An improved deep learning network for image detection and its application in Dendrobii caulis decoction piece.

In recent years, with the increasing demand for high-quality Dendrobii caulis decoction piece, the identification of D. caulis decoction piece species has become an urgent issue. However, the current methods are primarily designed for professional quality control and supervision. Therefore, ordinary consumers should not rely on these methods to assess the quality of products when making purchases. This research proposes a deep learning network called improved YOLOv5 for detecting different types of D. caulis decoction piece from images. In the main architecture of improved YOLOv5, we have designed the C2S module to replace the C3 module in YOLOv5, thereby enhancing the network's feature extraction capability for dense and small targets. Additionally, we have introduced the Reparameterized Generalized Feature Pyramid Network (RepGFPN) module and Optimal Transport Assignment (OTA) operator to more effectively integrate the high-dimensional and low-dimensional features of the network. Furthermore, a new large-scale dataset of Dendrobium images has been established. Compared to other models with similar computational complexity, improved YOLOv5 achieves the highest detection accuracy, with an average mAP@.05 of 96.5%. It is computationally equivalent to YOLOv5 but surpasses YOLOv5 by 2 percentage points in terms of accuracy.

Absorption, tissue distribution, and excretion of glycycoumarin, a major bioactive coumarin from Chinese licorice (Glycyrrhiza uralensis Fisch).

Licorice (Glycyrrhiza uralensis Fisch) is a natural plant resource widely used as a food and herbal medication in China. Glycycoumarin (GCM) is a major coumarin in licorice that possesses several biological activities. However, little is known about its pharmacokinetic profile. The present study aimed to describe the oral absorption, tissue distribution, and excretion of GCM in rats. Free (parent drug) and/or total (parent drug plus the glucuronidated metabolite) GCM in biological samples was quantified before and after the hydrolysis reaction with ß-glucuronidase using a reliable LC-MS/MS method. The results indicated that GCM was rapidly absorbed and transformed into its conjugated metabolites after administration. Free GCM plasma concentrations after i. v. (10 mg/kg) administration quickly decreased with an average t1/2,λz of 0.71 h, whereas the total GCM concentration reduced slowly with a t1/2, λz of 2.46 h. The area under the curve of glucuronidated metabolites was approximately four-times higher than that of free GCM. Presumably, because of hepatic and/or intestinal tract first-pass metabolism, GCM exhibited a poor bioavailability of 9.22%, as estimated from its total plasma concentration. Additionally, GCM was distributed rapidly and widely in various tissues except the brain. The liver had the highest concentration; further, GCM was promptly eliminated from test tissues after intraperitoneal (20 mg/kg) administration, but only a small amount of GCM was excreted via bile and urine. Overall, GCM is absorbed and rapidly transformed into its conjugated metabolites with low bioavailability; further, it is distributed in various tissues, except the brain. These pharmacokinetic results are helpful for better understanding the characteristics and pharmacological effects of GCM.

Pharmacological Activities and Pharmacokinetics of Glycycoumarin.

Glycycoumarin is a representative coumarin compound with significant pharmacological activities isolated from Glycyrrhiza uralensis Fisch., Fabaceae. Studies have shown that glycycoumarin has many biological activities, such as anti-tumor, liver protection, antispasmodic, antibacterial, and antivirus. However, the poor solubility of glycycoumarin in water and the accompanying reactions of the phase I (hydroxylation) and II (glucuronidation) metabolism limit its druggability, which manifests as low absorption in the body after oral administration and low free drug concentration, ultimately leading to low bioavailability. Therefore, a comprehensive review of the pharmacological effects and pharmacokinetics of glycycoumarin is presented to provide a reference for further research and application as a therapeutic agent. Supplementary Information: The online version contains supplementary material available at 10.1007/s43450-022-00342-x.

Predicting and Validating the Mechanism of Qingyi II Granules in the Treatment of Acute Pancreatitis by Network Pharmacology.

Network pharmacology, reverse molecular docking, and rat acute pancreatitis (AP) models were used to analyze the mechanism of protection by Qingyi II granules. The chemical components of 7 Chinese herbal medicines in Qingyi II granules were searched through the TCMSP (traditional Chinese medicine systems pharmacology database and analysis platform) database. The active ingredients were screened out in the OB (oral bioavailability) and DL (drug likeness) filters as a condition for inclusion. Then, the prediction analysis of potential targets was performed through databases. A GO (gene ontology) enrichment analysis of target proteins related to AP and KEGG (Kyoto Encyclopedia of Genes and Genomes) pathway annotation was performed using the DAVID (The Database for Annotation, Visualization, and Integrated Discovery) database. Finally, the "Herbal-Compound-Target" network was constructed using Cytoscape software. The active component structure and target name were uploaded to the Systems Dock database for reverse molecular docking. With octreotide as a positive control, Qingyi II decoction and Qingyi II granules were administered to AP rats at low, medium, and high doses. The pathological changes in the pancreas were observed using HE staining. The levels of Bcl-2, AMS, BAX, IL-2, and CASP3 in plasma were determined by an ELISA kit. Real-time PCR detected the expression of AKT1 and PIK3CA mRNA in the pancreas. The database predicted 94 active components of Qingyi II granules, 76 potential targets, and 64 signaling pathways. Twenty pathways were directly or indirectly associated with acute pancreatitis, including the TNF signaling pathway and the PI3K-AKT signaling pathway. In the reverse molecular docking experiment, the matching scores of the active components and the target were mainly between 6.0 and 7.0, with strong binding activity. Compared to the normal group, the plasma concentrations of BAX, IL-2, Bcl-2, AMS, and CASP3 in the model group were significantly increased (P < 0.05). Compared with the model group, the low-dose group of Qingyi II granules only significantly reduced IL-2 levels and had no effect on other indicators. The other groups could significantly reduce the levels of AMS, BAX, and CASP3 (P < 0.05). Compared with the model group, the octreotide group and Qingyi II granules high-dose group significantly increased the Bcl-2 level (P < 0.05), and there was no statistical difference in other drug-administered groups. Compared with the normal group, the expression of AKT1 and PIK3CA in the pancreas of the model group was significantly higher. Compared to the model group, the expression of PIK3CA was low in all drug-administered groups. In addition to the low-dose group, the other drug-administered groups significantly reduced the expression of AKT1. Qingyi can reduce the levels of AMS, BAX, IL-2, and CASP3 and increase the levels of Bcl-2. This mechanism may be related to the PI3K- AKT signaling pathway.

Stems and leaves of Aconitum carmichaelii Debx. as potential herbal resources for treating rheumatoid arthritis: Chemical analysis, toxicity and activity evaluation.

According to folk usage of Aconitum carmichaelii Debx., the present study was designed to determine the feasibility of the stems and leaves of Aconitum carmichaelii Debx. as a new medicinal resource. Fourteen alkaloids in mother roots, fibrous roots, stems, and leaves of Aconitum carmichaelii Debx. were measured by HPLC-MS/MS. And multivariate analysis methods, such as clustering analysis and principal component analysis, were applied to analyze the difference among various parts. In addition, the acute toxicity, analgesia, and anti-inflammatory tests were carried out. The results suggested that the contents of alkaloids in mother roots and fibrous roots were approximate, but those of leaves and stems were different from mother roots and fibrous roots. The results of the acute toxicity testing demonstrated the toxicity of fibrous root was strongest, and mother roots were slightly less toxic than fibrous roots. The stems and leaves were far less toxic than mother and fibrous roots. In addition, the analgesia and inflammatory tests showed the effects of the various tissues had no difference each other. These results provided a basis for developing new complementary and alternative treatments for rheumatoid arthritis patients. Simultaneously, the approach may also turn wastes into treasure and promote the development of circular economy.

[Dermatopharmacokinetic studies of liangfu cream in mice skin].

OBJECTIVE: To study the relationship between deposition content and time of the active ingredients in rat skin, and investigate the dermatopharmacokinetics of Liangfu Cream. METHOD: The contents of paeonol, dictamnine, fraxinellone and glycyrrhetinic acid in rat skin were determined by HPLC. The dermatopharmacokinetics parameters were calculated by DAS software. RESULT: The dermatopharmacokinetics of paeonol and glycyrrhetinic acid were two compartment model, while that of dictamnine and fraxinellone were one compartment model: T(1/2Ka) of four active ingredients were 0.307, 0.112, 0.146, 0.216 h, respectively; T(lag) of them were 0.006, 0.123, 0.136, 0.109 h, respectively; all the Tmax of them was 0.5 h; the Cmax, were 40.163, 1.607, 6.725, 100.553 microg x cm(-3), respectively; the t(1/2beta), were 14.719, 1.262, 0.838, 234.807 h, respectively; the AUC(0-infinity), were 16.987, 2.713, 9.345, 697.000 microg x cm(-3) x h(-1), respectively; and the MRT(0-infinity) were 3.662, 1.67, 1.585, 10.897, respectively. CONCLUSION: The skin pharmacokinetics characteristic of four ingredients in Liangfu cream is lined with the cataplasm long time.

[Effects of penetration enhancers on in vitro percutaneous absorption and amount retained in skin of paeonol, dictamnine, fraxinellone and glycyrrhetinic acid in Liangfu cream].

OBJECTIVE: To study the effects of different penetration enhancers on the in vitro percutaneous absorption and amount retained in skin of active ingredients in Liangfu cream and to screen out the effective accelerator. METHOD: Using improved Franz-type difusion cell and excised small mouse skin in vitro as transdermal barrier, the amount retained in skin and kinetics parameters of active ingredients such as cumulative permeation quantity, permeation rate and permeation lagged time were determined by HPLC. The enhancement ability of four different enhancers such as azone, oleic acid, transcutol P and isopropyl myristate were investigated. RESULT: 3% IPM enhanced the cumulative permeation quantity better than other penetration enhancers. The enhancive permeation multiples of paeonol, dictamnine, fraxinellone and glycyrrhetinic acid were 1.52, 1.24, 1.73 and 3.21 times (P < 0.05). The enhancive amount retained in skin multiple of glycyrrhetinic acid was 1.96 times (P < 0.05), but for other components there were no significant impacts. CONCLUSION: The effects of penetration enhancers on the in vitro percutaneous absorption and amount retained in skin of components in Liangfu cream are different. 3% IPM which can enhance the cumulative permeation quantity of four components and amount retained in skin of glycyrrhetinic acid is the most suitable penetration enhancer for Liangfu cream.