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(±)-Dimercochlearlactones A−J (1–10), ten pairs of novel meroterpenoid dimers and one known spirocochlealactone A (11), were isolated from Ganoderma mushrooms. The structural elucidation of new compounds, including their absolute configurations, depends on spectroscopic analysis and electronic circular dichroism (ECD) calculations. Biological studies showed that (+)- and (–)-2, (–)-3, and (+)- and (–)-11 are cytotoxic toward human triple negative breast cancer (TNBC) cells (MDA-MB-231) with IC50 values of 28.18, 25.65, 11.16, 8.18, and 13.02 μM, respectively. Wound healing assay revealed that five pairs of meroterpenoids (±)-5−(±)-8 and (±)-10 could significantly inhibit cell mobility at 20 μM in MDA-MB-231 cells. The results provide a new insight into the biological role of Ganoderma meroterpenoids in TNBC.

Additional file 1.

The 2019 novel coronavirus (2019-nCoV) causes novel coronavirus pneumonia (NCP). Given that approved drug repurposing becomes a common strategy to quickly find antiviral treatments, a collection of FDA-approved drugs can be powerful resources for new anti-NCP indication discoveries. In addition to synthetic compounds, Chinese Patent Drugs (CPD), also play a key role in the treatment of virus related infections diseases in China. Here we compiled major components from 38 CPDs that are commonly used in the respiratory diseases and docked them against two drug targets, ACE2 receptor and viral main protease. According to our docking screening, 10 antiviral components, including hesperidin, saikosaponin A, rutin, corosolic acid, verbascoside, baicalin, glycyrrhizin, mulberroside A, cynaroside, and bilirubin, can directly bind to both host cell target ACE2 receptor and viral target main protease. In combination of the docking results, the natural abundance of the substances, and botanical knowledge, we proposed that artemisinin, rutin, glycyrrhizin, cholic acid, hyodeoxycholic acid, puerarin, oleanic acid, andrographolide, matrine, codeine, morphine, chlorogenic acid, and baicalin (or Yinhuang Injection containing chlorogenic acid and baicalin) might be of value for clinical trials during a 2019-nCov outbreak.

Hepatocellular carcinoma (HCC) is a major threat to human health worldwide and development of novel antineoplastic drug is demanding task. BRM270 is a proprietary combination of traditional medicinal herbs, has been shown to be effective against a wide range of stem-like cancer initiating cells (SLCICs). However, the underlying mechanism and antitumor efficacy of BRM270 in human hepatocellular carcinoma (HCC) cells have not been well elucidated till date. Here we studied the tumoricidal effect of BRM270 on human-CD133+ expressing stem-like HepG-2 and SNU-398 cells. Gene expression profiling by qPCR and specific cellular protein expressions was measured using immunocytochemistry/western blot analysis. In vivo efficacy of BRM270 has been elucidated in the SLCICs induced xenograft model. In addition, 2DG-(2-Deoxy-d-Glucose) optical-probe guided tumor monitoring was performed to delineate the size and extent of metastasized tumor. Significant (P

Supplemental material, Supplementary data, for New Unsaturated Lactones and a Meroterpenoid from Ganoderma lucidum by Qi-Hang Xin, Qi Luo, Ze-Hong Wu, Jiao-Jiao Zhang, Li-Zhong Liu, and Yong-Xian Cheng in Natural Product Communications

Two new mertoterpenoids, australins A (1) and B (2), and a new alkaloid, australine (4), together with five known compounds (3, 5���8) were isolated from the fruiting bodies of Ganoderma australe. Their structures including absolute configurations were assigned by using spectroscopic methods and electronic circular dichroism (ECD) calculations. Racemic australin A was further purified by chiral HPLC. Biological assessments reveal that compounds (+)-1 and 7 could significantly protect SH-SY5Y cells from glutamate-induced neural excitotoxicity.

The athletic abilities of the horse serve as a valuable model to understand the physiology and molecular mechanisms of adaptive responses to exercise. We analyzed differentially expressed genes in triceps brachii muscle tissues collected from Eonjena Taeyang and Jigusang Seryeok Thoroughbred horses and their co-expression networks in a large-scale RNA-sequence dataset comparing expression before and after exercise. High-quality horse transcriptome data were generated, with over 22 million 90-bp pair-end reads. By comparing the annotations, we found that MYH3, MPZ, and PDE8B genes in Eonjena Taeyang and PDE8B and KIF18A genes in Jigusang Seryeok were upregulated before exercise. Notably further, we observed that PPP1R27, NDUFA3, TNC, and ANK1 in Eonjena Taeyang and HIF1A, BDNF, ADRB2, OBSCN, and PER3 in Jigusang Seryeok have shown upregulation at the postexercise period. This investigation suggested that genes responsible for metabolism and oxidative phosphorylations associated with endurance and resistance exercise were highly expressed, whereas genes encoding structural proteins were generally suppressed. The expression profile of racehorses at pre- and postexercise will provide credible reference for further studies on biological effects such as responses to stress and adaption of other Thoroughbred horse, which might be useful for selective breeding for improvement of traits in commercial production.

Tumor initiating cancer stem-like cells (TICSCs) have recently become the object of intensive study. Human-Lipocalin-2 (hLCN2) acts as a biomarker for cancers. The aim of the present study was to explore new insights regarding the potential role of LCN2 in inducing epithelial to mesenchymal transition (EMT) by transfecting LCN2 into CD133+-A549-TICSCs and its cross-talk with the NF-κB signaling pathway in adenocarcinoma of the lung. Furthermore, EMT was confirmed by transcriptomic analysis, immunoblotting and immunocyto/histochemical analyses. Tumorigenesis and metastasis were confirmed by molecular therapeutics tracer 2DG infrared optical probe in BALB/cSIc-nude mice. It was observed that the CD133+-expressing-LCN2-A549 TICSCs population increased in adenocarcinoma of the lung compared to the normal lung tissue. The expressions of genes involved in stemness, adhesion, motility and drug efflux was higher in these cells than in their non-LCN2 expressing counterparts. The present study revealed that elevated expression of LCN2 significantly induced metastasis via EMT. Overexpression of LCN2 significantly increased stemness and tumor metastasis by modulating NF-κB cellular signaling. BRM270, a novel inhibitor of NF-κB plays a significant role in the EMT reversal. BRM270, a naturaceutical induces cell shrinkage, karyorrhexis and programmed cell death (PCD) which were observed by Hoechst 33342 staining while flow cytometry analysis showed significant (P

This study investigated the capacity of 10 μM 17β-estradiol to inhibit immature boar Sertoli cell (SC) proliferation and the involvement of microRNA (miR)-1285 in this process. SC viability and cell cycle progression were investigated using a cell counting kit-8 and flow cytometry, respectively. Expression of AMP-activated protein kinase (AMPK), S phase kinase-associated protein 2 (Skp2), and miR-1285 was analyzed by real-time RT-PCR and Western blotting. 17β-Estradiol (10 μM) reduced SC viability and miR-1285 expression and promoted AMPK phosphorylation. A double-stranded synthetic miR-1285 mimic promoted SC viability, increased levels of ATP, and phosphorylated mammalian target of rapamycin (mTOR) and Skp2 mRNA and protein, whereas p53 and p27 expression decreased, and 17β-estradiol-mediated effects on SCs were significantly attenuated. A single-stranded synthetic miR-1285 inhibitor produced the opposite effects on these measures. Activation of AMPK inhibited SC viability, reduced levels of ATP, phosphorylated mTOR and Skp2 mRNA and protein, and increased p53 and p27 expression. An AMPK inhibitor (compound C) attenuated the effects of 17β-estradiol on SCs. This indicated that 17β-estradiol (10 μM) reduced SC proliferation by inhibiting miR-1285 and thus activating AMPK. Phosphorylated AMPK is involved in the regulation of 17β-estradiol-mediated inhibition of SC viability through increasing p53 and p27 expression and inhibiting mTOR and Skp2 expression. Our findings also implicated Skp2 as the downstream integration point of p53 and mTOR. These findings indicated that miR-1285 may represent a target for the manipulation of boar sperm production.

Through analysis, it is believed that major reasons for default risks in operation of small amount credit include low management level and vacancy of normative system, vacancy of risk sharing mechanism, rating distortion due to imperfect credit investigation system, and uncertainty of borrower's credit. On the basis of these, static and dynamic models are established to analyze the prevention mechanism for default risk in small amount credit. It is concluded that we must establish a restriction mechanism during operation of small amount credit as long as three values increase, namely, N (potential loss of bad credit record due to farmers' default) , Q (probability of successful recovery by small amount credit institution) , and S (cost of small amount credit institution punishing farmers after successful recovery). Finally, following countermeasures and suggestions are put forward: perfect laws and regulations and credit reward and punishment mechanism for risk management of small amount credit; bring into play proper function of loan officer in small amount credit practice; widely promote rural Group Credit Union system.

Through analysis, it is believed that major reasons for default risks in operation of small amount credit include low management level and vacancy of normative system, vacancy of risk sharing mechanism, rating distortion due to imperfect credit investigation system, and uncertainty of borrower's credit. On the basis of these, static and dynamic models are established to analyze the prevention mechanism for default risk in small amount credit. It is concluded that we must establish a restriction mechanism during operation of small amount credit as long as three values increase, namely, N (potential loss of bad credit record due to farmers' default) , Q (probability of successful recovery by small amount credit institution) , and S (cost of small amount credit institution punishing farmers after successful recovery). Finally, following countermeasures and suggestions are put forward: perfect laws and regulations and credit reward and punishment mechanism for risk management of small amount credit; bring into play proper function of loan officer in small amount credit practice; widely promote rural Group Credit Union system.

Japanese quail (Coturnix coturnix japonica) reach sexual maturity earlier, breed rapidly and successfully, and cost less and require less space than other birds raised commercially. Given the value of this species for food production and experimental use, more studies are necessary to determine chromosomal regions and genes associated with gender and breed-differentiation. This study employed Trinity and edgeR for transcriptome analysis of next-generation RNA-seq data, which included 4 tissues obtained from 3 different breeding lines of Japanese quail (random bred control, heavy weight, low weight). Differentially expressed genes shared between female and male tissue contrast groups were analyzed to identify genes related to sexual dimorphism as well as potential novel candidate genes for molecular sexing. Several of the genes identified in the present study as significant sex-related genes have been previously found in avian gene expression analyses (NIPBL, UBAP2), and other genes found differentially expressed in this study and not previously associated with sex-related differences may be considered potential candidates for molecular sexing (TERA, MYP0, PPR17, CASQ2). Additionally, other genes likely associated with neuronal and brain development (CHKA, NYAP), as well as body development and size differentiation (ANKRD26, GRP87) in quail were identified. Expression of homeobox protein regulating genes (HXC4, ISL1) shared between our two sex-related contrast groups (Female Brain vs. Male Brain and Ovary vs. Testis) indicates that these genes may regulate sex-specific anatomical development. Results reveal genetic features of the quail breed and could allow for more effective molecular sexing as well as selective breeding for traits important in commercial production.

A structural stable crystalline analogue of α-graphyne is predicted by an efficient semi-empirical Hamiltonian scheme based on quantum mechanics. This analogue can be derived by substituting carbon atoms in six corners of α-graphyne with Ge atoms, which is referred to as α-CGeyne. We investigate the structure stability, electronic and thermodynamic properties of this analogue, and the calculations indicate that the most stable structure is a hexagonal honeycomb planar structure with a lattice constant of 8.686 Å. This material is a semiconductor with a band gap of 1.078 eV and it can keep intact until 2280 K and recovers to its initial structure through quenching.

A study to shed light on the existence of silicon-graphdiyne as well as their stability, structural and other properties, has been carried out using an efficient semi-empirical Hamiltonian scheme based on quantum mechanics. Its most stable structure is a single planar structure with a lattice constant of 12.251 Å. The system occurs structural phase transition at 1520 K. When the temperature is above 1520 K, the basic structure will be destroyed, While the temperature is below 1520 K, the system can restore its initial structure. It is found that sp hybridization exists between Si and C atoms in this conjugated structure. The study of pair distribution function shows that sp bond length is about 1.58 Å. The sp hybridization would gradually transform into other forms of hybridization at high temperatures. Our calculation indicates that delocalized π-bonds exist in this system and all the lengths of Si-C bonds tend to be more uniform. The energy gap is 1.416 eV. LUMO and HOMO energy levels are 0.386 eV and –1.03 eV respectively. It is found that the silicon-graphdiyne should be n-type material.