Accumulation of functional metabolites and transcriptomics in postharvest fume-drying and air-drying process in rhubarb.

BACKGROUND: The active component content is an important factor affecting quality of traditional Chinese medicines. The fume-drying process can effectively improve the content of active components in rhubarb, but the accumulation dynamics and molecular mechanisms are not known. In this study, variations in the active components of rhubarb during the drying process were determined, and the most intense changes in the active components were preferred for transcriptome inquiry. RESULTS: The results showed that the accumulation of active ingredients could be significantly promoted in the early stage of fume-drying and air-drying. In particular, the active ingredients increased by 61.57% (from 44.58 to 72.02 mg g-1 ) on the fourth day of fume-drying. A total of 4191 DEGs (differentially expressed genes) were identified by transcriptome analysis when the active components changed significantly. Transcriptome data of different dried rhubarb samples revealed, that the fume-drying process could significantly improve the expression of genes relevant to respiration, phenolic acid, and anthraquinone synthesis pathways in rhubarb, which was more conducive to the synthesis and accumulation of the active components. CONCLUSION: Fume-drying stimulated respiration and secondary metabolite synthesis in rhubarb cells by exerting strong external stress on freshly harvested rhubarb. This study revealed the variations and molecular mechanism of active component accumulation in the rhubarb drying process and might serve as a guide for the development of alternative methods for rhubarb fumigation and drying process. © 2022 Society of Chemical Industry.

Progress of Phototherapy Applications in the Treatment of Bone Cancer.

Bone cancer including primary bone cancer and metastatic bone cancer, remains a challenge claiming millions of lives and affecting the life quality of survivors. Conventional treatments of bone cancer include wide surgical resection, radiotherapy, and chemotherapy. However, some bone cancer cells may remain or recur in the local area after resection, some are highly resistant to chemotherapy, and some are insensitive to radiotherapy. Phototherapy (PT) including photodynamic therapy (PDT) and photothermal therapy (PTT), is a clinically approved, minimally invasive, and highly selective treatment, and has been widely reported for cancer therapy. Under the irradiation of light of a specific wavelength, the photosensitizer (PS) in PDT can cause the increase of intracellular ROS and the photothermal agent (PTA) in PTT can induce photothermal conversion, leading to the tumoricidal effects. In this review, the progress of PT applications in the treatment of bone cancer has been outlined and summarized, and some envisioned challenges and future perspectives have been mentioned. This review provides the current state of the art regarding PDT and PTT in bone cancer and inspiration for future studies on PT.

Label-Free Proteomic Analysis of Smoke-Drying and Shade-Drying Processes of Postharvest Rhubarb: A Comparative Study.

Postharvest processing plays a very important role in improving the quality of traditional Chinese medicine. According to previous studies, smoke-drying could significantly promote the accumulation of the bioactive components and pharmacological activities of rhubarb, but so far, the molecular mechanism has not been studied yet. In this research, to study the molecular mechanisms of postharvest processing for rhubarb during shade-drying and smoke-drying, label-free proteomic analyses were conducted. In total, 1,927 differentially abundant proteins (DAPs) were identified from rhubarb samples treated by different drying methods. These DAPs were mainly involved in response and defense, signal transduction, starch, carbohydrate and energy metabolism, and anthraquinone and phenolic acid biosynthesis. Smoke-drying significantly enhanced the expression of proteins involved in these metabolic pathways. Accordingly, the molecular mechanism of the accumulation of effective ingredients of rhubarb was clarified, which provided a novel insight into the biosynthesis of active ingredients that occur during the rhubarb dry process.

Large-scale isolation and antitumor mechanism evaluation of compounds from the traditional Chinese medicine Cordyceps Militaris.

We established a large-scale separation and purification platform to obtain kilogram amounts of natural compounds from the extraction of the fruiting bodies of C. militaris. Seven monomeric compounds, N6-(2-hydroxyethyl) adenosine (HEA), ergosterol (E), ergosta-7,22-diene-3,5,6-triol (EI), 5α,8α-epidioxy-(22E,24R)-ergosta-6,22-dien-3ß-ol (ED),ergosta-7,22-dien-3ß,5α-dihydroxy-6-one (EO), (20S,22E,24R)-Eegosta-7,22-dien-3ß,5α,6ß,9α-tetraol (ET), and (24S)-5,22-stigmastadien-3ß-ol (SE), were harvested using different solvents, and the structure of each compound was identified. The activities and functions of the isolated compounds were tested by label-free, real-time cell analysis methods at the cellular level, and their antitumor effects were verified using mouse models of Lewis and H22 tumors. The anti-insomnia effect of HEA was tested in an anti-insomnia mouse model. The interactions between E and 8 A549 cell proteins were determined. The biosynthetic pathways of HEA and E, which possess pharmacologically active monomers, were determined. This platform can provide a theoretical basis for the further development and discovery of novel natural medicines.

Advanced High-Performance Potassium-Chalcogen (S, Se, Te) Batteries.

Current great progress on potassium-chalcogen (S, Se, Te) batteries within much potential to become promising energy storage systems opens a new avenue for the rapid development of potassium batteries as a complementary option to lithium ion batteries. The discussion mainly concentrates on recent research advances of potassium-chalcogen (S, Se, Te) batteries and their corresponding cathode materials in this review. Initially, the development of cathode materials for four types of batteries is introduced, including: potassium-sulfur (K-S), potassium-selenium (K-Se), potassium-selenium sulfide (K-Sex Sy ), and potassium-tellurium (K-Te) batteries. Next, critical challenges for chalcogen-based electrodes in devices operation are summarized. In addition, some pragmatic strategies are proposed as well to relieve the low electronic conductivity, large volumetric expansion, shuttle effect, and potassium dendrite growth. At last, the perspectives on designing advanced cathode materials for potassium-chalcogen batteries are provided with the goal of developing high-performance potassium storage devices.

Network Pharmacology Analysis to Uncover the Potential Mechanisms of Lycium barbarum on Colorectal Cancer.

BACKGROUND: Studies have shown that extracts from Lycium barbarum exerted protective effects against colorectal cancer (CRC) cells. We used the network pharmacology method to determine the effects of L. barbarum on CRC and to predict core targets, biological functions, pathways, and mechanisms of action. METHOD: We obtained the active compounds and their targets in L. barbarum via use of the Traditional Chinese Medicine System Pharmacology Database (TCMSP), gathered the CRC targets from Malacards, TTD, GeneCards, and DisGeNET, and chosen the overlapped targets as the candidate targets. After protein-protein interaction (PPI) network analysis, 20 with the highest node degree were selected as the core targets, and their enrichment and pathways were analyzed. Furthermore, we employed iGEMDOCK to validate the compound-target relation. RESULT: Eventually, 103 overlapped targets were chosen as the candidate targets. Targets with the top 20 highest node degree were selected as the core targets. Gene Ontology (GO) enrichment analysis indicated that the core targets were enriched in cell proliferation regulation, extracellular space, cytokine receptor binding, and so on. Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis proved that the core targets were significantly enriched in bladder cancer, pathways in cancer. The docking results demonstrated that beta-sitosterol, glycitein, and quercetin had good binding activity to CRC putative targets. CONCLUSION: Our work successfully predicted the functioning ingredients and potential targets of L. barbarum in CRC and illustrated the potential pathways and mechanisms comprehensively. Nevertheless, these results still call for in vitro and in vivo experiments to validate.

Chemotaxonomic studies of 12 Dioscorea species from China by UHPLC-QTOF-MS/MS analysis.

INTRODUCTION: Dioscorea species, which contain abundant steroidal saponins, have been used as folk medicines or raw materials to synthesise steroid drugs. OBJECTIVE: To establish a rapid chemotaxonomic method that will comprehensively resolve confusions about genetic relationships of genus Dioscorea. METHODS: A comprehensive strategy using ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UHPLC-QTOF-MS/MS) was firstly proposed to evaluate the chemotaxonomy of 12 species (27 taxa) from China by hierarchical cluster analysis (HCA) based on the variations of the identified metabolites. RESULTS: Twenty-eight secondary metabolites (mainly steroidal saponins) were identified. The MSn fragmentation patterns of DA (a new acetylated steroidal saponin at C-7 position) were firstly reported. Moreover, eight major steroidal saponins were further quantified simultaneously by UPLC-QTOF-MS method. According to HCA results, D. bulbifera L. was distinguished with species of sect. Stenophora Uline for pennogenin-type steroidal saponins. Dioscorea zingiberensis exhibited far distance from other members of sect. Stenophora Uline for two unique saponins. Dioscorea banzhuana may be reclassified into sect. Stenophora. Dioscorea nipponica subsp. rosthornii and D. collettii var. hypoglauca might be separated from their original subspecies/varieties as new species, respectively. CONCLUSION: The chemotaxonomic method was successfully applied in the study of genetic relationships of Dioscorea species. This study not only enhanced the understanding of chemical constituents, but also laid basic theoretical foundations for the rational utilisation and chemotaxonomy of genus Dioscorea.

Influence of the drying method on the bioactive compounds and pharmacological activities of rhubarb.

BACKGROUND: Raw rhubarb samples that have been subjected to different drying procedures will have different therapeutic effects, possibly due to processing-induced variations in the chemical composition. In the present work, the fresh materials were processed by smoking, sun-drying, shade-drying and oven-drying at low, moderate and high temperatures. To facilitate the selection of a suitable drying method for rhubarb, the quality of rhubarb processed under various drying conditions was evaluated based on the simultaneous determination of multiple bioactive constituents in combination with bioactivity assays. RESULTS: The total concentrations of 12 compounds in smoked rhubarb were higher than the concentrations of the same components in raw rhubarb and rhubarb products processed using other drying techniques. Smoked rhubarb was found to substantially inhibit Na+ /K+ -ATPase and thrombin. In addition, higher content of anthraquinones led to higher Na+ /K+ -ATPase inhibitory activities, and higher gallic acid content increased the antithrombin capacity. CONCLUSION: The results confirmed that post-harvest fresh plant materials, especially roots, were still physiologically active organs that could undergo series of anti-dehydration mechanisms, including the production of related secondary metabolites during the early stages of dehydration. Therefore, the proper design of drying processes could enhance the quality of rhubarb as well as other similar medicinal plants. © 2018 Society of Chemical Industry.

Novel phenanthrene and isocoumarin from the rhizomes of Dioscorea nipponica Makino subsp. rosthornii (Prain et Burkill) C. T. Ting (Dioscoreaceae).

The investigation of the constituents in the rhizomes of Dioscorea nipponica Makino subsp. rosthornii (Prain et Burkill) C. T. Ting afforded one new phenanthrene 2,2',7,7'-tetramethoxy-[1,1'-biphenanthrene]-4,4',6,6'-tetrol (7) and one new isocoumarin diorosthornoumarin (8), together with 16 known compounds (1-6 and 9-18). Their structures were established on the basis of extensive spectroscopic evidences (IR, HR-ESI-MS, NMR and optical rotation), as well as comparison with literature values. All the compounds 1-18 were firstly isolated from Dioscorea nipponica Makino subsp. Rosthornii (Prain et Burkill) C. T. Ting, and compound 9 was firstly obtained as a natural product from plants, while the compounds 11 and 14 were obtained from both the genus Dioscorea and the family Dioscoreaceae for the first time. Moreover, the antitumor activities of the compounds were tested against lung carcinoma NCI-H460 cell line. Compound 12, 13, 15 and 16 showed significant cytotoxic activities, whereas 7 displayed moderate cytotoxicity.

Study of neuroprotective function of Ginkgo biloba extract (EGb761) derived-flavonoid monomers using a three-dimensional stem cell-derived neural model.

An in vitro three-dimensional (3D) cell culture system that can mimic organ and tissue structure and function in vivo will be of great benefit for drug discovery and toxicity testing. In this study, the neuroprotective properties of the three most prevalent flavonoid monomers extracted from EGb 761 (isorharmnetin, kaempferol, and quercetin) were investigated using the developed 3D stem cell-derived neural co-culture model. Rat neural stem cells were differentiated into co-culture of both neurons and astrocytes at an equal ratio in the developed 3D model and standard two-dimensional (2D) model using a two-step differentiation protocol for 14 days. The level of neuroprotective effect offered by each flavonoid was found to be aligned with its effect as an antioxidant and its ability to inhibit Caspase-3 activity in a dose-dependent manner. Cell exposure to quercetin (100 µM) following oxidative insult provided the highest levels of neuroprotection in both 2D and 3D models, comparable with exposure to 100 µM of Vitamin E, whilst exposure to isorhamnetin and kaempferol provided a reduced level of neuroprotection in both 2D and 3D models. At lower dosages (10 µM flavonoid concentration), the 3D model was more representative of results previously reported in vivo. The co-cultures of stem cell derived neurons and astrocytes in 3D hydrogel scaffolds as an in vitro neural model closely replicates in vivo results for routine neural drug toxicity and efficacy testing. © 2016 American Institute of Chemical Engineers Biotechnol. Prog., 32:735-744, 2016.