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Fairmaire is a medicinal insect that has been used for a long time by minority ethnic groups in Yunnan, China, due to its immunomodulatory function. However, its potential applications in cosmetics have not been reported. experiments were used to verify whether the extracts of Fairmaire (EBR) have the effect of inhibiting TYR activity and eliminating melanin deposition. Subsequently, experiments were conducted to verify further the potential application of the EBR in whitening. To explore the whitening components of the EBR, we employed UHPLC-Q-TOF MS to identify the compounds present in the EBR and utilized network pharmacology to compare them with the genes involved in whitening in the database, thereby obtaining the intersection of compound targets and whitening targets. Then, protein-protein interaction network analysis, gene ontology enrichment and Kyoto Encyclopedia of Genes and Genomes pathway enrichment analysis were carried out to explore the main components of the whitening effect of the EBR. Further, molecular docking and molecular dynamics simulation were used to verify the correlation between the main components of the EBR and the essential target molecules. and studies have found that the EBR exhibits anti-oxidation, TYR-inhibiting activity, and the elimination of melanin deposition. Subsequently, 1538 metabolites were identified by UHPLC-Q-TOF MS analysis, indicating that EBR is a rich source of bioactive compounds. Among them, 82 kinds of phenols and flavonoids may be derived from external enrichment or self-synthesis. Network pharmacology revealed 41 genes related to pigmentation and TYR inhibition. Molecular docking and molecular dynamics simulation confirmed that myricetin, luteolin, apigenin and quercetin have a high binding affinity with TYR, which may regulate melanin production by inhibiting TYR activity. In this study, we identified the primary whitening active ingredients of and utilized network pharmacology and molecular dynamics simulation to investigate the mechanism underlying the whitening effect of EBR. This work reveals that insect extraction may have broad application prospects in the preparation of cosmetics. To our knowledge, this is the first report identifying the flavonoids quercetin, luteolin, myricetin, and apigenin as whitening-active components in insects.

Introduction: Antibiotic resistance is a global threat that has been increasing recently, especially with antibiotic overuse and misuse. The search for new antibiotics is becoming more and more indispensable. Methods: Design and synthesis of isatin derivatives as surrogates of SB-239629, a bacterial tyrosine-tRNA synthetases (TyrRS) inhibitor. The newly synthesized compounds were screened for their antimicrobial and antibiofilm activities. Docking studies were used to investigate potential binding modes of these compounds with TyrRS. Results and Discussion: Newly synthesized isatin-decorated thiazole derivatives (7b, 7d, and 14b) have shown potent antimicrobial activities against E. coli, a representative of gram-negative bacteria. Also, 7f showed the best activity against Methicillin Resistant Staphylococcus aureus (MRSA). In addition, 7h and 11f were found to have antifungal activities against Candida albicans equivalent to that of the reference Nystatin. All the new isatin derivatives with antimicrobial activities were found to exhibit strong biofilm distortion effects at half their minimum inhibitory concentrations (MIC). Moreover, thiazole derivatives 11a-f showed promising biofilm formation inhibition. Finally, molecular docking studies were used to investigate possible binding modes of target compounds with S. aureus and E. coli TyrRS. Conclusion: The novel isatin-decorated thiazole derivatives show strong antimicrobial and antifungal activities with potential action on TyrRS. Keywords: 5-bromoisatin, thiosemicarbazone, hydrazonoyl chlorides, thiazoles, Tyrosyl-tRNA synthetases (TyrRS) inhibitors, antimicrobial, molecular docking, MRSA, antibiofilm

Astragalus membranaceus Fisch. ex Bunge (syn. Astragalus mongholicus Bunge) is one of the notable medicinal and food plants. Therefore, the aim of this study was to calculate the phenolic composition and antioxidant, antimicrobial, as well as enzyme inhibitory [acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase (TYR)] activities with chemometric approaches of the hydromethanolic and water extracts of commercial A. membranaceus samples. Ten individual phenolic compounds were determined using high-performance liquid chromatography (HPLC), and only quercetin was found at a level of above 80 µg/g DW in both extracts. Moreover, the highest antioxidant activity in DPPH, FRAP, ABTS, and CUPRAC assays was found in the sample containing the roots in loose form from USA. A. membranaceus extracts displayed the inhibition zone diameters within the range from 10 to 22 mm antimicrobial activity against S. aureus, while there were no inhibition zones in any extracts in case of E. coli. The extracts of A. membranaceous showed an inhibition rate below 40% against TYR, and among tested extracts, only two samples were able to inhibit BChE with IC50 values of above 30 µg/mL. Correlation analysis showed a highly positive relationship between their phenolic composition and antioxidant activity. Concluding, the obtained results confirmed that A. membranaceus commercial samples could be an important dietary source of natural antioxidants.

In this research, the inhibition mechanism of a pairs of homoisoflavonoid analogues (6-aldehydo-isoophiopogonanone A (AIO-A) and 6-aldehydo-isoophiopogonanone B (AIO-B)) on tyrosinase (Tyr) was investigated by multi-spectroscopic techniques combined with molecular docking. The results demonstrated that AIO-A suppressed the activity of Tyr in a reversible competitive-inhibition with a half inhibitory concentration (IC50) of (12.67 ± 2.52) × 10–5 molˑL−1, while AIO-B was a reversible mixed-inhibition with IC50 of (4.81 ± 0.74) × 10–5 molˑL−1. AIO-A/AIO-B bound to Tyr driven by the intermolecular interactions, including van der Waals interaction, hydrogen bonding and hydrophobic interaction, thereby resulted in a secondary structure change of Tyr and its intrinsic fluorescence quenching. The molecular docking revealed that an aldehyde oxygen atom in AIO-A and methoxyphenyl in AIO-B formed coordination with two Cu ions in the active center of Tyr protein. It can be deduced that the coordination with two Cu ions may prevent the entrance of substrate and then inhibit the catalytic activity of Tyr. The research might provide new perspectives on the inhibition mechanism of AIO-A and AIO-B on Tyr and functional research for the prevention and treatment of pigmented skin diseases and anti-browning of homoisoflavonoids as a food supplement.

Tongue squamous cell carcinoma (TSCC) is one of the most common head and neck cancers. Cisplatin is effective as a single agent or in combination with other drugs for the treatment of TSCC. Treatment with cisplatin-based chemotherapy has been found to improve the prognosis of patients with TSCC. However, one of the most important clinical issues of cisplatin-based TSCC chemotherapy is the intrinsic/acquired chemoresistance to cisplatin. Increased expression of miR-23a reportedly promotes cisplatin chemoresistance in TSCC cells. High expression of Twist is also associated with cancer chemoresistance and poor prognosis of TSCC patients. In the present study, we explored the interaction between miR-23a and Twist in TSCC cells, and assessed its impact on TSCC chemoresistance to cisplatin. miR-23a and/or Twist were overexpressed or knocked down in SCC-4 and Tca8113 human TSCC cells. The expression levels of miR-23a and Twist were determined. The half maximal inhibitory concentration (IC50) of cisplatin and cell apoptosis rate under cisplatin treatment were used as measures of cisplatin chemoresistance. Overexpression of miR-23a in both SCC-4 and Tca8113 cells markedly increased Twist expression, c-Jun N-terminal kinase (JNK) activity and the half maximal inhibitory concentration (IC50) of cisplain, and decreased cisplatin-induced apoptosis, all of which was abolished by knockdown of Twist or selective JNK inhibitor SP600125. On the other hand, knockdown of miR-23a significantly decreased Twist expression, JNK activity and IC50 of cisplain, and increased cisplatin-induced apoptosis, all of which was completely reversed by overexpression of Twist. In conclusion, the present study for the first time demonstrates that miR-23a promotes cisplatin chemoresistance and protects cisplatin-induced apoptosis in TSCC cells through inducing Twist expression by a JNK-dependent mechanism. It adds new insights into the molecular mechanisms underlying TSCC chemoresistance.

From a clinical point of view, easily obtainable and useful markers of a particular pathological status are required for appropriate diagnosis and treatment. Analysis of the proteomic profile of saliva may allow for the selection of potential marker of preterm delivery in humans. Saliva samples were collected from 12 patients diagnosed with threatened preterm delivery and 10 controls with uncomplicated pregnancies at the same gestational age. Samples were analysed using 2D electrophoresis. Based on statistical analysis, spots of interest were selected and collected from gels. Subsequently, spots were decoloured and proteins were identified by mass spectrometry using the matrix assisted laser desorption ionization-time of flight technique. The results of identification were compared with the Swiss-Prot database. A total of 1,393 spots were detected in the present study with 59 significantly different between control and preterm samples. Increased intensity of staining of 32 spots was observed in the premature delivery group compared with control patients and 27 spots were stained more intensely in the control group compared with the premature delivery group. A total of nine spots, which were significantly different between examined samples were identified and three of them exhibited increased intensity of staining in premature delivery group compared with controls, including dedicator of cytokinesis protein 1, metallothionein-2, guanylyl cyclase-activating protein 1. The six remaining spots included, epithelial-stromal interaction protein 1, serum albumin, tyrosine-tRNA ligase, cytoplasmic, protein chibby homolog 3, leukemia inhibitory factor receptor and adenosylhomocysteinase 3, and exhibited increased intensity of staining in healthy controls compared with premature delivery group. Further studies with an increased number of patients and identification of the complete protein profile are required to confirm the results of the present study and applicability of saliva as a source of disease biomarkers.

The acidic-subunit of amarantin, main seed storage protein of Amaranthus hypochondriacus, carrying four antihypertensive biopeptides Val-Tyr was expressed in the fruit of transgenic tomato plants. Immunoblot analyses indicate that the expressed recombinant protein was stably accumulated at levels up to 12.71 % with respect to total protein content of transgenic fruits. There was a remarkable change in total protein content (5–22 % increase) of transgenic tomato fruits compared to non-transformed samples. Specific increases of the essential amino acids valine (31–40 %), tyrosine (29–34 %), isoleucine (21–31 %), leucine (28–31 %) and phenylalanine (28–29 %) were also detected in some transgenic lines versus wild type lines. Protein hydrolysates from transgenic tomato fruits showed in vitro inhibition of the angiotensin converting enzyme, with IC50 values that ranged from 0.376 to 3.241 μg ml−1; this represents an increase of up to 13-fold in the inhibitory activity compared with the protein hydrolysates of non-transformed fruits. These results suggest the possible application of transgenic tomato fruit for massive production of this engineered version of amarantin, which could be especially useful in the prevention and control of hypertension.