This research is to investigate study the flavonoids from stems of Nelumbo nucifera and the cytotoxic activities of iso- lated compounds. The constituents were separated by column chromatography,and their structures were elucidated by spectroscopic data analyses. The isolated compounds were evaluated for cytoxic activities by MTT method. Twelve compounds were isolated and identified as rhamnazin-3-O-beta-D-glucopyranoside (1), luteolin-3', 4'-dimethylether-7-O-beta-D-glucoside (2), kaempferol-3-O-beta-D-xylopyranosyl-(1-->2)-O-beta-D-glucopyranoside (3), quercetin-3,3'-di-O-beta-D-glucopyranoside (4), 1, 8-dihydroxy-3,7-dimethoxyxanthone (5), isorhamnetin-3-O-beta-D-glucopyranoside(6) , kaempferol(7), isorhamnetin (8), quercetin(9), astragalin(10), hyperoside (11) and 1-hy- droxy-3,7,8-trimethoxyxanthone(12). All compounds were isolated from stems of this plant for the first time, and compounds 1-5 were firstly isolated from the family nelumbonaceae. Compounds 24 and 6 showed significant cytotoxic activities against BEL-7402 carcinoma cell lines at a concentration of 1 x 10(-5) mol x L(-1) with the inhibitory rate of 67.36%, 53.25%, 57.78%, 60.13% and 52.11%, respectively.
Cell Line, Tumor ; Flavonoids ; chemistry ; pharmacology ; Humans ; Nelumbo ; chemistry ; Plant Extracts ; chemistry ; pharmacology ; Plant Stems ; chemistry

OBJECTIVETo investigate the chemical constituents of Excoecaria acerifclia and their antitumor activities.

METHODThe constituents were isolated and purified by column chromatography. Their structures were identified by their physicochemical properties and spectral features. Cytotoxicities of the purified compounds were evaluated by MTI method against human cancer cell lines HepG2.

RESULTEight compounds were isolated and identified as: 7-hydroxy-6-methoxy-coumarin (1), 8-hydroxy-6,7-methoxy-coumarin (2), kaempferol (3), kaempferol-3-O-beta-D-glucoside (4), quercetin-3-O-beta-D galactoside (5), kaempferol-3-O-beta-D-glucoside-2"-gallate (6), beta-sitosterol (7), daucosterol (8).

CONCLUSIONAll compounds were isolated from this plant for the first time. Compounds 5 showed inhibitory activity towards HepG2 with IC50 values of 7.13 mol x L(-1).

Cell Proliferation ; drug effects ; Euphorbiaceae ; chemistry ; Hep G2 Cells ; Humans ; Plant Extracts ; analysis ; isolation & purification ; pharmacology

Thirty-three compounds were isolated from the root decoction of Isatis indigotica by using a combination of various chromatographic techniques including silica gel, macroporous adsorbent resin, Sephadex LH-20, and reversed-phase HPLC. Their structures were elucidated by spectroscopic data as (+)-dehydrovomifoliol (1), (S)-(+)-abscisic acid (2), vomifoliol (3), cyclo (L-Phe-L-Leu) (4), cyclo(L-Phe-L-Tyr) (5), cyclo(L-Tyr-L-Leu) (6), cyclo(L-Pro-L-Tyr) (7), evofolin B (8), (+)-syringaresinol (9), (-)-(7R,7'R,8S,8'S)-4,4'-dihydroxy-3-methoxy-7,9';7',9-diepoxy-lignan (10), (-)-medioresinol (11), (+) -(7R,7'R,8S,8'S) -neo-olivil (12), (-) -5-methoxyisolariciresinol (13), 1,3-dihydro-2H-indol-2-one (14), isalexin (15), dihydroneoascorbigen (16), indican (17), (-) -(S) -cyanomethyl-3-hydroxyoxindole (18), isoformononetein (19), calycosin (20), stigamast-5-ene-3beta-ol-7-one (21), acetovanillone (22), 3, 5-dimethoxy-4-hydroxyacetophenone (23), dihydroconiferyl alcohol (24), dihyroferulic acid (25), 3-hydroxy-1-(4-hydroxyphenyl) propan-1-one (26), beta-hydroxypropiovanillone (27), 4-aminobenzoic acid (28), 3-(4-hydroxyphenyl) propan-1-ol (29), 4-(2-hydroxyethyl) phenol (30), 2-methoxy-4-vinylphenol (31), pyrocatechol (32), and 4-pentenamide (33). These compounds were isolated from the root of I. indigotica for the first time. In preliminary in vitro assays, compound 19 showed activity against the influenza virus A/Hanfang/359/95 (H3N2), the herpes simplex virus 1 (HSV-1), and Coxsackie virus B3 (Cox-B3), with IC50 values of 2.06, 6.84, and 8.70 micromol x L(-1), respectively, but other compounds were in-active at a concentration of 1.0 x 10 x (-5) mol x L(-1).
Animals ; Cell Line ; Humans ; Isatis ; chemistry ; Plant Extracts ; chemistry ; pharmacology ; toxicity ; Plant Roots ; chemistry

OBJECTIVETo identify the active material of anti-hepatic fibrosis from Amydae Carapax.

METHODSMembrane separation technology was adopted to screen active fraction in Amydae Carapax, and the active components were isolated from the active fraction using gel chromatography and high performance liquid chromatography. The purified active components in Amydae Carapax were further analyzed using 4700 series time-of-flight mass spectrometer.

RESULTSProteins and peptides of Amydae Carapax with molecular weight less than 6000 were proved to have biological activity. 8 components (Bj1-Bj8) were isolated from the active fraction. Bj4, Bj6 and Bj7 were screened as active components. Bj7 was further purified, resulting in 7 components (Bj701-Bj707). Bj704 and Bj707 showed significant biological activity. Mass spectrometry showed three molecular ion peaks with highest abundance, i.e. m/e 526, 542 and 572, i.e. m/e 526, 542 and 572, in Bj707 -A The amino acid sequences of above three peptide compounds were NDDY (Asn-Asp-Asp-Tyr), NPNPT (Asn-Pro-Asn-Pro-Thr), and HGRFG (His-Gly-Arg-Phe-Gly), respectively. And M572 was the most abandunt components.

CONCLUSIONThree active peptide compounds of anti-hepatic fibrosis of Amydae Carapax were identified.

Animals ; Cell Line ; Humans ; Liver Cirrhosis ; Medicine, Chinese Traditional ; Tissue Extracts ; isolation & purification ; pharmacology

OBJECTIVE: To investigate the role of petroleum ether extract of Rhizoma Amorphophalli (SLG) in inhibiting proliferation and promoting apoptosis and differentiation of leukemia K562 cells. METHODS: K562 cells were processed by SLG and PD98059 which was the ERK signaling pathway blocker. Then cell vitality was tested by MTT. Cell apoptosis rate and positive percentage of antigen expression related with differentiation were detected by flow cytometry. The protein expression levels of ERK1/2 and pERK1/2 were detected by Western blot. RESULTS: The proliferation activity of K562 was reduced by 50, 100, 200 mg/L SLG in a concentration dependent manner (r=0.9997). The apoptosis rate and positive expression rate of CD11b, CD14 and CD42b which were related with differentiation were raised by SLG, as well as the expression of pERK1/2, while PD98059 could reverse the promoting effect of SLG on apoptosis and differentiation partially. CONCLUSION SLG can inhibit the proliferation and promote apoptosis and differentiation of K562 cells through ERK signaling pathway.
Alkanes ; Apoptosis ; Cell Proliferation ; Humans ; K562 Cells ; Petroleum ; Plant Extracts/pharmacology*

The chemical constituents from the branches and leaves of Artocarpus incisus were isolated and purified via silica gel, ODS, and Sephadex LH-20 column chromatography as well as preparative HPLC. The chemical structures of all isolated compounds were identified in the light of their physicochemical properties, spectroscopic analyses, and comparisons of their physicochemical and spectroscopic data with the reported data in literature. As a result, 20 compounds were isolated and characterized from the 90% ethanol extract of the branches and leaves of A. incisus, which were identified as tephrosin(1), 6-hydroxy-6 a, 12 a-dehydrodeguelin(2), sarcolobin(3), lupiwighteone(4), 12-deoxo-12α-methoxyelliptone(5), 6 aα,12 aα-12 a-hydroxyelliptone(6), homopterocarpin(7), 3-hydroxy-8,9-dimethoxypterocarpan(8), pterocarpin(9), maackiain(10), medicarpin(11), calycosin(12), genistein(13), formononetin(14), 5-hydroxy-4',7-dimethoxy isoflavone(15), liquiritigenin(16), 4(15)-eudesmene-1β,7α-diol(17), ent-4(15)-eudesmene-1β,6α-diol(18), 1α-hydroxyisodauc-4-en-15-al(19), and guaianediol(20). Except compounds 13 and 16, all other compounds were isolated from the Artocarpus plants for the first time. Additionally, using MTS assay, compounds 1-20 were eva-luated for their anti-rheumatoid arthritis activities by measuring their anti-proliferative effects on synoviocytes in vitro. As a consequence, compounds 1-16 showed notable anti-rheumatoid arthritis activities, which displayed inhibitory effects on the proliferation of MH7 A synovial fibroblast cells, with the IC_(50) values in range of(9.86±0.09)-(218.07±1.96) μmol·L~(-1).
Arthritis ; Artocarpus ; Cell Proliferation ; Ethanol ; Genistein ; Plant Extracts/pharmacology* ; Silica Gel ; Synoviocytes

OBJECTIVETo investigate the inhibitory activities of caffeoyl glucopyranoses purified from Balanophora japonica Makino on HIV entry and their mechanism.

METHODSHIV-1 Env pseudovirus was used to evaluate the anti-HIV-1 activity of those compounds. ELISA and molecular docking were used to study the mechanism of the actions of the active compounds.

RESULTSWe used the HIV-1 Env pseudovirus to test the anti-HIV-1 activity of the six phenolic compounds (final concentration 25 microg/ml), and found that only 1,2,6-Tri-O-caffeoyl-beta-D-glucopyranose (TCGP) and 1,3-Di-O-caffeoyl-4-O-galloyl-beta-D- glucopyranose (DCGGP) could effectively inhibit the entry of HIV-1 Env pseudovirus into the target cells in a dose-dependent manner, with IC(50) values of 5.5-/+0.2 and 5.3-/+0.1 microg/ml, respectively. These two compounds could also blocked the gp41 six-helix bundle formation. Molecular docking analysis suggested that they might bind to the hydrophobic cavity of the gp41 N-trimeric coiled-coil.

CONCLUSIONTCGP and DCGGP are potent HIV-1 entry inhibitors targeting gp41 and can serve as lead compounds for developing novel anti-HIV-1 microbicides for prevention of sexual HIV-1 transmission.

Anti-HIV Agents ; pharmacology ; Balanophoraceae ; chemistry ; Cell Line ; Gallic Acid ; analogs & derivatives ; pharmacology ; Glucose ; analogs & derivatives ; pharmacology ; HIV-1 ; drug effects ; Humans ; Hydrolyzable Tannins ; pharmacology ; Plant Extracts ; pharmacology

OBJECTIVETo study the effect of anti-HIV III B virus with extractions from Juglans regia, so as to searching for the new and efficacious leading compound of AIDS therapy.

METHODPhytochemical and chromatographical techniques were used to isolate compounds from J. regia; MT4 cells and HIV III B virus were used to study the effect of anti-HIV activity in vitro. BIACORE 3000 molecule coupled equipment were used for the target research also.

RESULTTwo extractions (B&E) were isolated from J. regia which possess the effect of anti-HIV activity. Targets study found that extraction B could affected on HIV-1 gp-41 fusing protein and extraction E could affected on HIV-1 integrase respectively.

CONCLUSIONJ. regia is a traditional Chinese medicine with active anti-HIV activity and worth to be studied further.

Cell Line ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; HIV-1 ; drug effects ; Humans ; Juglans ; chemistry ; Plant Extracts ; chemistry ; pharmacology

OBJECTIVETo study the constituents in the chloroform extract of olibanum and their antitumor activities.

METHODThe compounds were isolated by chromatographic methods and their structures were identified on the basis of spectroscopic methods and X-ray diffraction. The antiproliferative effect of the compounds in human leukemia HL-60 cells was tested by viable cell counting.

RESULTFour cembrane diterpenes were isolated and identified as incensole-oxide (1), acetyl incensole-oxide (2), incensole (3), and acetyl incensole (4).

CONCLUSIONCompounds 2 and 4 were isolated from the genus Boswellia for the first time. Compound 4 showed growth inhibitory effect against human leukemia HL-60 cell lines with IG50 value of (16.3 +/- 3.4) micromol x L(-1).

Antineoplastic Agents, Phytogenic ; chemistry ; isolation & purification ; pharmacology ; Boswellia ; chemistry ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Diterpenes ; chemistry ; isolation & purification ; pharmacology ; Humans ; Plant Extracts ; chemistry ; isolation & purification ; pharmacology

OBJECTIVE1,25-dihydroxyvitamin D3 [1,25(OH)2D3] is a potent inducer of differentiation in myeloid leukemia cells, but its clinical use is limited due to its hypercalcaemic effect and resistance. Carnosic acid is a plant-derived polyphenol food preservative with chemoprotective effects against carcinogens. Recent research has shown that carnosic acid potentiates the effects of 1,25(OH)2D3 on differentiation of human leukemia cells. This study examined the effects of 1,25(OH)2D3 in combination with carnosic acid on monocytic differentiation as well as intracellular reactive oxygen species (ROS) and Ca2+ levels in human leukemia HL-60 cells.

METHODSHL-60 cells were randomly treated with 1 nmol/L 1,25(OH)2D3, 100 nmol/L 1,25(OH)2D3, 10 micromol/L carnosic acid, a combination of 1 nmol/L 1,25(OH)2D3 and 10 micromol/L carnosic acid or placebo. Cell growth was observed by MTT assay for 72 hrs at an interval of 24 hrs. Cells were harvested after 72 hrs of culture. Morphologic features of the cells were observed by microscopy. Flow cytometry was used to detect cell cycle, monocytic differentiation marker CD14 expression, and intracellular ROS and Ca2+ levels.

RESULTSA combination of 1 nmol/L 1,25(OH)2D3 and 10 micromol/L carnosic acid resulted in greater proliferation inhibition (Ab: 0.56 0+/- 0.020 vs 1.482 +/- 0.327; P <0.01), mature monocytic features, G0 /G1 cell arrest, higher CD14 expression (57.62 +/- 0.817% vs 2.76 +/- 0.828%; P <0.01), lower intracellular ROS levels (52.67 +/- 10.76% vs 86.46 +/- 40.52%; P <0.01 and similar intracellular Ca2+ levels in HL-60 cells when compared with the placebo group. The ability of a combination of 1 nmol/L 1,25(OH)2D3 and 10 micromol/L carnosic acid to inhibit the proliferation and induce the differentiation of HL-60 cells was similar to that of 100 nmol/L 1,25(OH)2D3, while the intracellular Ca2+ level (115.64 +/- 17.74 nmol/L vs 185.75 +/- 27.38 nmol/L) was significantly lower than that in the 100 nmol/L 1,25(OH)2D3 group.

CONCLUSIONSLow concentration of 1,25(OH)2D3 combined with 10 micromol/L carnosic acid can produce enhanced differentiation, proliferation inhibition and antioxidant effects of HL-60 cells. The combination of the two inducers dose not increases intracellular Ca2+ levels.

Calcitriol ; pharmacology ; Calcium ; metabolism ; Cell Cycle ; drug effects ; Cell Differentiation ; drug effects ; Diterpenes, Abietane ; pharmacology ; HL-60 Cells ; Humans ; Lipopolysaccharide Receptors ; analysis ; Plant Extracts ; pharmacology