Anthocyanin is a water-soluble flavonoid pigment which is widely found in plants. Studies showed that anthocyanin had protective effect on vision. However, whether anthocyanin has therapeutic effect on cataract remain unclear. In this study, we established the age-related and posterior capsule opacification cataract cell models through inducing oxidative damage of human lens epithelial cells (HLECs) by H₂O₂ and inducing epithelial-mesenchymal transition (EMT) by transforming growth factor β₂ (TGF-β₂). The preventative effects of anthocyanin on markers of oxidative damage and EMT were determined by respective assay kits and PCR analysis. Anthocyanin was beneficial to reduce oxidative stress of HLECs, protecting cells from H₂O₂ induced damage and increasing α-crystallin expression. The potential mechanisms might be that anthocyanin increased the activities of SOD and GSH-Px, which contributes to reduce cellular ROS and MDA level. Besides, anthocyanin inhibited Ca²⁺ overload, which contributes to protection of cell from apoptosis. Meanwhile, anthocyanin had inhibitory effect on EMT, slowed down cell proliferation, migration caused by TGF-β₂ through decreasing mRNA expression levels of EMT markers including COL1A1, COL1A2, COL3, COL4, Fn and α-SMA. The results suggest that anthocyanin could protect HLECs from oxidative damage induced by H₂O₂ and cell proliferation, migration and EMT induced by TGF-β₂, which indicated that anthocyanin may have protective and therapeutic effects on age-related cataract and posterior capsule opacification.

This study was designed to construct a "drug-core target-pathway" network of Erzhi Pill for hepatic injury treatment in an effort to explore the "multi-components, multi-targets, multi-pathways" mechanism. ADME/T calculation method was used to screen the active components of Erzhi Pill, and then predict the potential targets according to the reverse pharmacophore matching method. Biological information annotation databases (DAVID) was used to analyze the molecular function and biological process of the action targets. The Cytoscape software was used to construct the "ingredient-core target-pathway" network of Erzhi Pill for hepatic injury treatment. It was found that 39 major active ingredients of Erzhi Pill regulated 321 targets (HRAS, DCK, HSD17B1, UCK2, et al) and affected 51 pathways, such as insulin signaling pathway, FoxO signaling pathway, metabolic pathways and glycolysis/gluconeogenesis. The method revealed the action features of traditional Chinese medicine as multi-ingredients, multi-targets, multi-pathways, providing new clues for further basic study on the hepatic injury pharmacological mechanism of Erzhi Pill.

The impact of Rg1 in the disease progress and pathology of amyotrophic lateral sclerosis (ALS) was investigated in mouse model (SOD1 G93A). Body weight and survival rate were monitored to check the course of disease. Rotarod test was used to evaluate the coordination of muscle movement. Toluidine blue staining and immunofluorescence were used to check the effect of Rg1 on motor neuron and microglia. The expression of oxidative stress related protein Nrf2 and the miRNA were tested to investigate the mechanism of Rg1. We found that 20 mg·kg^-1·d^-1 Rg1 significantly postponed the disease onset and process, improved the motor syndrome, reduced the loss of motor neuron and inhibited the activation of microglia cells. Rg1 inhibited the aggregation of miR-153 in the spinal cord of ALS mice, which relieved the inhibition of Nrf2 and contributed to its up-regulation in the activation of HO-1 anti-oxidative signal pathway. Our study confirmed that Rg1 could protect ALS mice from oxidative damage through the up-regulation of miR-153/Nrf2/HO-1, which provides a theoretical foundation for Rg1 application to the ALS treatment.

Naozhenning granule, which is composed of 11 herbal drugs, is mainly used in the treatment of concussion, cerebral post-traumatic syndrome. As the chemical composition of Naozhenning was complex, the ultrahigh performance liquid chromatography coupled with hybrid quadrupole-orbitrap mass spectrometry was applied to identify the chemical constituents rapidly in the Naozhenning granule. By analyzing the retention behaviors, accurate molecular weight, the fragmentation pathway, and comparison with the MS data from the standards and references, as well as the automatic identification by the Compound Discover 2.0, a total of 161 compounds were identified or tentatively deduced, and the sources of constituents were also confirmed. The compounds identified in Naozhenning granule included 9 iridoids, 8 butylphthalides, 26 flavonoids and flavonoid glycosides, 8 phenolic acids, 8 monoterpenoid glycosides and 9 alkaloids, as well as the common compounds in the herbal drugs, such as organic acids, amino acids, and sugars. The chemical composition of Naozhenning was studied for the first time, which provides a scientific basis for the quality control and document of effective materials of Naozhenning granule.

The study was designed to establish a 2D UPLC-QTOF method to extrapolate the structure of an unknown substance in carboplatin injection and its relationship with the excipient. By using phenyl-hexyl column (250 mm×4.6 mm, 5 μm) with mobile phase consisting of tetrabutylammonium sulfate buffer (pH 7.5) and acetonitrile in gradient elution mode, an unknown impurity in carboplatin injection was found and quantitatively determined. Then a 2D UPLC-QTOF, HSS T3 column (100 mm×2.1 mm, 1.7 μm) was employed to confirm the molecular weight and the structure of the unknown impurity (electrospray ionization source, positive ion mode, MS^E mode) with mobile phase consisting of 0.1% formic acid and acetonitrile. The relationship among impurities, API and excipient was investigated by accelerated stability test with ICP-MS/MS, ICP-AES. Results showed that disodium edetate in the formulation interacted with carboplatin producing an unknown impurity containing platin, and induced the increase of 1, 1-cyclobutanedicarboxylic acid. The research should be done on the rationality of the addition of disodium edetate in such injections containing heavy metals.

The response surface method was used to evaluate the concentration range, property and degree of Scutellaria (HQ) and Coptis (HL) herb pair on improvement of glucose and lipid metabolism in this paper. Type 2 diabetes mellitus (T2DM) was induced in rats by low a dose of streptozotocin (STZ) in combination with high-fat diet feeding. The rats were administered with HQ-HL extract pairs at different ratio (1:0, 3:1, 2:1, 3:2, 1:1, 2:3, 1:2, 1:3, 0:1). To investigate the influence of herb pair extracts on glucose and lipid metabolism of T2DM rats, the multi index synthetic index method was adopted to integrate the indexes, then the response surface method was applied to analyze the integration results. The ratio of HQ and HL from 3:1 to 1:3 showed a synergistic effect (with the value between -0.2 and -0.8). Especially, when the proportion was between 3:2 and 1:3, herb pair extracts possessed stronger synergistic effects (value:-0.8). The high dose of HQ-HL with the ratio of 1:1 exhibited the strongest synergistic effect.

Flavonoids, especially chalcones such as hydroxysafflor yellow A and carthamin are the main active ingredients of safflower. To study the biosynthesis pathway of safflower flavonoids is of great significance for the quality control of safflower. Chalcone synthase (CHS) is an enzyme that plays an important role in regulation of the synthesis of flavonoids. However, for the time being, the role of CHS is not yet clear in the biosynthesis of safflower flavonoids. As a plant signaling regulator, JA/MeJA can activate CHS gene expression in plants. CtCHS1, one of the CHS genes in safflower, was elucidated in our previous work. In our continuous search for CtCHSs functions from this plant, other CHS genes CtCHS2 and CtCHS4 in safflower were examined. The floret was stimulated with methyl jasmonate (MeJA) and the transcriptome expression of CtCHS2 and CtCHS4 was analyzed by qRT-PCR at different time points of 0, 3, 6, and 12 h after stimulation. Further metabolites under stimulation by MeJA were analyzed by UHPLC/Q-TOF-MS. The results showed that the expression of CtCHS4 in response to MeJA significantly increased at 3 and 6 h, while the expression of CtCHS2 showed a trend of decrease after induction. Meanwhile, the accumulation of rutin, hydroxysafflor yellow A, D-phenylalanine, kaempferol-3-O-β-rutinoside and carthamin increased obviously. Especially, accumulation of hydroxysafflor yellow A was increased significantly at 3, 6 and 12 h after induction (P ≥ 0.05 or 0.01), but the change in kaempferol, kaempferol-3-O-β-D-glucoside, luteolin, quercetin-3-β-D-glucoside was not significant. The accumulation of hydroxysafflor yellow A and carthamin was positively correlated with the expression abundance of CtCHS4 with Pearson correlation analysis method (r ≥ 0.8). The data suggest that CtCHS4 may be a key gene for forming hydroxysafflor yellow A and carthamin and plays an important role in the accumulation of safflower chalcones. The CtCHS4-pMAL-C5X recombinant vector was successfully expressed in BL21 (DE3) Plys to express the product naringenin in vitro under the catalytic substrates p-coumaryol-COA and malonyl-CoA. The results of this study provide a new insight into synthetic genes involved in flavonoids biosynthetic pathway to elucidate the biosynthesis pathway of safflower chalcones.

Histone H3 lysine 79 (H3K79) methyltransferase DOT1L plays an important role in the activation and maintenance of gene transcription; it is also essential for maintenance of embryonic development, as well as the normal function of hematopoietic system, heart and kidney. However, the over expression of DOT1L is associated with the occurring and progress of numerous malignant tumors, so more and more attention has been paid to DOT1L. Therefore, it is of great significance to study and develop inhibitors of DOT1L. The inhibitors could serve as a tool in the investigation of the biological function, and have the potential to be developed into novel anti-cancer agents in the anticancer therapy. This paper mainly describes the structure and function of DOT1L, the relationship between DOT1L and tumors as well as the latest research progress of DOT1L inhibitors; with expect to provide some useful references for the subsequent research.

Sab (SH3 domain-binding protein that preferentially associates with Btk) that is also called SH3BP5 (SH3 domain-binding protein 5), is a scaffold protein on mitochondrial outer membrane in the modulation of mitochondrial function. Sab not only combines with the tyrosine kinase Btk (Bruton's tyrosine kinase), but also binds to the serine threonine kinase JNKs (c-Jun amino-terminal kinases) and p38γ. Thus Sab can regulate B cell antigen receptor, mitochondrial JNK and p38γ signaling pathway, which is associated with the critical physiological function, such as B-cell development and differentiation and regulation of mitochondrial signaling transcription. Inhibition or induction on the expression of Sab can ameliorate the diseases arising from the abnormal level of Btk, JNKs and p38γ, such as nervous system diseases and liver injury. Therefore, Sab could be expected as a new target for drug development. In this article, we provide an overview of the structure and functions of Sab and its relationship to diseases of diffuse large B-cell lymphoma, nervous system diseases and liver injury, aiming to provide new ideas and theoretical basis for the development of new drugs.

A change in vascular smooth muscle cell (VSMC) phenotype, known as converting from a contractile state into a synthetic phenotype, is a crucial event in vascular remodeling, which determines the occurrence, development and prognosis of cardiovascular diseases such as pulmonary hypertension and atherosclerosis. Research shows that the expression level of key signaling molecules, which controls the phenotype change of VSMC, is regulated by microRNA (miRNA), a type of non-encoding RNA. In this article, we provide a review of miRNA in the regulation of VSMC phenotype changes with a focus on the key molecules in MAPK, TGFβ/Smad and PI3K/Akt signaling pathways.