, 23-tetrahydroxy-urs-12-en-28-oic acid (10), four sitosterones: (24R)-24-ethylcholesta-4,22-dien-3-one (11), 3-oxo-4-en-sitosterone (12), 7-oxostigmasterol (13), and 7-oxo-beta-sitosterol (14), two lignans: eudesmin (15) and ciwujiatone (16), one coumarin: cnidilin (17), and four simple aromatic analogues: 5-hydroxymethylenefural (18), 3-hydroxy-4-methoxybenzoic acid (19), benzoic acid (20), and 2-hydroxy-5-methxoycinnamaldehydes (21). In the in vitro assays against human cancer cell lines (HCT-8, Bel7402, BGC-823, A549, and A2780), against deserum and glutamate induced PC12-syn cell damage, and against HIV-1 replication, and inhibiting protein tyrosine phosphatase 1B (PTP1 B), LPS induced NO production in macrophage, and Fe(2+)-cystine induced rat liver microsomal lipid peroxidation, at a concentration of 1 x 10(-5) mol x L(-1), no compound showed activity.
Animals ; Cell Line, Tumor ; Chromatography, High Pressure Liquid ; Humans ; Lignans ; analysis ; chemistry ; isolation & purification ; Mice ; Plant Roots ; chemistry ; Rubiaceae ; chemistry ; Sitosterols ; chemistry ; isolation & purification ; pharmacology ; Triterpenes ; chemistry ; isolation & purification ; pharmacology

OBJECTIVETo study the antiproliferative effects of beta-sitosterul and its mechanism in hepatoma HepG2 cells.

METHODCell proliferation was assessed by MTT assay. Cell cycle distribution, apoptosis and mitochondrial membrane potential were measured by high content screening (HCS). The protein expression of caspase-3, caspase-8, caspase-9, Bcl-2, Bax, tBid and cytochrome c in the HepG2 cells were evaluated by Western Blots.

RESULTbeta-Sitosterul exerted significant antiproliferative effects in HepG2 cells. Furthermore, beta-sitosterul also induced HepG2 cells apoptosis, lost mitochondrial membrane potential, activated caspase-3, caspase-8 and caspase-9, up-regulate Bax, tBid protein, down-regulation Bcl-2 protein. However, beta-sitosterul had hardly any effects on QSG7701 cells.

CONCLUSIONbeta-Sitosterul exerted antiproliferative effects and induced HepG2 cells apoptosis via mitochondrial pathway and membrane death receptor pathway.

Antineoplastic Agents ; pharmacology ; Apoptosis ; drug effects ; Apoptosis Regulatory Proteins ; metabolism ; Carcinoma, Hepatocellular ; metabolism ; pathology ; Cell Cycle ; drug effects ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Hep G2 Cells ; Humans ; Liver Neoplasms ; metabolism ; pathology ; Membrane Potential, Mitochondrial ; drug effects ; Sitosterols ; pharmacology

OBJECTIVETo study on the chemical constituents of Lobelia chinensis.

METHODThe coloumn chromatographic techniques were applied to isolate constituents, and their structures were elucidated by means of spectral data analysis.

RESULTSixteen compounds were isolated and identified as daucosterol (1), diosmetin (2), apigenin (3), chrysoeriol (4), loteolin (5), hesperidin (6), loteolin-7-O-beta-D-glucoside (7), apigenin-7-O-beta-D-glucoside (8), linarin (9), diosmin(10), 5,7-dimethoxy-8- hydroxycoumarin (11), palmitinic acid (12), lacceroic acid (13), stearic acid (14), beta-sitosterol (15), daucosterol (16).

CONCLUSIONAll of these compouds were obtained from L. chinensis for the first time.

Apigenin ; analysis ; Cholestenones ; analysis ; Flavones ; Flavonoids ; analysis ; Glycosides ; analysis ; Hesperidin ; analysis ; Lobelia ; chemistry ; Plant Extracts ; pharmacology ; Sitosterols ; analysis

OBJECTIVETo study the chemical constituents of the bee-collected rape pollen.

METHODThe compounds were isolated by column chromatography on silica gel; Sephadex LH-20 and C18. Their structures were elucidated on the basis of spectral analysis.

RESULTNine compounds were isolated from the bee-collected rape pollen and the structures of them were kaemferol-3-O-beta-D-glucosyl-(2-->1)-beta-D-glucoside (1), kaemferol-3,4'-di-O-beta-D-glucoside (2), quercetin-3-O-beta-D-glucosyl-(2-->1)-beta-D-glucoside (3), nicotinic acid (4), nicotinamide (5), trans-p-coumaric acid-4-O-beta-D-glucopyranoside (6), kaemferol (7), beta-sitosterol (8) and 5-hydroxymethylfurfural (9).

CONCLUSIONCompounds 1-6 were isolated from the bee-collected rape pollen for the first time.

Animals ; Bees ; physiology ; Brassica napus ; chemistry ; physiology ; Coumaric Acids ; chemistry ; Dextrans ; chemistry ; Glucosides ; chemistry ; Molecular Structure ; Plant Extracts ; pharmacology ; Pollen ; chemistry ; physiology ; Propionates ; Sitosterols ; chemistry

To study the chemical constituents of aerial parts of Laggera pterodonta (DC.) Benth., the air-dried aerial parts of this plant were powered and extracted with boiling water and purified by silica gel column chromatography and recrystallized. Eleven compounds were obtained from L. pterodonta. They were identified as to be 6-O-beta-D-glucopyranosyl-carvotanacetone (1), pterodontic acid (2), 1beta-hydroxy pterondontic acid (3), pterodontoside A (4), pterodondiol (5), pterodontriol B (6), 5-hydroxy-3,4', 6,7-tetramethoxyflavone (7), artemitin (8), chrysosplenetin B (9), quercetin (10) and beta-sitosterol (11). Compound 1 is a new monoterpene glucoside. Compounds 10 and 11 were isolated from this plant for the first time. Compounds 2 and 5 showed moderate activity against bacteria including Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, Mycobacteium phlei and Bacillus circulans by paper disc diffusion method, while they both displayed no activity against Escherichia coli.
Anti-Bacterial Agents ; pharmacology ; Asteraceae ; chemistry ; Chromatography, Gel ; Flavonoids ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Plant Components, Aerial ; chemistry ; Plants, Medicinal ; chemistry ; Pseudomonas aeruginosa ; drug effects ; Quercetin ; chemistry ; isolation & purification ; Sesquiterpenes ; chemistry ; isolation & purification ; pharmacology ; Sitosterols ; chemistry ; isolation & purification ; Spectrometry, Mass, Electrospray Ionization ; Staphylococcus aureus ; drug effects ; Terpenes ; chemistry ; isolation & purification

AIMTo study the transfection and anti-hepatitis B virus (HBV) effect of the co-modified hepatocytes-targeting cationic liposomes encapsulating anti-HBV antisense oligonucleotides (asON) , and to investigate the transfection mechanisms of the liposomes.

METHODSDipalmitoylphosphatidylcholine (DPPC) and 3beta-[N-(N',N'-dimethylaminoethane)-carbamoyl] cholesterol (DC-Chol) were used as the lipids, beta-sitosterol-beta-D-glucoside (sito-G) and Brij 35 were used to modify the liposomes. Flow cytometry (FCM), fluorescence microscopy and enzyme-linked immunosorbent assay (ELISA) were utilized to evaluate the transfection improvement of the asON encapsulated in the liposomes in primary rat hepatocytes and the antigens inhibition activity in HepG 2.2.15 cells. The transfection mechanisms were evaluated based on the influence of wortmannin, nigericin, and asialofetuin on the antigens inhibition in HepG 2.2.15 cells by ELISA.

RESULTSThe co-modification with sito-G and Brij 35 significantly improved the transfection of the liposomes in primary rat hepatocytes and antigens inhibition effect in HepG 2.2.15 cells. Both transfection efficiency and antigens inhibition effect showed to be concentration-dependent with the asON-encapsulating liposomes. In fluorescence microscopy, the transfected cells showed strong fluorescence in primary rat hepatocytes, especially in the nuclei. Wortmannin, nigericin and asialofetuin decreased the antigens inhibition of the asON-encapsulating liposomes to different levels. Cationic liposomes modification with sito-G and Brij 35 could improve the transfection and antigens inhibition effect of the asON. The transfection mechanisms of the co-modified liposomes included endocytosis and membrane fusion. The ligand sito-G was confirmed to be able to enhance asialoglycoprotein receptor (ASGPR)-mediated endocytosis.

CONCLUSIONCo-modified hepatocytes-targeting cationic liposomes would be a specific and effective carrier to transfer asON into hepatocytes.

Androstadienes ; pharmacology ; Animals ; Asialoglycoproteins ; pharmacology ; Cell Line, Tumor ; Cell Nucleus ; metabolism ; Cell Survival ; Cells, Cultured ; Endocytosis ; drug effects ; Female ; Fetuins ; Flow Cytometry ; Hepatitis B Antigens ; metabolism ; Hepatitis B virus ; genetics ; immunology ; Hepatocytes ; cytology ; drug effects ; metabolism ; Humans ; Liposomes ; Microscopy, Fluorescence ; Nigericin ; pharmacology ; Oligonucleotides, Antisense ; chemistry ; genetics ; Polyethylene Glycols ; chemistry ; Rats ; Rats, Wistar ; Sitosterols ; chemistry ; Transfection ; methods ; alpha-Fetoproteins ; pharmacology

OBJECTIVETo study the active components and their functionary mechanism of the extract of Brassica alba seeds, which inhibits experimental mice prostatic hyperplasia.

METHODProstatic hyperplasia of castrated male mice induced by testosterone propionate, the penetrability of capillary vessel of mice skin induced by histamine and the endermic flesh bud of rat induced by filter paper were used as experimental models. Sinalbin and beta-sitosterol separated from seeds of Brassica alba were used to test the activities.

RESULTSinalbin and beta-sitosterol(16.0 mg.kg-1.d-1 and 8.0 mg.kg-1.d-1) could significantly inhibit mice prostatic hyperplasia induced by testosterone propionate and activity of serum acid phosphatase(P < 0.01 or P < 0.05), Sinalbin(16.0 mg.kg-1.d-1)could significantly inhibit the hyperplasia of endermic flesh bud in rat induced by filter paper(P < 0.05), beta-sitosterol(16.0 mg.kg-1.d-1 and 8.0 mg.kg-1.d-1) could significantly decrease the penetrability of capillary vessel of mice skin induced by histamine.

CONCLUSIONSinalbin and beta-sitosterol have anti-androgen and anti-inflammation activities.

Androgen Antagonists ; pharmacology ; Animals ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacology ; Capillary Permeability ; drug effects ; Choline ; analogs & derivatives ; isolation & purification ; pharmacology ; Female ; Male ; Mice ; Mustard Plant ; chemistry ; Orchiectomy ; Plants, Medicinal ; chemistry ; Prostatic Hyperplasia ; blood ; chemically induced ; physiopathology ; Rats ; Rats, Sprague-Dawley ; Seeds ; chemistry ; Sitosterols ; isolation & purification ; pharmacology ; Testosterone Propionate