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Transcriptional reprogramming contributes to the progression and recurrence of cancer. However, the poorly elucidated mechanisms of transcriptional reprogramming in tumors make the development of effective drugs difficult, and gene expression signature is helpful for connecting genetic information and pharmacologic treatment. So far, there are two gene-expression signature-based high-throughput drug discovery approaches: L1000, which measures the mRNA transcript abundance of 978 “landmark” genes, and high-throughput sequencing-based high-throughput screening (HTS2); they are suitable for anticancer drug discovery by targeting transcriptional reprogramming. L1000 uses ligation-mediated amplification and hybridization to Luminex beads and highlights gene expression changes by detecting bead colors and fluorescence intensity of phycoerythrin signal. HTS2 takes advantage of RNA-mediated oligonucleotide annealing, selection, and ligation, high throughput sequencing, to quantify gene expression changes by directly measuring gene sequences. This article summarizes technological principles and applications of L1000 and HTS2, and discusses their advantages and limitations in anticancer drug discovery.

Basing on chromatographic separation techniques, fifteen aglycones (1–15), including two new anthraquinone aglycones (1, 2) and thirteen known compounds (3–15), were isolated from the small polar fraction of Cassia obtusefolia (petroleum ether extract). Structural elucidations were performed by 1D/2D NMR spectroscopy and mass spectrometry. The in vitro antioxidant and α-glucosidase inhibitory activities of these fifteen compounds were determined. Except compounds 12 (IC50 3.03 ± 0.31 μg/mL, stronger than ascorbic acid, which IC50 was 6.48 ± 2.30 μg/mL) and 13 (IC50 78.40 ± 2.39 μg/mL), the free radical scavenging capacities of other compounds were weak. Compounds 4, 5, 6 and 13 exhibited inhibitory activities on α-glucosidase with IC50 values of 50.60 ± 1.10, 22.57 ± 0.07, 60.09 ± 1.40, and 80.01 ± 2.66 μg/mL separately, however, all the α-glucosidase inhibitory activities were weaker than positive control (acarbose).

Andrographis Herba (AH), the dry aerial segments of Andrographis paniculata (Burm.f.) Nees, is a common herbal remedy with bitter properties in traditional Chinese medicine (TCM) theory. Although bitterness is one of the features representing Chinese medicine, it has not been implemented as an index to assess the quality and efficacy of TCM because of peoples&rsquo, subjectivity to taste. In this study, 30 batches of AH with different commercial classifications (leaves, stems, or mixtures of both) were collected. Bitterness of AH was quantified by electronic tongue technology. Meanwhile, chemical compositions were characterized through establishing high-performance liquid chromatography fingerprints. The result indicated that the radar curves of the bitterness from different AH commercial classifications displayed different taste fingerprint information. Based on six taste factors, a Principal Component Analysis (PCA) score three-dimensional (3D) plot exhibited a clear grouping trend (R2X, 0.912, Q2, 0.763) among the three different commercial classifications. Six compounds (Peaks 2, 3, 4, 6, 7, 8) with positive correlation to bitterness were discovered by a Spearman correlation analysis. Peaks 2, 6, 7, 8 were identified as andrographolide, neoandrographolide, 14-deoxyandrographolide, and dehydroandrographolide, respectively. The electronic tongue can be used to distinguish AH samples with different commercial classifications and for quality evaluation.

Ethnopharmacological relevance Magnoliae Officinalis Cortex (the dried bark of Magnolia officinalis), a widely used traditional Chinese medicine, is also known as ‘Houpo’ (Chinese: 厚朴). Magnoliae Officinalis Cortex has a wide range of pharmacological effects and has been used to treat conditions such as abdominal distention, vomiting, diarrhea, food accumulation, Qi stagnation, constipation, phlegm and fluid retention and cough resulting from asthma. Aims of the review The present paper reviews advances in research relating to the botany, ethnopharmacology, phytochemistry, pharmacology and toxicology of Magnoliae Officinalis Cortex. Prospects for future investigation and application of this herb are also discussed. Materials and methods Information on Magnoliae Officinalis Cortex was obtained from published materials, including ancient and modern books; PhD and MSc dissertations; monographs on medicinal plants; the pharmacopoeia of different countries and electronic databases, such as SCI finder, PubMed, Web of Science, ACS, Science Direct, Wiley, Springer, Taylor, AGRIS, Europe PMC, EBSCO host, CNKI, WanFang DATA, J-STAGE and Google Scholar. Results More than 200 chemical compounds have been isolated from Magnoliae Officinalis Cortex, including lignans, phenylethanoid glycosides, phenolic glycosides, alkaloids, steroids and essential oils. The plant has been reported to have pharmacological effects on the digestive system, nervous system and cardiovascular and cerebrovascular systems, as well as antibacterial, anti-tumour, analgesic, anti-inflammatory and anti-oxidative effects. Conclusions Magnoliae Officinalis Cortex is an essential traditional Chinese medicine with pharmacological activities that mainly affect the digestive system, nervous system and cardiovascular and cerebrovascular systems. This review summarises its botany, ethnopharmacology, phytochemistry, pharmacology and toxicology. These information suggest that we should focus on the development of new drugs related to Magnoliae Officinalis Cortex, including specific constituents, so that Magnoliae Officinalis Cortex can exert greater therapeutic potential. Meanwhile, it is important to pay attention to the rational use of Magnolia resources, avoiding over-harvesting which could lead to lack of resources. We should also pursue research on Magnolia substitutes and develop resources such as Magnoliae Officinalis Flos and Magnolia Leaf.

Ethnopharmacological relevance Trichosanthis Fructus (ripe fruits of Trichosanthes kirilowii Maxim. and Trichosanthes rosthornii Harms) is an essential traditional Chinese medicine to treat thoracic obstruction, angina, cardiac failure, myocardial infarction, pulmonary heart disease, some cerebral ischaemic diseases, etc. The present report reviews the advancements in research on the botany, traditional uses, phytochemistry and pharmacology of Trichosanthis Fructus. Finally, perspectives on future research and its possible directions are discussed. Aim of the study This review provides up-to-date information about the botany, traditional uses, phytochemistry, pharmacology, toxicity and quality control of Trichosanthis Fructus and discusses the perspectives on future research and possible directions of this traditional Chinese Medicine and its origin plants. Materials and methods The information on Trichosanthes kirilowii Maxim. and Trichosanthes rosthornii Harms was collected from published scientific materials, including books; monographs on medicinal plants; pharmacopoeia and electronic databases such as SCI finder, PubMed, Web of Science, ACS, Science Direct, Wiley, Springer, Taylor, CNKI and Google Scholar. Results Approximately 162 compounds, including terpenoids, phytosterols, flavonoids, nitrogenous compounds and lignans, have been isolated and identified from Trichosanthes kirilowii Maxim. and Trichosanthes rosthornii Harms. Numerous studies have shown that the extracts and compounds isolated from these two plants exhibit pharmacological activities, including protection against myocardial ischaemia, calcium antagonist, endothelial cell protection, anti-hypoxic, anti-platelet aggregation, expectorant, anti-inflammatory, cytotoxic and antioxidant. Conclusions Trichosanthis Fructus is an essential traditional Chinese medicine with pharmacological activities that mainly affect the cardiovascular system. This review summarises its botany, traditional uses, phytochemistry and pharmacology. Future research is needed to clarify the different uses of the seeds, pericarps and fruits. Quality control of investigations of the fruits should be improved, and the potential uses of the flesh, leaves and twigs should be further explored.