Objective: The so-called granules for prescription have been developed about 20 years ago as a new form of modernizing and simplification of the classical decoction common in Traditional Chinese Medicine (TCM) practice. Due to actual problems in Germany/Europe, which are caused by the lack of quality monographs and judicial classification of granules for prescription, the aim of the study was a comparison of the chemical composition of commercial granules versus decoctions. Taking an example, decoctions, commercial granules, and organic extracts of two well-established TCM herbal drugs, Scrophulariae Radix and Xanthii Fructus, were examined in their specific composition. Methods: Using high-performance thin-layer chromatography (HPTLC) for fingerprint analysis of different batches of herbal drugs and samples from various suppliers of Xanthii Fructus and Scrophulariae Radix were critically examined. The decoctions were prepared according to traditional rules, while the granules were dissolved in water in accordance with actual regulations. Furthermore, organic extracts of the plant material were examined and compared with aqueous extracts. Results: It could be demonstrated, that in some cases, there are remarkable differences in the specific composition between granules from different suppliers, the classical aqueous decoction and the organic extract used for the HPTLC fingerprinting. On the other hand, few examples exist for good comparability of decoctions and commercial granules. Conclusion: After critical evaluation of the above results, it can be questioned, if there is a so-called phytoequivalence between decoctions and commercial granules for prescription used in TCM practice.

Background: Artemisinin dimer oxime – dimer molecule synthesized from artemisinin possesses high bioavailability and marked in vitro anticancer activities against solid tumor-derived cell lines, endothelial cell proliferation, migration, and angiogenic processes. Numerous murine models have been developed to study human cancer. The most widely used models are the human tumor xenograft mouse model. Materials and Methods: In this study, human tumor cells (NCI-H640, 1 × 10⁷ in 100 μL) are implanted subcutaneously, or 1 × 10⁷ in 50 μL in the thoracic cavity, in athymic nude mice (nu/nu). The implanted cells were allowed to grow for 10 days before initiation of drug treatment (dimer oxime and topotecan, ip). Tumor volume and thoracic/body weight ratio were recorded. Results: We successfully established subcutaneous and thoracic xenografts with human nonsmall cell lung cancer cell line xenografts in athymic nude mice in only 10 days. Using these models, we attempted treatment of xenografts with topotecan – a known anticancer drug and artemisinin dimer oxime or combination of these two drugs. Combination therapy showed a significant reduction in tumor volume and tumor/body weight. Treatments with combination of topotecan and dimer oxime resulted in the reduced mortality rates in comparison with untreated mice. Conclusions: Xenograft tumor models are useful for preclinical screening of new pharmacophores. From this preliminary study, it appears that combination of dimer oxime and topotecan may be used as chemotherapeutic agents against nonsmall cell lung cancer. Further studies are needed to evaluate other combination treatment regimens as well as the mechanism(s) of action.

Objective: To clone and investigate two dehydrodolichyl diphosphate synthase genes of Tripterygium wilfordii by bioinformatics and tissue expression analysis. Materials and Methods: According to the T. wifordii transcriptome database, specific primers were designed to clone the TwDHDDS1 and TwDHDDS2 genes via PCR. Based on the cloned sequences, protein structure prediction, multiple sequence alignment and phylogenetic tree construction were performed. The expression levels of the genes in different tissues of T. wilfordii were measured by real-time quantitative PCR. Results: The TwDHDDS1 gene encompassed a 873 bp open reading frame (ORF) and encoded a protein of 290 amino acids. The calculated molecular weight of the translated protein was about 33.46 kDa, and the theoretical isoelectric point (pI) was 8.67. The TwDHDDS2 encompassed a 768 bp ORF, encoding a protein of 255 amino acids with a calculated molecular weight of about 21.19 kDa, and a theoretical isoelectric point (pI) of 7.72. Plant tissue expression analysis indicated that TwDHDDS1 and TwDHDDS2 both have relatively ubiquitous expression in all sampled organ tissues, but showed the highest transcription levels in the stems. Conclusions: The results of this study provide a basis for further functional studies of TwDHDDS1 and TwDHDDS2. Most importantly, these genes are promising genetic targets for the regulation of the biosynthetic pathways of important bioactive terpenoids such as triptolide.

Objective: Anthraquinone (AQ), a major bioactive component of the traditional Chinese medicine HeShouWu, has widespread applications in industry and medicine. The objective of the current study is to explore the differences in the bioavailability of anthraquinones in vivo and the metabolism in liver microsomes. Materials and Methods: In vivo, we used a reliable UPLC-ESI-QqQ-MS/MS method to measure seven AQ compounds in the jugular vein plasma of rats following oral administration of HeShouWu. Furthermore, in order to quantify the bioavailability of AQs in vivo and to further understand the metabolism of these compounds, we compared the in vitro metabolism of AQ in different species with respect to metabolic profiles, the enzymes involved, and catalytic efficiency using liver microsomes from human (HLM), mouse (MLM), rat (RLM), and beagle dog (DLM). Results: We identified two metabolic pathways, including the hydroxylation and glucuronidation of AQ, in the liver microsomes of humans and other species using UPLC-ESI-Q-TOF. We found that substitutions on the AQ ring were crucial to the activity and regioselectivity of its hydroxylation. In general, hydroxylation activity decreased greatly with β-COOH (rhein) and enhanced dramatically with β-OH (emodin). We also found that glucuronidation of the compound emodin-8-O-β-D-glucoside acts as the main isoform in AQ hydroxylation in HLM and DLM. Total microsomal intrinsic clearance values for AQ were greatest in mouse microsomes, followed by those in dog, human, and rat microsomes. Conclusion: The absorption of different anthrquinone compounds varied based on the compound structure, the metabolism types and products of anthraquinones in liver microsomes were different in different species. These findings provide vital information for a deeper unuunderstanding of the metabolism of AQs.

Objective: Our aim was to investigate the correlation between free fatty acid (FFA) spectrum, blood stasis (BS) score, and macroangiopathy in type 2 diabetic patients with or without BS, as well as the possible relationship between BS and lipotoxicity. Methods: A total of 50 type 2 diabetes (T2D) patients with or without BS were enrolled from June to December 2014 in Shenzhen Traditional Chinese Medicine (TCM) Hospital, with 25 patients allocated to each of two groups. Basic information, BS score, blood glucose, blood lipids, etc., were measured for each patient. In addition, we tested the levels of interleukin (IL)-6, tumor necrosis factor α (TNF-α), and IL-18 with enzyme-linked immunosorbent assay. The macroangiopathy status of patients in the two groups was examined by color ultrasound and all factors related to BS scores were analyzed. Gas chromatography-mass spectrometry was used to explore the difference in the serum FFA spectra between the two different groups. In addition, the relationship between FFA spectra, BS scores, and macroangiopathy was analyzed. Results: BS scores, total cholesterol (TC), total triglyceride (TG), low-density lipoprotein cholesterol, IL-6, TNF-α, IL-18, carotid and femoral artery plaque, carotid intima-media thickness, carotid plaque area, and femoral artery plaque area were all significantly increased in T2D patients with BS syndrome (P < 0.05). A positive correlation was observed between age, duration of diabetes, carotid intima-media thickness, carotid plaque area, femoral artery plaque area, and BS score (P < 0.05). A total of 21 fatty acids were found in the serum, and total FFA (TFFA), saturated fatty acid (SFA), lauric acid (C12:0), palmitic acid (16:0), stearic acid (C18:0), arachidonic acid (C20:4n6), behenic acid (C22:0), and lignoceric acid (C24:0) scores were all found to contribute to the difference between FFA spectrums of the two groups; of the fatty acids, C12:0, C16:0, C18:0, C22:0, TFFA, and SFA positively correlated with BS scores as evaluated by Pearson's or Spearman's correlation analysis (P < 0.05). Only SFA entered the regression equation in the multiple linear regression analysis. C12:0, C16:0, C18:0, C20:4n6, TFFA, and SFA were positively correlated with carotid plaque area, whereas linoleic acid (C18:3n3), Cis-5, 8, 11, 14, and 17-eicosapentaenoic acids (C20:5n3) were negatively correlated (P < 0.05). C16:0 was positively correlated with the femoral artery plaque area and C18:3n3, cis-4, 7, 10, 13, 16, and 19-docosahexaenoic acids (C22:6) and nervonic acid were negatively correlated (P < 0.05). Conclusion: Serum FFA spectra were significantly different between T2D patients with BS and those without, and long-chain SFA made the greatest contribution. Serum FFA spectra were correlated with BS scores and diabetic macroangiopathy, which means that lipotoxicity and BS are correlated in T2D.