Latest ArticlesOBJECTIVE To study the extraction method, quality, transdermal permeability, and transdermal promoting effects of Chuanxiong Rhizoma Hort. volatile oil (LVO) and Angelicase Sinensis Radix volatile oil (AVO) combined with the characteristic advantages of “unification of drugs and excipients” of traditional Chinese medicine volatile oil. METHODS The orthogonal design was used to screen and optimize extraction process of LVO and AVO. Quality control was carried out by detecting the physical parameters and indicator component content of LVO and AVO. Franz diffusion cells were used to conduct the studies of skin permeation in vitro. The contents of ligustilide and resveratrol(RSV) were determined by HPLC, and the steady-state transdermal rate(Jss) and enhancement factor (EF) compared with blank were used as evaluation indicators. And the transdermal permeability and transdermal promoting effects of different concentrations of LVO, AVO and mixed were investigated respectively. RESULTS The extraction process for LVO and AVO involves 8 times the amount of water, heating and refluxing for 8 h, collecting with ethyl acetate, dehydrating anhydrous sodium sulfate, and then volatilizing under reduced pressure. Perfect quality control methods were established for LVO and AVO, including the properties, relative density, pH, optical rotation, viscosity and ligustilide content. LVO and AVO have good permeability and promote RSV transdermal effect in vitro, and the maximum Jss values within 10 h were (48.23±6.53) and (27.84±3.03), respectively, and the maximum EF values were 4.51 and 19.34, respectively. CONCLUSION LVO and AVO have good transdermal permeability and transdermal promoting effects of RSV when used alone or in combination. The transdermal permeability of LVO was significantly higher than that of AVO, while the transdermal promoting effects of AVO was higher than that of LVO. The combination of LVO and AVO's own pharmacological effects and good transdermal absorption promoting effect plays a role of “unification of drugs and excipients”, which has a good advantage in clinical use, and lays a foundation for their development and application in transdermal drug delivery preparations of traditional Chinese medicine.
Polyporus umbellatus, a traditional medicinal fungus in China, is used medicinally for its sclerotium. It is commonly categorized into two types, Zhushiling and Jishiling, based on the morphology of the sclerotia. Cultivation of Polyporus umbellatus heavily relies on the asexual reproduction of its sclerotia and the absence of clear distinction between Zhushiling and Jishiling often results in the confusion and intermixing of seed sclerotia. This can lead to the instability in quality and yield of Polyporus umbellatus medicinal materials, thereby adversely affecting the robust development of the Polyporus umbellatus industry. This article provides a comparative overview of Zhushiling and Jishiling in 4 aspects: morphology, quality, genetics and spawn cultivation. The results indicate that although the differentiation between Zhushiling and Jishiling based on morphological features such as sclerotium branches and surface characteristics holds certain significance, there remains a necessity to develop more scientific and precise criteria for this classification. The traditional perspective that Zhushiling is of superior quality compared with Jishiling is often based on empirical observations rather than rigorous scientific evidence. It is imperative to conduct comprehensive and systematic studies to objectively evaluate the quality and medicinal properties of both types. The variation in the sclerotial morphology of Polyporus umbellatus may be the result of a complex interplay among genetic, geographic, environmental factors, as well as other factors that have yet to be identified. Key technological breakthroughs in cultivation of the Polyporus umbellatus spawn leading to the formation of the sclerotia have not yet been achieved. However, the strains of Jishiling may possess greater potential for the development of spawn cultivation techniques. Zhushiling and Jishiling exhibit differences across 4 distinct aspects. Conducting the systematic analysis of Polyporus umbellatus from various perspectives is significantly important for the evaluation of its resources and for maximizing its potential value.
OBJECTIVE To establish a method for preparing total saponins from Schizocapsa plantaginea Hance and establish a corresponding quality control method. METHODS The total saponins were extracted from the Schizocapsa plantaginea Hance tubers using a water bath reflux method, followed by purification of the crude extract through solvent extraction and macroporous resin. Subsequently, the purified product of total saponins of Schizocapsa plantaginea Hance(SSPHs) was prepared, and its quality was assessed using thin-layer chromatography, UV-visible spectrophotometry, and ultra-high performance liquid chromatography-mass spectrometry(UHPLC-MS) combined method. RESULTS The developed preparation method resulted in a yield of total saponin products from the Schizocapsa plantaginea Hance tuber ranging from 0.29% to 2.81%, with a purity from 57.30% to 77.02%. After detection, saponin substances such as Schizocapsa Plantaginea Hance Ⅰ(SSPH Ⅰ) and Schizocapsa plantaginea Hance Ⅱ(SSPH Ⅱ) were found in the total saponin products. The content of SSPH Ⅰ was 10.77-85.60 mg·g-1 and the content of SSPH Ⅱ was 0.19-4.75 mg·g-1. CONCLUSION The established preparation method is simple, efficient, and environmentally friendly, with high product quality. The established qualitative and quantitative detection method can effectively reflect the quality of SSPHs and provide method reference for the quality control of SSPHs.
OBJECTIVE To evaluate the testing capability of the vaccine quality control laboratories and vaccine manufacturer laboratories which participated in the proficiency testing of pH, osmotic pressure molar concentration and aluminum content of inactivated COVID-19 vaccine. METHODS Samples of inactivated COVID-19 vaccine were tested for uniformity and stability by F-test and t-test, and then distributed to participating laboratories by cold chain transportation. The abilities of the participating laboratories for determination of pH, osmotic pressure molar concentration, and aluminum content were evaluated by Z ratio. RESULTS A total of 30 laboratories across the country participated in this proficiency testing, and the pH and aluminum content assessment results were all satisfactory, while the osmotic pressure molar concentration results of two laboratories were unsatisfactory. After participating in measurement audits, satisfactory results were obtained. CONCLUSION The provincial vaccine quality control laboratories, and vaccine production enterprises participating in this proficiency testing have good testing capabilities and quality control levels.
Since the end of 2019, the new coronavirus swept the world, causing irreversible harm to social economy and human health, so the search for corresponding antiviral drugs has aroused wide attention. SARS-CoV-2 is mainly transmitted by droplets, and after the process of replication, transcription and translation in the host cell, the mature virus is excreted in the form of endocytosis, forming a closed loop of infection. Notably, the papain like protease (PLpro) encoded by non-structural protein 3 (nsp3) plays an important role in this process. At the same time, PLpro also helps the virus evade the corresponding immune response in inflammatory reactions such as deubiquitination. Therefore, targeted inhibition of PLpro can not only block the overall replication process of the virus, but also restore the host's own immune function, so as to achieve a better anti-SARS-CoV-2 effect. In summary, based on the different structures of the compounds, this paper intends to conduct an exploratory summary of the recent studies on inhibitor targeting SARS-CoV-2 PLpro, in order to provide theoretical reference for the discovery of anti-SARS-CoV-2 drugs.
OBJECTIVE To investigate the chemical constituents from Ferula bungeana Kitagawa. METHODS The chemical constituents from Ferula bungeana Kitagawa were investigated by silica gel chromatography, TLC, preparative HPLC, NMR, and HR-MS. RESULTS Thirty-three compounds were isolated from Ferula bungeana Kitagawa and identified, namely palmitic acid(1), oleic acid(2), linoleic acid(3), linolenic acid(4), dehydrofalcarinol(5), falcarinol(6), β-itosterol(7), 2, 6, 11, 15-tetramethyl-2, 6, 10, 14-hexadecanetetraene(8), arteordoyn A(9), falcarindiol(10), dehydrofalcarindiol(11), umbelliprenin(12), conferone(13), farnesiferone A(14), ferukrinone(15), polyanthinin(16), assafoetidnol B(17), actylfekrynol(18), fekrynol(19), kellerin(20), mogoltacin(21), gummosin(22), farnesiferol A(23), ferukrin(24), deacetylkellerin(25), assafoetidnol A(26), karatavicinol (27), 14'-hydroxy-karatavicinol (28), galbanic acid(29), 6, 7-dimethoxycoumarin(30), vanillin(31), 7-hydroxycoumarin(32) and 6, 7-dihydroxycoumarin(33). CONCLUSION Compounds 5-6, 9-11 are isolated in this genus for the first time, and others are isolated from this plant for the time.
OBJECTIVE To design, synthesize and evaluate a series of 3', 4'-ethylendioxy chalcone derivatives as monoamine oxidase B (MAO-B) inhibitors, and summarize the structure-activity relationship (SAR). METHODS The targeted compounds were synthesized via Claisen-Schmidt condensation reaction starting from 6-acetyl-1, 4-benzodioxan and corresponding benzaldehydes. The inhibition of these compounds on human MAO-B (hMAO-B) was determined, and the inhibiting selectivity, dynamics and reversibility were investigated as well. The binding mode between active compounds and hMAO-B was revealed by molecular docking study. Additionally, the inhibitory effect of active compounds on the proliferation of BV2 cell line was determined by MTT assay. RESULTS Sixteen targeted compounds were successfully prepared. Most compounds showed good inhibitory effects on hMAO-B. Representative compounds 9 and 13 exhibited IC50 values of 0.021 and 0.042 μmol·L-1, respectively, which showed high inhibiting selectivity towards hMAO-B. Both compounds acted as competitive and reversible hMAO-B inhibitors. The main interactions between active compounds and hMAO-B were hydrophobic interaction and hydrogen bond. The most active compound 9 exhibited low cytotoxicity in BV2 cells. CONCLUSION This class of 3', 4'-ethylendioxy chalcone derivatives represent potential novel inhibitors of hMAO-B, and compound 9 could be further investigated as a potent lead for future studies.
OBJECTIVE To predict the potential quality marker (Q-Marker) components of Suanzaoren Decoction based on the prototype chemical composition of in vivo by using network pharmacology. METHODS Firstly, the plasma samples and urine samples of rats were collected within 4 h and 24 h after intragastric administration of Suanzaoren Decoction, respectively. Then, based on the chemical components found in vivo, the key action targets and key pathway were obtained by network pharmacology, and the network map of "component-target-pathway" was carried out to predict the quality markers of Suanzaoren Decoction against insomnia, anxiety and depression. RESULTS A total of 20 prototype compounds were detected in rats. The 23 core targets were predicted and 14 prototype components associated with pharmacodynamic efficacy were screened through network pharmacology, the 14 components including jujuboside A, enoxolone, ferulic acid, magnoflorine, liquiritigenin, isoliquiritigenin, poricoic acid A, spinosin, coclaurine, timosaponin BII, glycyrrhizic acid, jujuboside B, liquiritin and senkyunolide A played multiple targets and multiple pathways to regulate insomnia, anxiety, depression. CONCLUSION It is predicted that the 14 chemical components are considered as potential quality markers of Suanzaoren Decoction by analyzing prototype chemical composition in vivo combined with network pharmacology. The results can provide reference for the quality control of Suanzaoren Decoction, and lay a foundation for elucidating the mechanism of its pharmacodynamic substances.
Pain management remains as a global public health issue, with 20% of the adult population worldwide impacted and many patients still suffer from unrelieved or undertreated pain. Classic opioids exert antinociceptive effects by activating μ opioid receptor (MOR), but they are associated with many side effects (including respiratory depression, addiction, and constipation) which have aggravated the ongoing and escalating opioid crisis in worldwide. Therefore, there is an urgent need for the development of novel analgesics free of MOR-mediated unwanted adverse effects. Multi-target therapeutics target two or more related targets in a disease network system simultaneously, which can potentially provide greater efficacy and improve treatment outcomes compared with single-target therapies. Due to the key role of MOR in regulating pain signal transmission, MOR-based multi-target ligands have been accepted as one of the mainstream strategies for designing new potent analgesics without side effects. In this review, recent advances in multitarget-directed drugs toward MOR are summarized, which may provide references for the development of potent and safer analgesics.
The discovery of drug targets is crucial for understanding the mechanism of drug action and facilitating the development of novel drug therapeutics. Microscale thermophoresis (MST), renowned for its minimal sample consumption, rapid detection speed, high sensitivity, and the absence of the need for protein immobilization, has emerged as a pivotal tool in drug target research. This article outlines the strategies for identifying drug targets, with a focus on elucidating the principles of MST and its application in drug target discovery. Furthermore, it summarizes the promising prospects of MST in this field. The applications of MST are found in both forward and reverse strategies for target discovery, enabling the identification of target proteins for compounds, single herbal ingredients, and compound prescriptions, as well as facilitating drug screening. Additionally, the integration of MST with other molecular interaction techniques, such as surface plasmon resonance (SPR), provides a potent arsenal for studying the interactions between drugs and their targets. Despite certain limitations, MST holds immense potential for application in the realms of novel drug development and drug mechanism research.