Network pharmacology identifies the inhibitory effect of Yiqiyangyinquyu prescription on salivary gland inflammation in Sjögren's syndrome.

This study aimed to explore the mode of action of Yiqiyangyinquyu prescription (YP) against Sjögren's syndrome (SS) by combining network pharmacology with molecular docking techniques. YP's active components and target proteins were identified using the BATMAN-traditional Chinese medicine database. Concurrently, targets associated with SS were extracted from databases, including Genecards, Online Mendelian Inheritance in Man, and Therapeutic Target Database. The standard targets were then imported into the STRING database to construct a protein-protein interaction network. We then conducted gene ontology and Kyoto encyclopedia of genes and genomes enrichment analyses, which were succeeded by molecular docking studies to validate core active components and key targets. Finally, in vitro experiments and molecular dynamics simulation were conducted to substantiate the therapeutic efficacy of YP in treating SS. A total of 206 intersection targets and 46 active compounds were identified. Gene ontology analysis unveiled that YP targets were primarily enriched in cellular responses to chemical stress, inflammation, and cell proliferation. Key enriched signaling pathways encompassed the interleukin 17, hypoxia-inducible factor-1, tumor necrosis factor (TNF-α), and advanced glycation end products-receptor for AGEs (AGE-RAGE) signaling pathways. Molecular docking results demonstrated high-affinity between neotanshinone C, tanshiquinone B, miltionone I, TNF-α, interleukin 1 beta (IL-1ß), and interleukin 6 (IL-6). Noteworthy, TNF-α, considered the most important gene in YP against SS, binds to YP most stably, which was further validated by molecular dynamics simulation. In vitro experiments confirmed YP's capacity to reduce TNF-α, IL-1ß, and IL-6 expression, effectively alleviating SS-related inflammation. YP demonstrated a significant anti-inflammatory effect by suppressing inflammatory cytokines (TNF-α, IL-6, and IL-1ß), providing experimental evidence for its clinical application in treating SS.

[Dead heart of pith-decayed Scutellariae Radix: a study based on multi-omics].

Dead heart is an important trait of pith-decayed Scutellariae Radix. The purpose of this study was to clarify the scientific connotation of the dead heart using multi-omics. Metabolomics and transcriptomics combined with multivariate statistical analysis such as principal component analysis(PCA) and partial least squares discriminant analysis(PLS-DA) were used to systematically compare the differences in chemical composition and gene expression among phloem, outer xylem and near-dead xylem of pith-decayed Scutella-riae Radix. The results revealed significant differences in the contents of flavonoid glycosides and aglycones among the three parts. Compared with phloem and outer xylem, near-dead xylem had markedly lowered content of flavonoid glycosides(including baicalin, norwogonin-7-O-ß-D-glucuronide, oroxylin A-7-O-ß-D-glucuronide, and wogonoside) while markedly increased content of aglycones(including 3,5,7,2',6'-pentahydroxy dihydroflavone, baicalin, wogonin, and oroxylin A). The differentially expressed genes were mainly concentrated in KEGG pathways such as phenylpropanoid metabolism, flavonoid biosynthesis, ABC transporter, and plant MAPK signal transduction pathway. This study systematically elucidated the material basis of the dead heart of pith-decayed Scutellariae Radix with multiple growing years. Specifically, the content of flavonoid aglycones was significantly increased in the near-dead xylem, and the gene expression of metabolic pathways such as flavonoid glycoside hydrolysis, interxylary cork development and programmed apoptosis was significantly up-regulated. This study provided a theoretical basis for guiding the high-quality production of pith-decayed Scutellariae Radix.

[Nature-effect transformation mechanism of mulberry leaves and silkworm droppings based on chemical composition analysis].

Starting with the relationship between mulberry leaves and silkworm droppings as food and metabolites, this study systematically compared the chemical components, screened out differential components, and quantitatively analyzed the main differential components based on ultra-high performance liquid chromatography with quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS) and UPLC-Q-TRAP-MS combined with principal component analysis(PCA) and orthogonal partial least squares-discriminant analysis(OPLS-DA). Moreover, the in vitro enzymatic transformation of the representative differential components was studied. The results showed that(1) 95 components were identified from mulberry leaves and silkworm droppings, among which 27 components only exist in mulberry leaves and 8 components in silkworm droppings. The main differential components were flavonoid glycosides and chlorogenic acids.(2) Nineteen components with significant difference were quantitatively analyzed, and the components with significant differences and high content were neochlorogenic acid, chlorogenic acid, and rutin.(3) The crude protease in the mid-gut of silkworm significantly metabolized neochlorogenic acid and chlorogenic acid, which may be an important reason for the efficacy change in mulberry leaves and silkworm droppings. This study lays a scientific foundation for the development, utilization, and quality control of mulberry leaves and silkworm droppings. It provides references for clarifying the possible material basis and mechanism of the pungent-cool and dispersing nature of mulberry leaves transforming into the pungent-warm and dampness-resolving nature of silkworm droppings, and offers a new idea for the study of nature-effect transformation mechanism of traditional Chinese medicine.

[Research advances in chemical constituents and pharmacological activities of Dendrobium plants].

Dendrobii Caulis are commonly used tonic Chinese medicinal materials with a long history of application. As demonstrated by pharmacological results, the chemical constituents and the extracts of Dendrobii Caulis have anti-inflammatory, antibacte-rial, antioxidant, and anti-tumor effects, and can also regulate immunity, lower blood pressure, and regulate blood sugar. The active ingredients contained are widely concerned by scholars. This paper comprehensively summarized the chemical constituents and pharmacological activities of Dendrobium plants reported so far. The chemical constituents isolated from Dendrobium plants are mainly alkaloids, sesquiterpenoids, flavonoids, fluorenones, coumarins, bibenzyls, phenanthrenes, lignans, steroids, phenols, and polysaccharides. This paper is expected to provide a reference for further research, development, and utilization of Dendrobium plants.

[Textual research on "Gui" in Chinese classical prescriptions].

Through consulting the ancient herbs and medical books, combining with modern literature, this paper makes textual research on herbal medicine, and textual research on the name, origin, position and harvest and processing changes of the medicinal herbs in ancient classical prescriptions. According to research, Cinnamon medicinal materials were first listed in the Shennong's Herbal Classic, as the name of "Jungui" and "Mugui". Among them, Jungui has undergone the evolution of "Qungui-Jungui-Tonggui-Jungui". After the Northern and Southern Dynasties, a half-volume fatty "Gui" was added, but the usage of the three was no different. The names of Cinnamomi Ramulus and Cinnamomi Cortex did not appear until the Tang Dynasty, and they were preferably thick-skinned and with no cork cambium, and they were mostly used in the name of "Guixin"; Since the Song and Yuan Dynasties, the medicinal parts of cassia have gradually separated. Cinnamomi Cortex is the trunk bark of sapling or branch bark, the twig is Cinnamomi Ramulus, and the tenderest twig is Liugui, Song Dynasty unified the name as "Guizhi"; After the Ming and Qing Dynasties, Cinnamomi Cortex was used as the trunk bark, and Cinnamomi Ramulus was used as the tender twig; In modern times, the Chinese Pharmacopoeia stipulates that the Cinnamomi Ramulus is the young branch of C. cassia, which is Cinnamomum, and Cinnamomi Cortex was the dried trunk bark. From the plant morphology recorded in the previous herbals and the drawings, combined with the distribution of the origins described in the previous herbals, the mainstream plant used as a medicine in the past generations should be C. cassia, but there are other sect. Cinnamomum plants that are also used in medicine everywhere, such as C. chekiangensis, C. bejolghota, C. wilsonii, etc. Throughout the ages, different plant morphologies and medicinal traits have been used to distinguish different categories. The origins of the past dynasties are mostly present in Guangdong, Guangxi province and Vietnam, and are regarded as authentic. The methods for the harvest and processing of cinnamon medicinal materials are basically the same from ancient to modern times.

[Textual research on medicinal blue herbs].

In this paper, through the collection and collation of ancient herbs, medical books and prescriptions, combined with modern literature, the historical changes of the name, origin, position, medicinal parts, collection, processing and processing of bluegrass were systematically combed and verified.It can be seen from the research that bluegrass was first used as medicine by the fruit, namely blueberry, which was originally Polygonum tinctorium. Since the Ming and Qing Dynasties, blueberry was rarely used, and it has been no longer used medicinally. In the Wei and Jin Dynasties, the medicinal parts extended to the stems and leaves, and most of them used juice as medicine.Since the Tang Dynasty, origin has been extended to Isatis indigotica, Baphicacanthus cusia, Indigofera tinctoria, Compositae plant Wulan, etc. In the Song Dynasty, the medicinal parts extended to the roots, and the "Banlangen" began to appear, and gradually became the main medicinal parts of blue medicinal materials, the main base of which was B. cusia. Since the Qing Dynasty, I. indigotica, a Cruciferae, has gradually become a genuine indigo root, while B. cusia has become a southern indigo root. It was the first mineral dye imported from abroad for thrush, and then used as medicine, also known as clam powder. Because it was found that it had the same effect with the extract of bluegrass, it was also named indigo naturalis in China, which has lasted till now. The main stream of Isatidis Folium in the past dynasties is the dry stem and leaf of Clerodendrum cyrtophylum. Since the Qing Dynasty, the stem and leaf of Isatis indigotica, P. tinctorium and other blue grasses have been gradually mixed as substitutes and gradually become the mainstream.

Electrochemical biosensor based on Se-doped MWCNTs-graphene and Y-shaped DNA-aided target-triggered amplification strategy.

A highly sensitive electrochemical biosensor for detection of platelet-derived growth factor-BB (PDGF-BB) is developed by using Se-doped multi-walled carbon nanotubes (MWCNTs)-graphene hybrids as electrode supporting substrate, hemin/G-quadruplex as trace labels and Y-shaped DNA-aided target recycling as signal magnifier. The aptamer-containing hairpin probes were first immobilized on the electrode. When target PDGF-BB was added, the aptamer binded PDGF-BB to trigger catalytic assembly of two other hairpins to form many G-quadruplex Y-junction DNA structures, which released PDGF-BB to again bind the intact aptamer to initiate another assembly cycle. G-quadruplex/hemin complexes were produced when hemin was added to generate substantially amplified current output. The developed assay showed a linear range toward PDGF-BB from 0.1 pM to 10 nM with a detection limit of 27 fM (S/N = 3). The method showed excellent specificity and repeatability, and could be expediently applied for sensitive detection of other molecules by simply changing the aptamers.

Comparative pharmacokinetics of senkyunolide I in a rat model of migraine versus normal controls.

Senkyunolide I is an active ingredient of Rhizoma Chuanxiong, a Chinese medicinal herb commonly used for the treatment of cardiovascular ailments. In the present paper, we describe the isolation and elucidation of senkyunolide I from the ethanol extract of Rhizoma Chuanxiong and its pharmacokinetic behavior after intravenous and oral administration to normal and migrainous rats. After intravenous administration, senkyunolide I was rapidly distributed (V ( z )/F 2.07 ± 0.43 L/kg) and eliminated from the plasma (CL( z ) 2.56 ± 0.29 L/h/kg and t (1/2z ) 0.56 ± 0.13 h). After administration orally to normal rats at two dosages (20 and 72 mg/kg), the pharmacokinetic parameters of senkyunolide I were as follows: T (max) 0.25 ± 0.06 and 0.38 ± 0.11 h, C (max) 5,236.3 ± 802.8 and 22,071.9 ± 3,456.1 mg/L, Area under the curve(AUC)((0-t)) 5,217.5 ± 1,029.5 and 21,480.2 ± 3,003.1 µg h/L, respectively. Its oral absolute bioavailability at the two dosages was 67.2 and 76.9%, respectively. Intriguingly, migraine caused some significant changes in its pharmacokinetic parameter. For example, when compared with its pharmacokinetic behavior in normal rats at the two dosages, on average, its clearance decreased by 68% and volume of distribution increased by 342% in migrainous rats, both of which contributed to its several-fold increase in t (1/2z) and AUC. C (max) and AUC of senkyunolide I increased almost proportionally with dose between 20 and 72 mg/kg and the pharmacokinetics fit linear kinetic feature. The pharmacokinetic parameters of senkyunolide I were significantly different in normal and migrainous rats, which should be taken into account during the design of a clinical dosage regimen for senkyunolide I.

Effect and mechanism of senkyunolide I as an anti-migraine compound from Ligusticum chuanxiong.

OBJECTIVE: To evaluate the analgesic and anti-migraine activities of senkyunolide I from Ligusticum chuanxiong. METHODS: Mice were orally administered various doses of senkyunolide I, and their pain levels were assessed in a hot-plate test and by application of acetic acid. The levels of 5-hydroxytryptamine (5-HT), 5-hydroxytryptophan (5-HTP), 5-hydroxyindoleacetic acid (5-HIAA), norepinephrine (NE) and dopamine (DA) in plasma and brain were assessed, and the monoamine turnover rates (5-HT/5-HTP, 5-HIAA/5-HT and NE/DA) were also calculated. RESULTS: Mice given senkyunolide I at 16 and 32 mg/kg had significantly elevated pain thresholds in the hot-plate test, and a dose of 32 mg/kg also reduced the number of abdominal writhing responses caused by acetic acid. Significant improvements were observed in the neurotransmitter levels of the drug-treated rats compared with the saline-administered controls. Compared to the rats with nitroglycerin-induced migraines, the levels of nitric oxide in the plasma and whole brain of rats given senkyunolide I were lower. CONCLUSIONS: The present study suggests that senkyunolide I may be an active component of L. chuanxiong, traditionally used to treat migraine. The mechanism of pain relief in migraine model rats may be through adjusting the levels of monoamine neurotransmitters and their turnover rates, as well as decreasing nitric oxide levels in the blood and brain. Therefore, senkyunolide I may be developed as a potential treatment for migraine pain.

[Study on preparation of glycyrrhiza total flavones effective components sustained-release pellets and its properties].

OBJECTIVE: To prepare the glycyrrhiza total flavones effective components pellets by extrusion-spheronization, and to optimize the formulation of glycyrrhiza total flavones effective components sustained release pellets coated with mixed Eudragit RS 100. METHODS: The sustained-release pellets of glycyrrhiza total flavones were prepared by Glatt fluid bed technique. The factors influencing the drug release behaviors and their properties were evaluated. RESULTS: The optimal drug sustained-release was shown at the loading weight of copolymers of 6% and the plasticizer concentration of 10%. And the curves of cumulative drug release were fit for Peppas and Higuchi equation. CONCLUSION: The pellets show obviously sustained-release effect.

[Preparation and properties of sustained-release pellets of glycyrrhizin effective components].

OBJECTIVE: To prepare the glycyrrhizin pellets by extrusion-spheronization, and optimize the formulation of sustained release pellets of glycyrrhizin effective components coated with mixed Eudragit RS 100 and Eudragit RL 100. METHOD: The sustained-release pellets of glycyrrhizin were prepared by Glatt fluid bed technique. The ratio of Eudragit RS 100 to Eudragit RL 100 in the formulation was optimized. The factors that influence the drug release behaviors and their properties were evaluated. RESULT: The optimal coat for drug sustained-release was shown at the ratio of Eudragit RS 100 to Eudragit RL 100 of 4:1, the loading weight of copolymers of 5% and the plasticizer concentration of 15%. The curves of cumulative drug release were fit for Peppas and Higuchi equation. CONCLUSION: The optimal sustained release of the glycyrrhizin effective component pellets is featured by adjusting the ratio of Eudragit RS 100 to Eudragit RL 100 and the loading weight of copolymers.