Latest ArticlesChemical investigation on the rice culture of an endophytic fungus Colletotrichum fioriniae F18, inhabiting in the stems of the medicinal plant Mahonia fortunei, led to the isolation of nine compounds. They included a new indole alkaloid, makomotindoline B (1), and two known indole derivatives, 3-indoleacetic acid methyl ester (2) and N-acetyltryptamine (3), together with six known aromatic compounds, 2-(4-hydroxyphenyl) acetic acid (4), 4-(2-hydroxyethyl)phenol (5), 2-(4-methoxyphenyl)acetic acid (6), 4-hydroxyphenethyl 2-(4-hydroxyphenyl)acetate (7), regiolone (8) and N-phenethylacetamide (9). The structures of these compounds were elucidated based on the analysis of spectroscopic data including MS and NMR. The absolute configuretion of compound 1 was determined by electronic circular dichroism (ECD) calculation. Antibacterial activity assay indicated that compounds 1-9 had no antibacterial activities against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa, as well as no quorum sensing inhibitory (QSI) activity for Chromobacterium violaceum.
Tripterygium glycosides tablets (TGT) have good immunosuppressive activity, but they can also significantly injure the liver and kidney and its mechanism is unclear. In this study, delayed-type hypersensitivity (DTH) Balb/c mouse were administrated with different doses of TGT. Then the changes of sphingolipids levels in live, kidney and plasma as well as the mRNA expression levels of their metabolic enzymes were studied by the integrated targeted sphingolipidomics and transcriptomics methods to reveal the mechanism of efficacy and toxicity of TGT. It was found that low dose of TGT could significantly decrease levels of total ceramide in the plasma, long chain sphingolipids and saturate sphingolipids in the liver and kidney, but increase them in the plasma, which were related to the efficacy mechanism of TGT. High dose of TGT can significantly increase levels of total ceramide, Cer(d18:1/18:0)-1-P, long chain sphingolipids and decrease saturation sphingolipids mechanism. TGT can also cause significant changes of mRNA expression levels of various sphingolipid metabolic enzymes in the liver and kidney, which were correspond to the changes of sphingolipid levels. The efficacy and toxicity of TGT were related to the regulation of these key enzyme expression levels. In conclusion, the efficacy and toxic mechanism of TGT were closely related to the sphingolipids metabolism. A variety of potential biomarkers were found and they can provide valuable information for the evaluation of the efficacy and toxicity of TGT.
The toxicity of heavy metals and harmful elements is close related to their speciation. In the present study, the methods for mercury and arsenic speciation analysis based on high-performance liquid chromatography conjunction with inductively coupled plasma mass spectrometry (HPLC-ICP-MS) were established and applied to the determination of 31 kinds of animal drugs, 29 of which were included in the Chinese Pharmacopeia (2015 edition). The results showed that the LODs for all the speciation were within 0.1-0.65 μg·kg-1, and the recoveries were within 86.9%-116.6% with the RSD of 1.49%-4.23%. Inorganic mercury (Hg2+) was detected in all the 87 batches of samples that came from 31 kinds of animal drugs, and the contents were 2.39-6567 μg·kg-1. Methylmercury (MeHg) was detected in 33 batches of samples that came from 12 kinds of animal drugs, and the contents were 2.83-319.7 μg·kg-1. Ethylmercury (EtHg) were detected in none of the samples. The detection rates of As(Ⅲ), As(Ⅴ), monomethylarsononous acid (MMA), dimethylarsinic acid (DMA), arsenobetaine (AsB) and arsenocholine (AsC) in the 31 batches of animal drugs was 96.77%, 100%, 45.16%, 90.32%, 93.55% and 22.58%, respectively. According to the toxic level of different speciation, the animal drugs with high risks of mercury were Agkistrodon, Bungarus Parvus, Zaocys, and Scolopendra; the animal drugs with high risks were Pheretima, Agkistrodon, Zaocys, and Aspongopus. This study can provide important evidence for the risk assessment, setting and revision of the limit standards of heavy metals and harmful elements.
An HPLC method was established for the simultaneous determination of saikosaponin a, b2, c, d, e, f of Bupleurum chinense DC. in order to study the content difference of saikosaponins in different producing areas, different harvest time and different processed products of Bupleurum chinense DC. The Agela Venusil MP C18 (4.6 mm×250 mm, 5 μm) column was used with a gradient elution of acetonitrile-water at the wavelength of 210 and 254 nm with the flow rate of 1.0 mL·min-1 and the column temperature at 30℃. Based on the content of six kinds of saikosaponins, the differences of saikosaponins in four producing areas, eight harvest periods and 11 processing methods of Bupleurum chinense DC. were systematically studied. The results showed that the content of saikosaponins in Bupleurum chinense DC. was higher in May and August of Liaoning, Shaanxi and Gansu, but only in August from Shanxi in the four producing areas. The content of saikosaponins in 11 processed products was as follows:raw product > bran-stir-fried product > stir-fried product > wine-moistened product > turtle blood-stir-fried product > bran-wine-stir-fried product > wine-stir-fried product > vinegar-moistened product > turtle blood-wine-stir-fried product > vinegar-stir-fried product > honey-stir-fried product > honeymoistened product.
Timolol maleate cubic nanoparticles (TM-LCNPs) were prepared via fragmentation of a bulk GMO/poloxamer 407 cubic phase gel by high-pressure homogenization. The optimal prescription was selected based on particle size and entrapment efficiency by orthogonal design method. Malvern particle sizer, polarized light microscopy, and differential scanning calorimetry were used to characterize the cubic nanoparticles. Commercial eye drops were used as a control for the release and corneal permeation experiment in vitro. Fluorescence imaging was used to observe the retention of Rhodamine B cubic nanoparticles (RhB-LCNPs) in rabbit cornea. The results indicated that the optimal prescription and preparation of TM-LCNPs was oil-water ratio (7:3), homogenous pressure (900 bar), the number of homogenizations (6) and drug loading (1%). Corneal permeability of TM-LCNPs was significantly higher than that of commercially available eye drops. The residence time in eyes was longer which suggested a sustained release behavior. The pathology result of rabbit corneal after multiple administration of TM-LCNPs showed that there was no apparent damage.
The aim of this study is to apply 3D printing technology to hospital drug dosing operations, and explore its feasibility and scalability. Drugs often dosed in hospitals are selected as models. The commercially available drug was ground into powder, diluted with medicinal excipients and then mixed with 75% ethanol and binder to prepare a paste for 3D printing. The dose and physicochemical properties of divided tablets were controlled by setting print parameters and printing models in computer software. Different 3D printers were employed to evaluate the impact of the device on the dosing tablet. Two drugs were dosed in this study to explore the scalability of 3D printing technology between different drugs. The drug content of the three divided dose tablets (warfarin sodium 1 mg, 2 mg, hydrochlorothiazide 5 mg) was 1.02±0.03, 1.96±0.01, 5.19±0.06 mg. The content uniformity was 1.0, 5.3, 2.6, respectively. The drug dissolution rate was (99.3±1.2)%, (101.5±0.3)%, (98.1±0.8)% in 45, 45 and 30 min. The mechanical properties of the three sub-doses and the stability within 30 days were in line with the Chinese Pharmacopoeia (2015) requirements. At the same time, it was found that the printing parameters and prescriptions can affect the properties of the divided dose tablets. By controlling the dilution ratio of commercial drug and printing parameters, the drug release rate can be customized to achieve individualized treatment. Both different modes of 3D printers can produce qualified sub-doses, and 3D print dispensing technology was also versatile between the two drugs. 3D printing can prepare small-volume, high-precision, high-repetition dosing tablets, with all properties in compliance with pharmacopoeia regulations. Thus, this method can be used as a new and scalable sub-dosing method.
Anthraquinones are not only the main active constituents but also the index components for the quality control of Rhei Radix et Rhizoma. To study the anthraquinone biosynthesis, Rheum palmatum L. seedlings were subjected to a high-throughput transcriptomic sequencing analysis by Illumina HiSeqTM 2000 150PE. The Illumina sequencing generated a total of 11.04 G clean data resulting in 736 309 74 clean reads, deposited in the sequence read archive (SRA accession SRP160030). Trinity do novo assembly yielded 93 646 unigenes, with an average of 1 108 nt. Functional annotation revealed that all unigenes were successfully annotated in the NR, NT, Swiss-port, PFAM, and KOG databases. GO enrichments showed that 57 subgroups were involved in biological process, cellular component, and molecular function. KEGG analysis indicated that 1 107 unigenes were implicated in 19 standard secondary metabolic pathways. 172 unigenes were analyzed to encode 28 key enzymes during the MVA, MEP, shikimic acid, and polyketide pathways related to anthraquinone biosynthesis. 125 CYP450 and 73 UGTs unigenes were related the modification of secondary metabolites in R. palmatum L. Furthermore, seven unigenes with full length cDNAs were successfully verified by RT-PCR and sequencing analyses. Then, MISA prediction produced a number of 18 885 simple sequence repeats (SSRs). Herein, the transcriptomic gene expression profiles of R. palmatum L. and candidate genes during the anthraquinone biosynthesis pathway were obtained for the first time. The results provided basic information for subsequent gene function characterization, secondary metabolic pathway analysis, and anthraquinone biosynthesis and regulation elucidation in R. palmatum L.
Traditional Chinese medicine Baitouweng have a long history of application. The pharmacopoeia included dry roots of Pulsatilla chinensis (Bge.) Regel of Ranunculaceae. There are easily confused species in the market circulation, such as P. cernua (Thunb.) Bercht. et Opiz., P. dahurica (Fisch.) Spreng., P. turczaninovii Kryl. et Serg., and P. chinensis (Bge.) Regel var. kissii (Mandl) S. H. Li et Y. H. Huang, etc. In this study, using the method of metagenomics, based on high-throughput sequencing technology, the ITS2 sequence of mixed samples of five species of Baitouweng medicinal materials was sequenced. First, the total DNA extraction of medicinal materials mixing powder, and the ITS2 fragment of total DNA was amplified by PCR. Second, the Illumina MiSeq platform was used to carry out Paired-end sequencing for DNA fragments. Last, using FLASH, QⅡME and GraPhlAn software to arrange and analyze, and clustering analysis with the sequences of uploaded to GenBank by our group in the early stage. The results showed that a total of 53 024 sequences of ITS2 were obtained from the mixed samples, there are 52 295 effective sequences, there are a total of 49 079 of five species of medicinal materials of P. Miller. After the representative sequences and the sequence of uploaded to GenBank by our group in the early stage were clustering analysis, 5 species of Baitouweng medicinal materials were clustered into one branch separately, presenting monophyletic. The results showed that using the high-throughput sequencing technology, using ITS2 sequence as DNA barcode, the mix powder of 5 species of Baitouweng medicinal materials could be effectively identified. It provides a new method and thought for the origin identification of mixed Chinese medicinal materials.
Depression is currently the most popular disease in the world with a high suicide rate. Selective 5-HT reuptake inhibitors have been used as first-line drugs in clinics, but the therapeutic effect is greatly limited. The pathogenesis of depression is complicated, meanwhile the cholinergic hypothesis has received more and more attention. A large number of clinical and preclinical studies have shown that antagonists and partial agonists acting on nicotinic acetylcholine receptors have a significant effect on antidepressant therapy, which can improve the hippocampus recognizes, influence rewards and anxiety systems controlled by the ventral midbrain and ventral tegmental area, and regulate the amygdala pressure system, thereby improving mood and relieving depression. At present, the relationship between the cholinergic system and depression is still undergoing a lot of research. In this article, the relationship between α4β2 nicotinic acetylcholine receptor (nAChRs) and depression is reviewed to provide a reference for study of new anti-depression drugs.
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