Antrodia cinnamomea exerts an anti-hepatoma effect by targeting PI3K/AKT-mediated cell cycle progression in vitro and in vivo

Antrodia cinnamomea is extensively used as a traditional medicine to prevention and treatment of liver cancer. However, its comprehensive chemical fingerprint is uncertain, and the mechanisms, especially the potential therapeutic target for anti-hepatocellular carcinoma (HCC) are still unclear. Using UPLC‒Q-TOF/MS, 139 chemical components were identified in A. cinnamomea dropping pills (ACDPs). Based on these chemical components, network pharmacology demonstrated that the targets of active components were significantly enriched in the pathways in cancer, which were closely related with cell proliferation regulation. Next, HCC data was downloaded from Gene Expression Omnibus database (GEO). The Cancer Genome Atlas (TCGA) and DisGeNET were analyzed by bioinformatics, and 79 biomarkers were obtained. Furtherly, nine targets of ACDP active components were revealed, and they were significantly enriched in PI3K/AKT and cell cycle signaling pathways. The affinity between these targets and their corresponding active ingredients was predicted by molecular docking. Finally, in vivo and in vitro experiments showed that ACDPs could reduce the activity of PI3K/AKT signaling pathway and downregulate the expression of cell cycle-related proteins, contributing to the decreased growth of liver cancer. Altogether, PI3K/AKT-cell cycle appears as the significant central node in anti-liver cancer of A. Cinnamomea.

Simultaneous Determination of 5 Nucleosides from Different Parts of Cultured Cordyceps militaris by HPLC / 中国药房

OBJECTIVE:To establish a method for simultaneous determination of 5 nucleoside from different parts of cultured Cordyceps militaris. METHODS:HPLC method was adopted. The determination was performed on InertSustain C18 column with mobile phase consisting of methanol-0.02 mol/L monobasic potassium phosphate solution (gradient elution) at the flow rate of 0.6 mL/min. The detection wavelength was set at 254 nm,the column temperature was 30 ℃. RESULTS:The linear ranges of uridine, inosine,guanosine,adenosine and cordycepin were 0.568-3.408 μg(r=0.9999),0.284-1.704 μg(r=0.9999),0.264-1.584 μg(r=0.9999),0.232-1.392 μg(r=0.9999)and 1.672-10.032 μg(r=0.9998),respectively. RSDs of precision,stability and repeatabili-ty tests were all lower than 3.0%. The recoveries were 98.2%-103.9%(RSD=1.97%,n=9),96.2%-101.6%(RSD=1.76%,n=9),96.7%-102.0%(RSD=1.94%,n=9),95.1%-99.4%(RSD=1.43%,n=9) and 95.6%-101.3%(RSD=1.82%,n=9). CON-CLUSIONS:The method is simple,precise,stable and repeatable,and can be used for simultaneous determination of 5 nucleoside from cultured C. militaris,the content of nucleosides are different in different parts of C. militaris.

Simultaneous Determination of Contents of 4 Heavy Metal Elements in Cultured Cordyceps militaris by ICP-MS / 中国药房

OBJECTIVE:To establish the method for the simultaneous determination of contents of 4 heavy metal elements in cultured Cordyceps militaris. METHODS:The samples were digested by nitric acid heating method and then determined by ICP-MS including radio-frequency power of 1.15 kW,sampling depth of 65 nm,auxiliary gas flow rate of 1.0 L/min,cooling gas flow of 13.0 L/min,temperature of 25 ℃,automatic plasma. RESULTS:The linear ranges of arsenic(As),cadmium(Cd),mer-cury (Hg) and lead (Pb) were 0-20 μg/mL(r=0.9970),0-10 μg/mL(r=0.9995),0-5 μg/mL(r=0.9955),0-20 μg/mL(r=0.9960),respectively. Detectio limit were 0.128,0.003,0.002,0.004 mg. RSDs of precision,stability and reproducibility tests were all lower than 6.5%. Recoveries of them were 90.4%-100.6%(RSD=3.45%,n=9),94.3%-101.3%(RSD=2.93%,n=9), 90.0%-102.3%(RSD=4.03%,n=9),92.3%-103.0%(RSD=3.53%,n=9),respectively. CONCLUSIONS:The method is sim-ple,precise,stable,reproducible,and can be used for simultaneous determination of contents of 4 heavy metal elements in cul-tured C. militaris. The contents of As,Cd,Hg and Pb in 10 batches of sample are all in line with related national standards.

Detection and Identification of Volatile Constituents from Leaves and Fruits of Piper nigrum by HS-SPME-GC-MS / 中国药房

OBJECTIVE:To establish a method for the detection of volatile constituents from the leaves and fruits of Piper ni-grum. METHODS:HS-SPME-GC-MS was used. The chromatographic conditions:column was HP-5 MS quartz elastic capillaries, carrier gas was high purity helium(99.999%),flow rate was 1.0 mL/min,the inlet temperature was 250 ℃,initial temperature of column was 50 ℃(temperature programmed),split injection with split ratio of 10:1. MS conditions:ionization mode was electron impact ion source,ionization energy was 80 eV,ion source temperature was 230 ℃,quadrupole temperature was 150 ℃,trans-mission line temperature was 280 ℃,electron multiplier voltage was 1588 V,mass scanning range was m/z 30-400. The spectra were retrieved using RTLPEST3. L and NIST08. L,and the relative contents of the volatile constituents were determined by area normalization method. RESULTS:There were 28 volatile constituents in the leaves and 15 in the fruits,respectively accounting for 67.13% and 36.85%. The major volatile constituents of leaves were β-caryophyllene (15.72%),limonene (9.39%),3-carene (9.32%),β-pinene(6.80%),α-terpine(4.98%),etc.,the main volatile constituents of fruits were 1,7,7-trimethyl-2-vinylbicyclo [2.2.1]hept-2-ene(10.45%),espatulenol(8.28%),caryophyllene oxide(4.81%),etc. 5 constituents were owned in both. CON-CLUSIONS:The study basically clears the main volatile constituents from the leaves and fruits of P. nigrum,and verifies existing obvious differences.

Inhibitory Activity of α-Glucosidase from Extracts of Different Processed Salvia Miltiorrhiza Bunge . Products / 世界科学技术-中医药现代化

This article was aimed to evaluate the α-glucosidase inhibitory activity of extracts from the root of Salvia miltiorrhiza Bunge and different processed products. The α-glucosidase inhibitory activity was screened with acarbose as positive control and by α-glucosidase inhibitory model in v itro . The results showed that the ex-tracts from the root of S. miltiorrhiza and different processed products had inhibitory activity. And the activity was higher than that of acarbose. In addition to the MeOH extract of S. miltiorrhiza carbon, the inhibitory activity of MeOH extracts from other processed products were higher than that of MeOH extract of S. miltiorrhiza. The in-hibitory activity of petroleum ether extracts of different processed products were close to S. miltiorrhiza. EtOAC extracts were lower than that of S. miltiorrhiza. The n-BuOH extracts were higher than that of S. miltiorrhiza. The inhibitory activity of extracts was positively correlated with concentrations, and it depended on the concentra-tion. It was concluded that the processed products of S. miltiorrhiza can strengthen α-glucosidase inhibitory activ-ity in different degrees.

Volatile Constituents from Three Parts of Cucurbita Moschata Duch. (Miben) by Head-Space Solid Phase Micro-Extraction Coupled with GC-MS / 世界科学技术-中医药现代化

This study was aimed to analyze the volatile constituents from flower, stem tip and seed of Cucurbita moschata Duch.(Miben). The volatiles were analyzed by head-space solid micro-extraction, coupled with GC-MS and Kovats indices for the first time . The results showed that 22 compounds were identified from the flower , 20 from the stem tip and 21 from the seed of the C. moschata (Miben). The total essential constituents from each part were 91 . 89%, 89 . 24% and 96 . 26%, respectively . A total of 10 compounds in the flower and stem tip were mutual. And 3 compounds in the flower, stem tip and seed were mutual. It was concluded that the β-bourbonene (17.57%) and heneicosane (11.90%) were the highest components of the total essential constituents of the flower of C. moschata (Miben). Decanal (28.77%) was the highest components of the stem tip and hexadecanoic acid ethyl ester (29.12%), 2,3-butanediol (16.90%) and linoleic acid ethyl ester (16.52%) were the highest compo-nents of seed of C. moschata (Miben).

Alpha-glucosidase inhibitory active constituents contained in nutshell of Trapa acornis / 中国中药杂志

<p><b>OBJECTIVE</b>To study chemical constituents in nutshell of Trapa acornis and in vitro inhibitory activity against alpha-glucosidase.</p><p><b>METHOD</b>EtOAC and n-butanol extractive fractions were separated by chromatography and their structures were identified by multiple spectroscopic techniques.</p><p><b>RESULT</b>Nine compounds were separated, they were 4,23,24-trimethylcholest-22-en-3-ol (1), stigmasterol (2), alpha-amyrin (3), (+)-nyasol (4), oleanolic acid (5), ursolic acid (6), hederagenin (7), 3,23-dihydroxy-12-ursen-28-oic acid (8) and beta-daucosterol (9). Total extracts from T. acornis nutshells, petroleum ether fractions, acetic ether fractions and normal butanol fractions showed inhibitory activity against alpha-glucosidase. Compound 5 (IC50 2.88 mg x L(-1)) and 6 (IC50 4.42 mg L(-1)) showed stronger inhibitory activity against alpha-glucosidase.</p><p><b>CONCLUSION</b>All compounds except compound 2 were separated from the genus for the first time, and compound 1-9 were separated from this plant for the first time.</p>

Effects of waste batteries leaching solution stress on resistance physiological indices of volatile constituents from Schizonepeta tenuifolia / 中国中药杂志

<p><b>OBJECTIVE</b>The effect of waste batteries leaching on the seedling growth and volatile constituents in leaves of Schizonepeta tenuifolia was assayed.</p><p><b>METHOD</b>The different concentrations of waste batteries leaching on the seedling growth were discussed. Volatile compounds were analyzed by solid-phase micro-extraction (SPME) coupled with gas chromatography-mass spectrometry (GC-MS).</p><p><b>RESULT</b>The results indicated that S. tenuifolia showed resistance to heavy metal polluting, but the high rate of waste batteries leaching had the inhibiting effect to seedlings growth. The waste batteries leaching cause the major volatile constituents in leaves of S. tenuifolia was changed greatly under waste batteries leaching solution stress.</p><p><b>CONCLUSION</b>Heavy metal leached by waste batteries had great effect on growth of S. tenuifolia, reducing its value for food and medical purposes.</p>

Anti-bacteria activity of Puraboeo rutescens and Lysionotus pauciflorus / 中国中药杂志

<p><b>OBJECTIVE</b>Antibacteria activity of compounds from Puraboeo ruescens and Lysionotus pauciflorus was assayed.</p><p><b>METHOD</b>Disc diffusion was used to isolate compounds in vitro and berberine was positive control. The value of IC50 was assayed by the method of liquid culture. All kinds of chromatography were used to isolate the chemical constituent and structure was identified by MS and NMR spectroscopy.</p><p><b>RESULT</b>Eight compounds were isolated and identified as beta-sitosterol (1), E-3,4-dihydroxy cinnamic acid (2), barbinervic acid (3), 3beta,19alpha-dihydroxy12-en-28-ursolic acid (4), 28-O-beta-D-glucopyranosyl pomolic acid (5), 5,7-dihydroxy-6,8,4'-trimethoxy flavone (6), 5, 6, 4'-trihydroxy-7,8-dihydroxy flavone (7), 5-hydroxy-6,8,4'-trimethoxy flavone-7-O-beta-D-glucopyranosyl (8). Compound 3, 4 and 6 had activity against SA, MRSA and ESBLs respectively. Compound 3 showed (IC50 = 0.098 g x LU(-1), IC50 = 0.27 g x L(-1)) against SA and ESBLs-SA respectively. Compound 4 (IC50 = 0.130 g x L(-1)) was best to against MR SA.</p><p><b>CONCLUSION</b>Compound 1 - 5 were isolated from this plant for the first time. Compound 7 and 8 was isolated from Gesneriaceae for the first time.</p>

Alpha-glucosidase inhibitors from leaves of Forsythia suspense in Henan province / 中国中药杂志

<p><b>OBJECTIVE</b>The alpha-glucosidase inhibitory compounds were searched from Forsythia suspense.</p><p><b>METHOD</b>The active compounds were isolated by the method of bioassay-guided in vitro and column chromatographic techniques. The structures of compounds were identified by MS and NMR spectroscopy. The inhibitory kinetics of the isolated compounds were investigated.</p><p><b>RESULT</b>The ethyl acetate extract showed the strongest inhibitory activity, and five active compounds were isolated from this extract. The IC50 value of compound 1-5 were all lower than that of acarbose as positive control. Compound 1, the mixture of 1, 2 and 4 all showed noncompetitive type model on alpha-glucosidase.</p><p><b>CONCLUSION</b>Compound 1-3 as the inhibitors of alpha-glucosidase were reported for the first time. Compound 3 was isolated from the genus for the first time.</p>

Active compounds from rhizomes of Musa basjoo / 中国中药杂志

<p><b>OBJECTIVE</b>To study the active compounds from the rhizomes of Musa basjoo.</p><p><b>METHOD</b>Antioxidant and alpha-glucosidase inhibitory activity of different extracts were tested. Using bioassay-guided fractionation, the chemical constituents in EtOAC extracts were isolated by column chromatography and identified by MS and NMR spectroscopy.</p><p><b>RESULT</b>Five compounds were isolated and identified as 2',3, 4'-trihydroxyflavone (1), 3,3'-bis-hydroxyanigorufone (2), irenolone (3), 4-dihydroxy-9-(4'-hydroxyphenyl)-phenalenone (4) and 3,4-dihydroxybenzaldehyde (5). Compound 1(IC50 8.61 mg x L(-1)), 3 (IC50 19.55 mg x L(-1)) and 5 (IC50 1.1 mg x L(-1)) had antioxidant activity. Compound 2 (IC50 24.15 mg x L(-1)) and 4(IC50 2.81 mg x L(-1)) had alpha-glucosidase inhibitory activity. Compound 5 showed MIC of 0.078, 0.313, 0.039 microg/disc against SA, MRSA and ESBLs, respectively.</p><p><b>CONCLUSION</b>Compound 1-5 were isolated from this plant for the first time. Compound 5 was isolated from the genus Musa for the first time. All compound except 5 were first reported about activity.</p>

Alpha-glucosidase inhibitors from Luculia pinciana / 中国中药杂志

<p><b>OBJECTIVE</b>To search alpha-glucosidase inhibitors from Luculia pinciana.</p><p><b>METHOD</b>The alpha-glucosidase inhibitor was isolated by the column chromatographic techniques and the bioassay-guided method in vitro. A combination of MS and NMR spectroscopy was used to identify the chemical structures. The inhibitory kinetic of the isolations was also investigated.</p><p><b>RESULT</b>The ethyl acetate extract showed strongest inhibitory activity, and five active compounds were isolated and identified as scopletin (1), 5-methoxy-8-hydroxycoumarin (2), lalpha,3beta,24-trihydroxyursolic acid (3), ursolic acid (4) and oleanolic acid (5). The IC50 values of all compounds were lower than that of acarbose. Four of them shown noncompetitive type manner on alpha-glucosidase inhibition except that compound 3 is competitive type manner.</p><p><b>CONCLUSION</b>Compounds 1-4 as the inhibitors of alpha-glucosidase were reported for the first time.</p>

Triterpenes from Corallodiscus kingianus / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents from Corallodiscus kingianus.</p><p><b>METHOD</b>The column chromatographic techniques were applied to isolate constituents. A combination of ESI-MS and NMR spectroscopy was used to identify structures.</p><p><b>RESULT</b>Six compounds were isolated from the acetone extract of this plant, and the structures of them have been identified as castanopsol (1) , 3beta-hydroxy-9 (11), 12-oleanadien-28-oic acid (2), 2,3,7-trihydroxy-6-oxo-1,3,5 (10), 7-tetraene-24-nor-frie-delane-29-oic acid methylester (3), 3-epicyclomusalenol (4), palmitinic acid (5) and stearic acid (6).</p><p><b>CONCLUSION</b>Compounds 1-6 were isolated for the first time from Gesneriaceae.</p>

Chemical constituents from Aeschynanthus longicaullis / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents from Aeschynanthus longicaullis.</p><p><b>METHOD</b>The column chromatographic techniques were applied to isolate the constituents. The spectroscopie methods were used of EI-MS and NMR to identify the structures of the separated compounds.</p><p><b>RESULT</b>Seven compounds were isolated from the ethyl acetate extract of A. longicaullis, whose structures were elucidated as cryptomeridiol (1), 4 (15) -eudesmene-1beta, 6alpha-diol (2), 2,5-bornanediol (3), isovanillic acid (4), vanillic acid (5), stigmast-5 (6) , 22 (23)-diene-3beta-ol (6) and beta-sitosterol (7).</p><p><b>CONCLUSION</b>Compounds 1-5 were isolated for the first time from Gesneriaceae and 6-7 were isolated for the first time from this plant.</p>

Chemical constituents and bioactivity of Teucrium pilosum / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents and bioactivity of Teurium pilosum.</p><p><b>METHOD</b>Various column chromatographic techniques were used to isolate the constituents. A combination of EI-MS, NMR spectroscopy and X-Ray were applied to identify the structures. The anti-microorganism was accomplished by disk diffusion method, the antioxidant activity was assayed by the DPPH microanalysis models and the inhibitory activity of alpha-glucosidase was screened In vitro.</p><p><b>RESULT</b>Eight compounds were isolated and identified as: glyceryl tristearate (1), 2,5-dioxolanone (2), fernenol (3), stigmasta-5,22-dien-3P-ol (4), 24-nor cholesta-5,22 (E)-dien-3beta-ol (5), ca-spinasterol (6), (3,4-dihydroxyphenyl) acrylate (7), 3,4-dihydroxy phenyl acrylic acid (8).</p><p><b>CONCLUSION</b>All compounds have been isolated from the genus for the first time. Compound 3 [IC50 = (37.63 +/- 3.45) mg +/- L(-1)], 6 [IC50 = (178.92 +/- 4.99) mg x L(-1)] and 8 [IC50 = (44.32 +/- 7.02) mg x L(-1)] are of higher inhibitory alpha-glucosidase activity than that of acarbose [IC50 = (1081.27 +/- 12.3) mg x L(-1)]. Compound7 [IC50 = (4.81 +/- 0.96) mg x L(-1)] and 8 [IC50 = (4.16 +/- 0.11) mg L(-1)] showed higher antioxidant activity than that of BHT [IC50 = (35.64 +/- 0.36) mg x L(-1)] and BHA [IC50 = (8.74 +/- 0.39) mg x L(-1)]. Compound 5-8 exhibited inhibitory activity against Fusarium graminearum. Compound 5 and 8 showed inhibitory activity against Botrytis cinerea.</p>

Alpha-glucosidase inhibitors from Rubia cordifolia / 中国中药杂志

<p><b>OBJECTIVE</b>To search alpha-glucosidase inhibitors from Rubia cordifolia.</p><p><b>METHOD</b>The alpha-glucosidase inhibitors were isolated by the column chromatographic techniques and the bioassay-guided method in vitro. A combination of MS and NMR spectroscopy was used to identify the chemical structures. The inhibitory kinetics of the inhibitors were also investigated.</p><p><b>RESULT</b>The chloroform extract showed high inhibitory activity, and three active compounds were isolated and identified as 1,3-dihydroxy-2-methylanthraquinone (1), 1-hydroxy-2-methylanthraquinone (2) and 1,2-dihydroxyanthraquinone (3). The IC5o values of compound 1-3 were all lower than that of acarbose. Compound 1 and 2 shown competitive type manner on alpha-glucosidase, whereas compound 3 shown noncompetitive type model.</p><p><b>CONCLUSION</b>Compounds 1-3 as strong inhibitors of alpha-glucosidase were reported for the first time.</p>

Study on Volatile Constituents from Tamarix ramosissima / 中国药房

OBJECTIVE: To conduct a quantitative analysis of volatile constituents from Tamarix ramosissima.METHODS: The volatile constituents were extracted from T.ramosissima using solid phase microextraction and identified using GC-MS combined with Kvotas retention index.RESULTS: 34 constituents were separated from T.ramosissima and 25 constituents were identified.The relative mass content of volatile constituents was determined by peak area normalization method,accounting for 89.50% of total peak area.The main chemical constituents were pentadecane (16.83%),nonanal (12.45%),hexadecane (8.20%),tetradecane (8.08%) and hexanal (7.37%).The result showed hydrocarbon (37.11%),aldehyde (27.56%),ketone (8.89%) and alcohol (8.04%) were the main constituents.CONCLUSION: The study can provide scientific basis for the further development of T.ramosissima.

Study on Effect of the Extracts of Polygonum lapathifolium on the Activity of ?-glucosidase / 中国药房

OBJECTIVE:To investigate the effect of the extracts of Polygonum lapathifolium on the activity of ?-glucosidase.METHODS:Soxhlet extraction was applied to extract overground part of P.lapathifolium,and the inhibition effect of extracts on ?-glucosidase was determined with 96-microplate-based method,and the inhibitory kinetic characteristics of methanol extract was investigated using Lineweaver-Burk method.RESULTS:The extracts from P.lapathifolium showed good inhibitory activity.The methanol extract had the highest inhibitory activity (IC50=2.13 ?g?mL-1)followed by ethyl acetate extract (IC50=3.826 ?g?mL-1),petroleum ether extract (IC50=230.86 ?g ? mL-1).And they were all higher than that of acarbose (IC50=1 103.01 ?g?mL-1) as positive control.Inhibitory kinetics test indicated that methanol extract was noncompetitive inhibitor.CONCLUSION:The extracts of P.lapathifolium have good inhibition effect on the activity of ?-glucosidase with a good prospect of development and utilization.

Studies on the Volatile Component from the Flower of Tamarix chinensis / 中国药房

OBJECTIVE:To conduct a quantitative analysis on the volatile constituents from the flower of Tamarix chinensis. METHODS:The volatile constituents were extracted from the flower of T. chinensis by solid-phase microextraction technique and component identification was carried out by GC-MS combined with retention index. RESULTS:36 kinds of compounds were identified,among which pentadecane took up a greatest proportion (9.80%),followed by 6,10,14-trimethyl-2-pentadecanone (7.61%),5,6-dihydro-6-pentyl-2H-pyran-2-one(6.83%),hexadecane(6.25%)and 5,6,7,7a-tetrahydro-4,4,7a-trimethyl-2(4H)-benzofuranone(5.13%).CONCLUSION:This study serves as a scientific basis for the further development and utilization of T. chinensis.

Analysis of Volatile Components of Eriobotrya japonica by Headspace SPME-GC-MS / 中国药房

OBJECTIVE: To analyze the volatile components in the Eriobotrya japonica by headspace solid-phase microextraction-gas chromatography-mass spectrometry(SPME-GC-MS) and to optimize the operating conditions for SPME.METHODS: DB-5 MS elastic silica capillary column(30.0 m?250 ?m?0.25 ?m) was used as the chromatographic column with helium of high purity(99.999%) as carrier gas at a flow rate of 1.0 mL?min-1.The injector temperature was 250 ℃;MS condition: ionization mode was EI with electron energy of 70 eV and the mass scan range of 30～440 amu.RESULTS: After headspace absorption for 30 min at 80 ℃ using 65 ?m polydimethylsiloxane-divinyl-benzene extraction head followed by desorption for 1 min at 250 ℃,the E.japonica sample was separated and identified by GC-MS analysis.A total of 34 peaks were obtained and 29 components were identified which accounted for 97.42% of the total peak area,topping the list were benzaldehyde and 4-methoxybenzaldehyde.CONCLUSION: HS-SPME-GC-MS can be used for the rapid analysis of the volatile components in E.japonica.