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??Chrysanthemum morifolium has a long history of culture and use in China. Due to different germplasm resources, producing areas, and processing methods, many cultivated varieties have formed now. The varieties and processing methods of C. morifolium are affected by economic interests and processing cost, which change gradually. On the basis of spot investigation and related literature study, the changes of the varieties and processing methods of C. morifolium were summarized in this paper. It will provide theoretical evidence for the culture, processing, quality evaluation, and clinical application of C. morifolium.     

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??OBJECTIVE To study the monthly dynamics of physical and chemical indexes in Achyranthis Bidentatae Radix(ABR, the dried root of Achyranthes bidentata Bl.) stored in simple and cool warehouses. METHODS ABR was stored in simple and cool warehouses for 27 months. The color was observed. The water content was determined based on the drying method. The contents of ??-ecdysone and 5-hydroxymethylfurfural (5-HMF) were determined by HPLC method. The accumulation of temperature difference between the simple and cool warehouses was evaluated with a relative temperature cumulation (RTC) method. The monthly dynamics of physical and chemical indexes of ABR was analyzed with RTC. RESULTS As the extension of storage time, the ABR stored in the simple warehouse showed deeper color and harder texture, but the ABR stored in the cool warehouse still had soft texture without significant color change. The contents of ??-ecdysone in ABR stored in the two warehouses both gradually decreased and dropped to lower than the limit of 0.030% ruled by China Pharmacopoeia when being stored for up to 27 months. The contents of 5-HMF of ABR stored in the two warehouses both increased and were higher for the sample in the simple warehouse than that in the cool warehouse. CONCLUSION The concept of RTC is put forward and used to study the monthly dynamics of chemical constituents in traditional Chinese medicine during storage for the first time. The physical and chemical indexes of ABR varies during storage. Two years of storage time of ABR is suggested.     

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??OBJECTIVE To discuss the problem of instrumental test method of clarity and degree of opalescence of liquids in the general notice 0902 of China Pharmacopeia(Ch.P)2015, find out the causes and offer solutions. METHODS The test methods of clarity in Ch.P 2015 and European Pharmacopeia (EP) 8.0 were compared, including instrumental types, applicability, sample requirements, and result evaluation. RESULTS The primary opalescent suspension for the instrumental method is the same as the visual method, using the absorbance (A=0.12-0.15) at 550 nm to control the opalescence. Because the resolving power of the instrumental method is far higher than the visual method, the limit becomes interval distribution instead of simple point. The opalescent value (NTU) of the upper limit (A=0.15) is about 1.35 times of the lower limit (A=0.12).When the NTU value of the test liquid is in this interval, the result evaluation will be hard.CONCLUSION The preparation of the primary opalescent suspension in Ch.P 2015 is different from EP8.0. For this reason, the limit set by Ch.P 2015 is actually stricter than that of EP8.0. The opalescent value of the standard solution used by Ch.P 2015 is about 75% of that used by EP8.0.     

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??OBJECTIVE To determine the optimum ultrasonic-assisted extracting process of total flavonoids from Zingiber mioga by response surface methodology, and then study the antioxidant activity of the extract. METHODS On the basis of single factor experiments, a 4-factor, 3-level Box-Behnken center-united experiment was conducted. The Box-Behnken experiment analyzed and optimized the processing conditions by response surface methodology, then the antioxidant activity of the extract was determined. RESULTS The optimum conditions at ultrasonic power of 300 W were as follows treatment temperature 60 ??, ethanol concentration 85.99%, liquid-to-solid ratio 98.08 mL??g^-1, treatment time 15 min. Under the optimum conditions, the extraction rate of the total flavonoids was 37.01%, with a bias of 4.28% compared with the predicted value of 35.49%; the reducing power of the total flavonoids from Zingiber mioga at the concentration of 1.038 7 mg??mL^-1 was equal to that of vitamin C of 56.60 ??g??mL^-1; the ??OH radical scavenging ratio of the total flavonoids from Zingiber mioga was 73.07%, the DPPH radical scavenging ratio was 65.72%, and the inhibition rate of anti-lipid peroxidation was 49.94%. CONCLUSION The total flavonoids from Zingiber mioga can be developed as a new type of antioxidant agents, and regression analysis and parameter optimization of the extracting process can be conducted by using response surface methodology.     

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??OBJECTIVE To design and synthesize brain targeting danshensu (DSS) derivatives and study their metabolism in rat plasma and brain homogenate in vitro. METHODS Tetramethylpyrazine and its derivatives were selected as carriers to design the brain targeting danshen suderivatives. Lipid-water partition coefficient (logP), brain blood concentration ratio (BB), and P-glycoprotein affinity of the derivatives were predicted by some calculation softwares and the better compound DT3 was chosen for the next synthesis. The degradation of DT3 and its intermediate DT1 in rat plasma and brain homogenate were measured by HPLC-UV. RESULTS Two danshensu-pyrazine ester derivatives were synthesized, ie DT1 and DT3. A simultaneous determination method of DT3, DT1, and (3,5,6-trimethylpyrazine-2-yl)methanol (TMPM) in rat plasma and brain homogenate was established. The degradation of DT3 in rat plasma and brain homogenate underwent the following processDT3??DT1??the active metabolites of DSS and TMPM.Compared with DT1, the degradation of DT3 in rat plasma slowed down.The half-lives (t_1/2) of TMPM were 1.68 and 1.71 min, respectively. Also,DT3 could quickly release the active metabolitein rat brain homogenate, and the concentration of TMPM showed a steady increase with a t_1/2 of 222.88 min. CONCLUSION The danshensu-pyrazine ester derivative DT3 has an extended t_1/2 in rat plasma, and it can be degraded to active metabolite quickly in rat brain homogenate.     

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??OBJECTIVE To design and synthesize a series of oleanolic acid analogs posessing anti-tumor activity based on survivin target. METHODS Using the techniques of computer-aided drug design, the docking of Survivin and known active small molecules was simulated and then the key amino acid residue fragment of the target protein was analyzed. It led to the discovery of active groups capable of binding to the critical sites. Through using the natural product, oleanolic acid, as a lead compound, the active groups were introduced onto its A-ring, and the carboxyl group at the C-28 position was modified using amidation. SGC-7901 and A549 cells were used to screen the antitumor activity in vitro through the standard MTT method. RESULTS Ten new oleanolic acid derivatives were designed and synthesized,and their structures were confirmed by MS and NMR. The compounds ??₅ and ??₅ exhibited more potent cytotoxicity than the positive control drugs. CONCLUSION The novel oleanolic acid analogues have better antitumor activity than the parent compound, which are worthy of further study.     

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??OBJECTIVE To develop an LC-MS/MS method for the determination of vonoprazan pyroglutamate and vonoprazan fumarate in rat urine to determince the urine excretion of the two drugs in SD rats. METHODS The detection was performed on an API 4000 tandem mass spectrometer equipped with an electrospray ionization (ESI) source. Multiple reaction monitoring (MRM) was selected with the transitions of m/z 346.2 to 315.2 for TAK-438 P and m/z 237.2 to 194 for IS, respectively. Separation of the analytes was achieved by a Shimadzu liquid chromatography system with an Agelient C₁₈ analytical column (4.6 mm??150 mm, 3.5 ??m). Isocratic elution was adopted with mobile phase A (10 mmol??L^-1 ammonium acetate and 0.1% formic acid) and mobile phase B (methanol) at the ratio of 40??60, at a flow rate of 0.6 mL??min^-1. The total run time was 6 min and the injected sample volume was 5 ??L. All the features of the developed method suggested it met the criteria for bioanalytical METHODS recommended by regulatory authorities. The accumulative urine excretion rates of TAK-438 F and TAK-438 P were determined after oral administration of TAK-438 P and equimolar TAK-438 F in SD rats.RESULTS The accumulative urine excretion rates of the prototype drugs were 2.11% and 2.03%, respectively. The low excretion rates indicated that metabolism might be the major clearance mechanism of TAK-438 P and TAK-438 F. CONCLUSION This was the first time to establish and validate a simple, rapid and sensitive LC-MS/MS method for the quantification of TAK-438 P. There is no significant difference of the accumulative urine excretion rate between TAK-438 P and TAK-438 F in SD rats, which provides the basis for the druggability of TAK-438 P.     

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??OBJECTIVE To evaluate the bioequivalence of cefdinir suspension and reference cefdinir capsule in Chinese healthy male subjects.METHODS A single oral dose of 100 mg cefdinir suspension or cefdinir capsule was given to 24 subjects according to a 2-way crossover design. The plasma concentrations of cefdinir were determined by UPLC-MS/MS. The pharmacokinetic parameters were calculated and bioequivalence was compared by WinNonlin 6.3 program. RESULTS The main pharmacokinetic parameters of cefdinir suspension and cefdinir capsule were as follow: ??_max were (1 034.78??358.17), (969.71??297.38) ng??mL^-1;t_max were (2.98??0.60), (3.44??0.70) h; AUC_0-12 were (4 911.24??1 675.30), (4 522.35??1 600.13) ng??h??mL^-1; AUC_0-?? were (5 026.24??1 735.32),(4 680.69??1 699.93) ng??h??mL^-1;t_1/2 were (1.71??0.23), (1.79??0.39) h. The 90% confidential interval of ??_max, AUC_0-12, AUC_0-?? of tested formulation were 95.6%-115.3%, 99.9%-117.2%, 99.0%-116.0%. CONCLUSION The two formulations are bioequivalent.     

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??OBJECTIVE To prepare ion-sensitive ophthalmic in situ gel containing bendazac lysine (BDZL-ISG) and preliminarily study its rheological behavior, in vitro drug release, corneal permeation, and pharmacokinetics in rabbit aqueous humor. METHODS Single factor investigation was carried out to optimize the formulation, taking viscosity and gelling capacity as evaluation indices. Using aqueous solution or eye drops as control, the in vitro release of the formulation was evaluated by dialysis membrane method. Then, the corneal permeation experiment of the optimum formulation was carried out with Franz diffusion cell. The pharmacokinetics of BDZL-ISG in rabbit aqueous humor was preliminarily studied by microdialysis. RESULTS Compared with the control group, the optimum formulation had shear thinning behavior and significant sustained release effect. There was no significant difference in the corneal permeation between the two groups. The RESULTS of pharmacokinetic study showed that ??_max (13.25 ??g??L^-1) and AUC_0-t of BZDL-ISG were 2.38 and 2.2 times higher than those of BDZL eye drops respectively, which suggested that the ocular bioavailability of BDZL was greatly enhanced by the optimum in situ gel formulation. CONCLUSION With significant sustained release effect, the ion-sensitive ophthalmic in situ gel will become a promising alterative formulation for bendazac lysine for treatment of cataracts.     

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??OBJECTIVE To establish the HPLC fingerprints of Feijiehe pills and provide a foundation for its quality control and evaluation. METHODS A gradient elution method was applied. Ten batches of samples were analyzed by HPLC on a Diamonsil C₁₈ (4.6 mm??250 mm,5 ??m) column with mobile phase composed of acetonitrile-0.01% phosphoric acid solution at a flow rate of 0.8 mL??min^-1, the detection was carried out at 270 nm, and the column temperature was maintained at 25 ??. RESULTS There were 10 common peaks in the HPLC fingerprints. The similarity between peaks was more than 0.90. CONCLUSION The method is simple, accurate, reliable, and suitable to be applied to the quality control of Feijiehe pills.     

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??OBJECTIVE To study the chemical constituents of Noni enzyme (Morinda citrifolia L.) and their antitumor activities. METHODS Compounds were isolated by various chromatographic techniques, including silica gel, TLC, sephadex LH-20, and semi-preparative HPLC, and their structures were identified by their physicochemical properties and ¹H-NMR and ¹³C-NMR data. The in vitro antitumor activities of the isolated compounds were studied by MTT method. RESULTS Sixteen compounds were isolated from Noni enzyme. They were xylogranatinin(1), pelargonic acid(2), 1,5,15-tri-O-methylmorindol(3), sesquipinsapol B(4), (+)-syringaresinol(5), pinonesinol(6), 3-methylhexahydropyrrolopyrazine-1,4-dione(7), (2S)-3??-hydroxybutan-2-yl-2-hydroxypropanoate (8), 3-(sec-butyl)-6-methylpiperazine-2,5-dione(9), cyclo-(L-Pro-L-Leu)(10), gentisic acid(11), vomifoliol(12), scopoletin(13), 3-(2-hydroxy-4,5-dimethoxyphenyl) propanoic acid(14), medioresinol(15), hydroxychavicol(16). CONCLUSION Compounds 1-10, 12 and 14-16 are isolated from Noni enzyme for the first time. Compound 10 displays the stronger cytotoxicity against HepG2 and HeLa cells with an IC₅₀ value of 23.73, 16.55 ??g??mL^-1. Compound 5 had a certain inhibitory activity against HeLa cells with an IC₅₀ value of 47.12 ??g??mL^-1.     

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??OBJECTIVE To study the chemical constituents of Yao medicine, Zhongliuteng, the stems of Pileostegia tomentella. METHODS The chemical constituents were isolated and purified by silica gel chromatography repeatedly, and their structures were identified by spectral analysis and chemical METHODS. RESULTS Thirteen compounds were isolated from the stems of P. tomentella and the structures were identified as 1-O-(??-D-glucosyl)-2-[2-methoxy-4-(??-hydroxypropyl) phenoxy]propan-3-ol(1),(+)-lyoniresinol-3a-O-??-D-glucopyranoside (2),syringin (3),coniferin (4),dihydroconiferin (5),but-3-enyl-??-D-glucoside (6),4-(2,3-dihydroxypropyl)-2,6-dimethoxy phenyl ??-D-glucopyranoside (7),nikoenoside (8),protocatechuic acid ethyl ester (9),8-methoxy coumarin-7-O-??-D-glucopyranoside (10),6-O-R-L-rhamnopyranosyl-??-D-glucopyranoside methyl salicylate (11), nicotinamide (12), and 3,5-di-O-caffeoyl quinicacid methyl ester (13). CONCLUSION All compounds were obtained from the genus for the first time.     

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??OBJECTIVE To study the flavonoid glycosides of Urena lobata. METHODS Compounds were isolated and purified using various column chromatographies such as D101 macroporous adsorption resin, silica gel, Sephadex LH-20, and prep HPLC. Their structures were identified on the basis of their physicochemical properties and various spectroscopic experiments, including HRESIMS, ¹H-NMR, ¹³C-NMR, HSQC, and HMBC. RESULTS Ten flavonoid glycosides were obtained from the n-BuOH extract of U. lobata including quercetin-3-O-??-D-glucopyranosyl-(1??2)-??-D-galactopyranoside(1), kaempferol-3-O-??-D-glucopyranosyl-(1??2)-??-D-glucopyranosyl-7-O-??-L-rhamnopyranoside(2), quercetin-3-O-??-D-apiofuranosyl-(1??2)-??-D-glucopyranosyl-7-O-??-L-rhamnopyranoside(3), kaempferol-4'-O-??-D-apiofuranosyl-3-O-??-D-glucopyranosyl-7-O-??-L-rhamnopyranoside(4), kaempferol-3-O-??-D-apiofuranosyl-(1??2)-??-D-glucopyranosyl-7-O-??-L-rhamnopyranoside(5), quercetin-3-O-??-D-glucopyranosyl-7-O-??-L-rhamnopyranoside(6), quercetin-3-O-??-D-glucopyranosyl-(1??2)-??-D-glucopyranoside(7), kaempferol-3-O-??-L-rhamnopyranosyl-(1??6)-??-D-glucopyranosyl-(1??2)-??-D-glucopyranoside(8), kaempferol-3-O-??-D-glucopyranosyl-(1??2)-[??-L-rhamnopyranosyl-(1??6)]-??-D-glucopyranoside(9) and kaempferol-3-O-??-D-glucopyranosyl-(1??2)-??-D-glucopyranoside(10). CONCLUSION Compounds 1-3 and 6-10 are firstly obtained from U. lobata.     

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??OBJECTIVE To establish an HPLC method for simultaneous determination of ginsenoside Rg₁, Re, Rb₁ and jujuboside A, B in Renshen Jianpi Pellets (RSJPW). METHODS The determination was conducted on an Eclipse XDB C₁₈ column (4.6 mm??250 mm, 5 ??m) with the mobile phase of acetonitrile (A)-water (B) gradiently eluted at the following flow rates:0-90 min, 1.0 mL??min^-1; 90-130 min, 1.0-0.5 mL??min^-1; 130-140 min, 0.5 mL??min^-1. And the column temperature was maintained at 35 ??; the detection wavelength was set at 203 nm. RESULTS The calibration curves of ginsenoside Rg₁, Re, Rb₁ and jujuboside A, B were in good linearity over 0.32-2.24 ??g (r=0.998 2), 0.16-1.12 ??g (r=0.995 3), 0.32-2.24 ??g (r=0.999 6), 0.16-1.12 ??g (r=0.991 5), 0.08-0.56 ??g (r=0.999 6). The corresponding average recovery rates were 97.18%, 97.62%, 98.79%, 98.48%, 94.51%; the standard deviations were 1.10%, 0.98%, 0.34%, 1.09%, 1.88%, respectively. CONCLUSION The established HPLC method is accurate, reliable and reproducible, which can be used as a reference for the quality control of RSJPW.     

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??OBJECTIVE To study the chemical constituents from the stems of Acorus tatarinowii Schott. METHODS The chemical constituents were isolated from the 70% ethanol-soluble extract of the stems of Acorus tatarinowii Schott and purified by a series of column chromatography methods, including MCI, silica gel, Sephadex LH-20, HPLC and so on, and their structures were identified by physical chemical constants and NMR techniques. RESULTS A total of twelve compounds were isolated and identified as(7S,8R)-4,9??-dihydroxyl-3,3??-dimethoxyl-7,8-dihydrobenzofuran-1??-propylneolignan(1),(-)-lyoniresinol(2), dihydrocubebin(3), evofolin B(4),(+)-icariol A₂(5), ??-sitosterol(6),(+)-13-hydroxyspathulenol(7), aromadendrane-4??,10??-diol(8), anomallenodiol(9),(9CI)-cis-4-(3,4-dihydroxy-2,6,6-trimethyl-1-cyclohexen-1-yl)-2-butanone(10),(3E)-rel-4-[(3R,4S)-3,4-dihydroxy-2,6,6-trimethyl-1-cyclohexen-1-yl]-3-buten-2-one(11), and ixerol B(12), respectively. CONCLUSION Compounds 2-4 and 7-12 are isolated from the genus Acorus for the first time, and compound 5 is isolated from this plant for the first time.     

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??OBJECTIVE To study the secondary metabolites of marine-derived fungus Aspergillus fumigatus YK-7. METHODS The compounds were isolated by several column chromatographic techniques, including silica gel, ODS, Sephadex LH-20 column chromatography, and HPLC, and their structures were identified on the basis of physicochemical properties and spectroscopic analysis. Trypan blue and MTT methods were applied for determining the effects of the compounds on proliferation of cancer cells in vitro. RESULTS Ten compounds were obtained, and their structures were identified as pseurotin A (1), pseurotin A₁(2), 14-norpseurotin A (3), FD-838 (4), demethoxyfumitremorgin C (5), 9??-hydroxyverruculogen TR-2 (6), 6-methoxyspirotryprostatin B (7), spiro[5H,10H-dipyrrolo[1,2-a:1??,2??-d]pyrazine-2-(3H),2??-[2H]indole]-3??,5,10(1??H)-trione (8), terezine D (9), and 14-hydroxyterezine D (10). CONCLUSION Compounds 3, 6, 7, 9, and 10 are isolated from marine-derived fungus Aspergillus fumigatus for the first time. Compounds 1-4 exhibite moderate antiproliferative activity against selected cancer cell lines in vitro.     

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??OBJECTIVE To establish an LC-MS/MS method to determine (S)-pantoprazole sodium in dog plasma and investigate its toxicokinetics. METHODS After protein precipitation with acetonitrile, the analyte and internal standard were separated on CHIRALCEL OJ-RH column (4.6 mm ??150 mm, 5 ??m) with acetonitrile-water (28??72) as mobile phase eluted at a flow rate of 0.6 mL??min^-1. Detection was carried out by electrospray positive ionization mass spectrometry in the multiple reaction monitoring (MRM) mode. The MRM transitions of m/z 384.0/199.8 and m/z 180.0/110.0 were used to quantify (S)-pantoprazole sodium and phenacetin, respectively. Beagle dogs were intravenously given (S)-pantoprazole sodium for 4 weeks at low, medium, and high dosages (10, 20, 40 mg??kg^-1??d^-1). RESULTS The calibration curve was linear over the concentration range of 50-30 000 ng??mL^-1. The RSDs were less than 15%, and the accuracy was in the range of 85%-115%. The AUC_{0-4 h} and ??_max of (S)-pantoprazole sodium were proportional to the dosages. CONCLUSION The established method can be applied to the determination of (S)-pantoprazole sodium in plasma of dogs and is suitable for the toxicokinetic study.     

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??OBJECTIVE To study the chemical constituents from the rhizome of Drynaria fortunei and the protective effects of them on PC12 cells induced by A??_25-35. METHODS The compounds were isolated and purified by silica gel, Sephadex LH-20, ODS column chromatography, and their structures were identified on basis of spectroscopic methods, such as MS and NMR. PC12 cells were treated with A??_25-35 to establish the Alzheimer' s disease models. The compounds of different concentrations were added into culture medium to detect the protection. MTT assay was used to detect cell vitality and to observe the protective effects of compounds on PC12 cells induced by A??_25-35. RESULTS Nine compounds were isolated and identified as naringin(1), neoeriocitrin(2), 5,7-dihydroxychromone-7-neohesperidoside(3), (E)-4-O-??-D-glucopyranosyl caffeic acid(4), kaempferol(5), luteolin(6), protocatechoic acid(7), psoralen(8), and ??-sitosterol(9) . The cell experiments were performed on the compounds 1-8 and the results showed they can promote the proliferation of PC12 cells. The cell vitality increase with concentration rising, and the difference is statistically significant (P<0.05). CONCLUSION Compounds 1-8 play an important role in protecting A??_25-35-induced injury in PC12 cells and they are the main active components of Drynaria fortunei in the protection of central nervous function.     

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??OBJECTIVE To study the pharmacokinetics and bioequivalence of hydroxysafflor yellow A (HSYA) and hydroxysafflor yellow A nanoemulsion (HYAN) in rats.METHODS Twelve male rats were randomly divided into two groups. The rats were administered intragastrically with HSYA or HYAN, respectively, and then blood was collected from the venous plexus at different time points. HPLC method was used for the determination of HSYA blood concentration.RESULTS The main pharmacokinetic parameters of HYAN were as follows: the area under curve (AUC_{0-24 h}), peak concentration (??_max), peak time (t_max) and clearance (CL) were (31.56??4.58) mg??L??h^-1, (12.75??2.64) mg??L^-1, (0.83??0.54) h and (1.89??0.93) L??h^-1??kg^-1, respectively. The AUC_{0-24 h}, ??_max and t_max of HYAN increased by 5.49, 10.22 and 2.50 times, respectively, and the CL of HYAN was only 1/4 of that of HSYA. The 90% confidence intervals for AUC_{0-24 h} and ??_max were not within the prescribed range of bioequivalence criteria.CONCLUSION Relative to HSYA, the high plasma concentration and prolonged peak time of HYAN in vivo can significantly improve the oral bioavailability of HSYA. HSYA solution and HYAN are not bioequivalent.     

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??OBJECTIVE To establish a high performance size exclusion chromatography(HPSEC) method for the separation and analysis of polymers in cefotaxime sodium and cefotaxime sodium for injection, and determine the structures of the impurities by LC-MS. METHODS HPSEC was performed by using Sepax SRT SEC-150(7.8 mm??300 mm, 5 ??m)column. The mobile phase was 0.1 mol??L^-1 disodium hydrogen phosphate and 0.1 mol??L^-1 phosphate buffer solution. The flow rate was 0.8 mL??min^-1, the detection wavelength was set at 235 nm, the injection volume was 10 ??L, and the column temperature was maintained at 35 ??. The concentration of polymers was quantified by external standard method. The LC-MS/MSⁿ system conditions were as following: the mobile phase was 20 mmol??L^-1 amonium acetate, the flow rate was 0.8 mL??min^-1, ESI source with positive and negative ion scan was utilized, the scanning range was m/z 200-1 600, and the post-column diversion ratio was 1??4. RESULTS Eight impurity peaks were obtained in total; the resolutions were all greater than 1.5. The linear range of cefotaxime was 1-100 ??g??mL^-1(r=1.000 0). The RSD repeatability was 1.2%(n=6). The limit of detection was 0.2 ??g and the limit of quantitation was 0.4 ??g. Three polymers were identified by LC-MS. CONCLUSION The HPSEC method can be used for the quantitative and qualitative analyses of individual polymer impurities. It is also sensitive for the control of polymers in cefotaxime.