Neuroprotective Effects of Ginseng Phytochemicals: Recent Perspectives.

As our global population ages, the treatment of neurodegenerative diseases is critical to our society. In recent years, researchers have begun to study the role of biologically active chemicals from plants and herbs to gain new inspiration and develop new therapeutic drugs. Ginseng (Panax ginseng C.A. Mey.) is a famous Chinese herbal medicine with a variety of pharmacological activities. It has been used to treat various diseases since ancient times. Extensive research over the years has shown that ginseng has potential as a neuroprotective drug, and its neuroprotective effects can be used to treat and prevent neurological damage or pathologically related diseases (such as Alzheimer's disease, Parkinson's disease, Huntington's disease, depression symptoms, and strokes). Moreover, evidence for the medicinal and health benefits of ginsenoside, its main active ingredient, in the prevention of neurodegenerative diseases is increasing, and current clinical results have not reported any serious adverse reactions to ginseng. Therefore, we briefly review the recent research and development on the beneficial effects and mechanisms of ginseng and its main active ingredient, ginsenoside, in the prevention and treatment of neurodegenerative diseases, hoping to provide some ideas for the discovery and identification of ginseng neuroprotection.

Formulation and Characterization of Novel Dry Suspension and Dry Emulsion of 20(S)-Protopanaxadiol.

To improve the absorption of poorly water-soluble 20(S)-protopanaxadiol (20(S)-PPD), novel 20(S)-PPD-loaded redispersible dry suspension and dry emulsion were developed in this study. 20(S)-PPD dry suspension (PPD-DS) was prepared by enabling drug fully dispersed with suspending agent Avicel CL611 and solubilizer Poloxamer 188. 20(S)-PPD dry emulsion (PPD-DE) was prepared by employing oleic acid as oil phase, Cremophor RH-40 as surfactant, and n-butyl alcohol as co-surfactant. Both PPD-DS and PPD-DE were evaluated for their physicochemical characterization after being dispersed in distilled water. The in vivo pharmacokinetics was evaluated by UPLC-MS/MS. The droplet size of PPD-DS and PPD-DE was in the scope of 1446-1653 nm and 652.8-784.5 nm. The sedimentation volume ratios of PPD-DS and PPD-DE were both at value of 1. The zeta potential of PPD-DS and PPD-DE were from - 53.7 to - 70.4 mV and - 27.5 to - 34.5 mV, respectively, which indicated stable systems. PPD-DS and PPD-DE both achieved dramatically enhanced aqueous solubility and higher perfusion of 20(S)-PPD in rats' intestine. Although statistically, no oral bioavailability enhancements of 20(S)-PPD were achieved in PPD-DE and PPD-DS, there were some improvements in the pharmacokinetic behaviors. Especially, PPD-DS could be a promising drug delivery carrier for 20(S)-PPD with the advantages of long-term stability, dosing flexibility, and the convenience of administering to infants and to those who have difficulty swallowing tablets or capsules.

Techniques for the analysis of pentacyclic triterpenoids in medicinal plants.

Triterpenes are a major class of chemical compounds found in natural plants and can be categorized into acyclic triterpenoids, monocyclic triterpenoids, tricyclic triterpenoids, tetracyclic triterpenoids, and pentacyclic triterpenoids. Among them, pentacyclic triterpenoids have gained more extensive attention due to their biological activities, including anti-inflammation, antibacterial, antioxidation, antitumor, anti-HIV, hepatoprotection, and immunological adjuvant properties. In this review, we summarize the extraction and analytical methods for pentacyclic triterpenoids, where more than 56 triterpenes from 49 kinds of plants were involved. The analysis methods include gas chromatography, liquid chromatography, capillary electrophoresis, thin-layer chromatography, supercritical fluid chromatography, NMR spectroscopy, and X-ray spectroscopy. This review provides valuable reference for the determination of pentacyclic triterpenoids in medicinal plants.

Advances in Pharmaceutical Strategies Enhancing the Efficiencies of Oral Colon-Targeted Delivery Systems in Inflammatory Bowel Disease.

Inflammatory bowel disease (IBD) is a common disease characterized by chronic inflammation in gastrointestinal tracts, which is primarily treated by administering anti-inflammatory and immunosuppressive drugs that inhibit the burden of intestinal inflammation and improve disease-related symptoms. However, the established therapeutic strategy has limited therapeutic efficacy and adverse drug reactions. Therefore, new disease-targeting drug-delivery strategies to develop more effective treatments are urgent. This review provides an overview of the drug-targeting strategies that can be used to treat IBD, and our recent attempts on the colon-specific delivery system (Pae-SME-CSC) with a paeonol-loaded self-microemulsion (Pae-SMEDDS) are introduced.

Comparison of critical methods developed for fatty acid analysis: A review.

Fatty acids are important nutritional substances and metabolites in living organisms. These acids are abundant in Chinese herbs, such as Brucea javanica, Notopterygium forbesii, Isatis tinctoria, Astragalus membranaceus, and Aconitum szechenyianum. This review illustrates the types of fatty acids and their significant roles in the human body. Many analytical methods are used for the qualitative and quantitative evaluation of fatty acids. Some of the methods used to analyze fatty acids in more than 30 kinds of plants, drugs, and other samples are presented in this paper. These analytical methods include gas chromatography, liquid chromatography, near-infrared spectroscopy, and NMR spectroscopy. The advantages and disadvantages of these techniques are described and compared. This review provides a valuable reference for establishing methods for fatty acid determination.

Characterization, Molecular Docking, and In Vitro Dissolution Studies of Solid Dispersions of 20(S)-Protopanaxadiol.

In this study, we prepared solid dispersions (SDs) of 20(S)-protopanaxadiol (PPD) using a melting-solvent method with different polymers, in order to improve the solubility and dissolution performance of drugs with poor water solubility. The SDs were characterized via differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance (NMR), and molecular docking and dynamics study. DSC and PXRD results indicated that PPD crystallinity in SDs was significantly reduced, and that the majority of PPD is amorphous. No interaction was observed between PPD and polymers on FTIR and NMR spectra. Molecular docking and dynamic calculations indicated that the PPD molecule localized to the interpolated charged surface, rather than within the amorphous polymer chain network, which might help prevent PPD crystallization, consequently enhancing the PPD dispersion in polymers. An in vitro dissolution study revealed that the SDs considerably improved the PPD dissolution performance in distilled water containing 0.35% Tween-80 (T-80). Furthermore, among three PPD-SDs formulations, Poloxamer188 (F68) was the most effective in improving the PPD solubility and was even superior to the mixed polymers. Therefore, the SD prepared with F68 as a hydrophilic polymer carrier might be a promising strategy for improving solubility and in vitro dissolution performance. F68-based SD, containing PPD with a melting-solvent preparation method, can be used as a promising, nontoxic, quick-release, and effective intermediate for other pharmaceutical formulations, in order to achieve a more effective drug delivery.

Optimization of Ultrasonic-assisted Extraction of Fatty Acids in Seeds of Brucea Javanica (L.) Merr. from Different Sources and Simultaneous Analysis Using High-Performance Liquid Chromatography with Charged Aerosol Detection.

Our research aimed to optimize the oil extraction process and determine the fatty acids in Brucea javanica (L.) Merr. seeds. The extraction technology was optimized using response surface methodology. A Box-Behnken design was employed to investigate the effects of three independent variables on an ultrasonic-assisted extraction technique, namely, sonication time (X1: 20-40 min), liquid-solid ratio (X2: 16:1 mL/g-24:1 mL/g), and ethanol concentration (X3: 90%-100%). The optimum conditions of sonication time, liquid-solid ratio, and ethanol concentration were 40 min, 24:1 mL/g, and 100%, respectively. The content of fatty acids and the oil yield were 14.64 mg/g and 16.87%, respectively, which match well with the predicted models. The optimum number of extraction times was eventually identified as two. A new rapid method for the qualitative and quantitative analysis of the fatty acids of B. javanica (L.) Merr. seed oil using HPLC with a charged aerosol detector was described. The fatty acid contents of 14 batches of B. javanica (L.) Merr. seed oil were determined, and the relevance and difference were analyzed by fingerprint analysis. The fingerprint has five common peaks, and the similarity was greater than 0.991. HPLC analysis represents a specialized and rational approach for the quality identification and comprehensive evaluation of B. javanica (L.) Merr. seed oils.

20(S)-Protopanaxadiol Phospholipid Complex: Process Optimization, Characterization, In Vitro Dissolution and Molecular Docking Studies.

20(S)-Protopanaxadiol (PPD), a bioactive compound extracted from ginseng, possesses cardioprotective, neuroprotective, anti-inflammatory, antiestrogenic, anticancer and anxiolytic effects. However, the clinical application of PPD is limited by its weak aqueous solubility. In this study, we optimized an efficient method of preparing its phospholipid complex (PPD-PLC) using a central composite design and response surface analysis. The prepared PPD-PLC was characterized by differential scanning calorimetric, powder X-ray diffraction, Fourier-transformed infrared spectroscopy and nuclear magnetic resonance analyses associated with molecular docking calculation. The equilibrium solubility of PPD-PLC in water and n-octanol increased 6.53- and 1.53-times, respectively. Afterwards, using PPD-PLC as the intermediate, the PPD-PLC-loaded dry suspension (PPD-PLC-SU) was prepared with our previous method. In vitro evaluations were conducted on PPD-PLC and PPD-PLC-SU, including dissolution behaviors and stability properties under different conditions. Results of in vitro dissolution behavior revealed the improved dissolution extents and rates of PPD-PLC and PPD-PLC-SU (p < 0.05). Results of the formulation stability investigation also exposed the better stability of PPD-PLC-SU compared with free PPD. Therefore, phospholipid complex technology is a useful formulation strategy for BCS II drugs, as it could effectively improve their hydrophilicity and lipophilicity.

Self-microemulsifying Drug Delivery System Improved Oral Bioavailability of 20(S)-Protopanaxadiol: From Preparation to Evaluation.

20(S)-Protopanaxadiol (20(S)-PPD) is one type of sapogenin of protopanaxadiols and has a variety of pharmacological activities. In order to improve the dissolution of 20(S)-PPD as well as its oral bioavailability, a self-microemulsifying drug delivery system (SMEDDS) was utilized for 20(S)-PPD preparation. Following the preparation of the 20(S)-PPD SMEDDS, its dissolution, stability, and intestinal absorption in rats were studied, and the pharmacokinetics and optimal dosage after oral administration were evaluated. The dissolution tendency of the SMEDDS in phosphate buffered saline (PBS), 0.1 M HCl and distilled water was consistent. SMEDDS was stable under a condition of high temperature (40°C), high humidity or with strong light irradiation, or within 6 h in artificial digestive tracts. 20(S)-PPD SMEDDS was well-absorbed in all intestinal segments in rats. When the drug concentration was higher than 200 µg/mL or the perfusion flow was faster than 0.5 mL/min, passive diffusion of drug in the duodenum reached a saturated level. In addition, P-glycoprotein inhibitor did not affect the intestinal absorption of 20(S)-PPD SMEDDS. Pharmacokinetic study showed that Tmax in male rats was shortened significantly, while Cmax and area under the curve (AUC(0-t)) were remarkably increased. The relative oral bioavailability of 20(S)-PPD SMEDDS was increased approximately three fold compared with the 20(S)-PPD carboxy methyl cellulose (CMC). 20(S)-PPD SMEDDS (100 mg/mL) was administered by gastric infusion to both mice and rats for 14 d. SMEDDS improved the oral bioavailability of 20(S)-PPD and reduced the necessary drug dosage. 20(S)-PPD SMEDDS could become a promising clinical alternative as an anti-tumor or antidepressant drug.

Effects of aqueous extracts and volatile oils prepared from Huaxiang Anshen decoction on p-chlorophenylalanine-induced insomnia mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Insomnia occurs frequently in modern society, and its common symptoms include difficulty in falling asleep and decreased sleep quality and time, memory, and attention. With the advantages of having few side-effects and reduced drug-dependence, a compound traditional Chinese medicine (TCM) prescription called Huaxiang Anshen Decoction (HAD) has been widely used in clinical practice in China mainly for primary insomnia treatment. Although the effects of volatile oils from TCM herbs have been increasingly reported, volatile oils in HAD are conventionally neglected because of its preparation process and clinical usage. Therefore, exploring the anti-insomnia effects of volatile oils from HAD is of great importance. AIM OF THE STUDY: The sedative and hypnotic effects of the conventional aqueous extracts, the volatile oils from HAD, and their combinations were investigated. METHODS: The main components in HAD volatile oils (HAD-Oils), were analyzed through gas chromatography-mass spectrometry (GC-MS). The HAD volatile oil inclusion complex (HAD-OIC) was prepared with ß-cyclodextrin, and characterized. P-chlorophenylalanine (PCPA) was used to induce insomnia mice model and the test groups of HAD aqueous extract (HAD-AE), HAD-OIC and their combination (AE-OIC). An open field test was used in evaluating the mice's activities, and the levels of 5-hydroxytryptamine (5-HT) in mice sera, glutamate (Glu) in the hypothalamus, and γ-aminobutyric acid (γ-GABA) and dopamine (DA) in the brain tissues were assayed by enzyme-linked immunosorbent assay (ELISA). RESULTS: A total 74 components in HAD-Oil were determined by GC/MS, and cyperenone (20.46%) and α-cyperone (10.39%) had the highest relative content. The characterization results of the physical phase showed that volatile oils were successfully encapsulated by ß-cyclodextrin and HAD-OIC was produced. The average encapsulation rates of cyperenone and α-cyperone were 79.93% and 71.96%, respectively. The results of pharmacology study showed that all the test groups increased the body weight and decreased voluntary activity when compared with the model group (P < 0.05). The HAD-AE, HAD-OIC, and AE-OIC groups increased the levels of 5-HT in the sera and DA and Glu/γ-GABA in the brains, and AE-OIC groups showed better performance than the other test groups. CONCLUSIONS: HAD-Oil exerts sedative and hypnotic effects, which are increased when it is used with HAD-AEs. This result provides a favorable experimental evidence that volatile oils should be retained for the further development of HAD.

Rapid and Sensitive Determination of Timosaponin AIII in Rat Plasma by LC-MS/MS and Its Pharmacokinetic Application.

A rapid sensitive and selective liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for determination of timosaponin AIII (TA-III) in rat plasma, using ginsenoside Re as an internal standard (IS). TA-III and the IS were detected in MRM mode with a negative ionization electrospray mass spectrometer. The calibration curves were linear over the concentration ranges from 11.14 to 1114 ng/mL and the lower limit of quantification (LLOQ) was 11.14 ng/mL. Intra-day and inter-day precisions (RSD) were within 10%, and accuracy ranged from 6.4% to 9.1%. The extraction recovery at three concentrations ranged from 92.3% to 95.5%. The validated method was successfully applied to monitor the concentrations of TA-III in rat plasma after intragastric administration. The best fit pharmacokinetic model to estimate the pharmacokinetic parameters was a single compartment model with weight of 1/x2 for oral administration groups of rats for TA-III.

Bioactive components of Banxia Xiexin Decoction for the treatment of gastrointestinal diseases based on flavor-oriented analysis.

ETHNOPHARMACOLOGICAL RELEVANCE: Banxia Xiexin Decoction (BXD) was first recorded in a Chinese medical classic, Treatise on Febrile Diseases and Miscellaneous Diseases, which was written in the Eastern Han dynasty of China. This ancient prescription consists of seven kinds of Chinese herbal medicine, namely, Pinellia ternata, Rhizoma Coptidis, Radix scutellariae, Rhizoma Zingiberis, Ginseng, Jujube, and Radix Glycyrrhizaepreparata. In clinic practice, its original application in China mainly has focused on the treatment of chronic gastritis for several hundred years. BXD is also effective in treating other gastrointestinal diseases (GIDs) in modern medical application. Despite available literature support and clinical experience, the treatment mechanisms or their relationships with the bioactive compounds in BXD responsible for its pharmacological actions, still need further explorations in more diversified channels. According to the analysis based on the five-flavor theory of TCM, BXD is traditionally viewed as the most representative prescription for pungent-dispersion, bitter-purgation and sweet-tonification. Consequently, based on the flavor-oriented analysis, the compositive herbs in BXD can be divided into three flavor groups, namely, the pungent, bitter, and sweet groups, each of which has specific active ingredients that are possibly relevant to GID treatment. AIM OF THE REVIEW: This paper summarized recent literatures on BXD and its bioactive components used in GID treatment, and provided the pharmacological or chemical basis for the further exploration of the ancient prescription and the relative components. METHOD: ology: Relevant literature was collected from various electronic databases such as Pubmed, Web of Science, and China National Knowledge Infrastructure (CNKI). Citations were based on peer-reviewed articles published in English or Chinese during the last decade. RESULTS: Multiple components were found in the pungent, bitter, and sweet groups in BXD. The corresponding bioactive components include gingerol, shogaol, stigmasterol, and ß-sitosterol in the pungent group; berberine, palmatine, coptisine, baicalein, and baicalin in the bitter group; and ginsenosides, polysaccharides, liquiritin, and glycyrrhetinic acid in the sweet group. These components have been found directly or indirectly responsible for the remarkable effects of BXD on GID. CONCLUSION: This review provided some valuable reference to further clarify BXD treatment for GID and their possible material basis, based on the perspective of the flavor-oriented analysis.

[Purification of geniposide in the extract fluid of Gardenia jasminoides with macroporous absorption resin].

OBJECTIVE: To optimize the process for purification of geniposide in the extract fluid of Gardenia jasminoides with macroporous absorption resin. METHODS: By comparing the content and transfer ratio of geniposide during the process of purification, we optimized the process for purification of geniposide. RESULTS: The optimal process for purification of geniposide with D301R macroporous absorption resin included the diameter height ratio 1:7.5, the concentration of the extract fluid of Gardenia jasminoides 2:1, the flow rate 1BV/h (1BV represented one column volume), the sample volume 1/3BV. We loaded the sample and left it for 2 hours, afterwards, rinsed the macroporous absorption resin using 2BV water until the solution became colourless. Then we rinsed the macroporous absorption resin with 20% alcohol,and the volume of elution solvent was 2BV. We collected 20% alcohol elution solvent and recycle alcohol using rotating evaporation and dried the rest solution in a vacuum to get the light yellow powder which was the purified geniposide. CONCLUSION: This process is simple and affordable, can be used to refine and purify geniposide in the extract fluid of Gardenia jasminoides Ellis. It provides a guidance for industrial production basis.

[Technology study on extraction and purification of alkaloid from Stemona japonica].

OBJECTIVE: In order to obtain the optimal conditions for separating the alkaloids from the extract of Stemona japonica by selecting appropriate cation exchange resins. METHODS: Seven types of cation exchange resins were evaluated in separating efficiency with measuring the adsorption ratio and eluting ratio of total alkaloids as indices, and the content of total alkaloids from Stemona japonica was determined as an index by spectrophotometry to choose the optimal technological parameters. RESULTS: The optimal result of extraction was obtained as Stemona japonica shattered into thick powder, adding eight times amount of 90% alcohol and refluxing and extracting for 3 h (totally extracting for 3 times). Each gram of D004 cation exchange resin could absorb 0.5003 mg of the total alkaloid, and the desorption ratio was 68.45%. The transfer rate of total alkaloids was 58.70%. the product purity of alkaloids was up to 70%. CONCLUSION: The D004 cation exchange resin can be used for purificating total alkaloids from Stemona japonica and the established procedure is simple and feasible.

Comparison of Pinoresinol and its Diglucoside on their ADME Properties and Vasorelaxant Effects on Phenylephrine-Induced Model.

Pinoresinol (PINL) and pinoresinol diglucoside (PDG), two natural lignans found in Eucommia ulmoides Oliv. (Duzhong), have several pharmacological activities. However, there is no report available on their absorption, distribution, metabolism, and elimination (ADME) properties. Given the possible wide spectrum of their application in therapeutic areas, this area should be investigated. This work studied the in vitro ADME properties of PDG and PINL, including their kinetic solubility, permeability across monolayer cells (PAMPA), protein binding, and metabolic stabilities in liver microsomes. The in vivo pharmacokinetic study and in vitro vasorelaxant effects on isolated phenylephrine-induced aortic rings of PINL and PDG were also investigated. It was found that both of their kinetic solubility in PBS (pH 7.4) was greater than 100 µM, indicating that they are both soluble compounds. The permeability investigations (P eff ) by PAMPA indicated that PINL had higher permeability than PDG (p < 0.05). Both components represented moderate plasma protein binding activities (average binding rate in human plasma: PINL 89.03%, PDG 45.21%) and low metabolic rate (t 1/2 in human liver microsome: PINL 1509.5 min, PDG 1004.8 min). Furthermore, the results of pharmacokinetic studies indicated that PINL might be eliminated less quickly than PDG from the rat plasma, and its cumulative urinary excretion was much lower than that of PDG. The phenylephrine-induced aortic rings demonstrated concentration-dependent vasorelaxation in PDG, PINL, or their combination group. The vasorelaxant effects of PINL were more obvious than those of PDG, whereas the vasorelaxant effect of the combinations was significantly better than that of the single component (p < 0.05). The similarity or difference between PINL and its diglucoside in these pharmaceutical aspects may offer valuable insights into the further exploration of lignans and might contribute to relevant studies involving natural products with similar molecular structure and their glucosides.

Exploration of the potential mechanism of Banxia Xiexin Decoction for the effects on TNBS-induced ulcerative colitis rats with the assistance of network pharmacology analysis.

ETHNOPHARMACOLOGICAL RELEVANCE: Banxia Xiexin Decoction (BXD), an ancient TCM prescription originating from Treatise on Febrile Diseases (Shang Han Lun) of the Han Dynasty, has been widely used in modern clinical practice, especially for gastrointestinal diseases, including ulcerative colitis (UC). However, the modern decoction method of BXD differs from that of the original method. Thus, an exploration of the influence of the different decoction methods on the pharmacological effects is interesting and significant. AIM OF THE STUDY: This study aimed to systematically compare the pharmacological effects of extracts of BXD on TNBS induce UC rats that were prepared by different methods, the ancient method and the modern method. The findings may provide important information for the further mechanical exploration of the classical prescription, contributing to the rational application and enhancing the understanding of BXD in modern applications or scientific research. METHODS: Fifty-four SD rats were randomly divided into the following nine groups at n = 6/group: control group; model group; salicylazosulfapyridine group; BXD ancient extraction method's low-dose group (BXD-AED-L, 3.6 g BXD-AED/kg), medium-dose group (BXD-AED-M, 7.2 g BXD-AED/kg), and high-dose group (BXD-AED-H, 14.4 g BXD-AED/kg); and BXD modern extraction method's low-dose group (BXD-MED-L, 1 g BXD-MED/kg), medium-dose group (BXD-MED-M, 2 g BXD-MED/kg), and high-dose group (BXD-MED-H, 4 g BXD-MED/kg). All the groups, except the control group, were rectally injected with 70 mg/kg ethanol solution containing TNBS (2,4,6-trinitrobenzenesulfonic acid) to establish the UC models. The pharmacological evaluations including disease activity index, colon weight index, macroscopic and histological evaluation of colon damage, and inflammatory cytokine levels (IL-4, IL-10, IL-1ß, TNF-α, and IL-6)were measured. In the network pharmacology analysis, the "herbs-components-targets-disease" network was constructed and visually analyzed with which the targets with a strong correlation with UC were screened out. RESULTS: The results showed that both BXD-AED and BXD-MED might alleviate the severity of UC with different degrees according to the majority of indices that were evaluated. At similar doses, the BXD-AED groups performed better compared with the BXD-MED groups. With the assistance of the network pharmacology analysis, some key active components (quercetin, baicalein, wogonin, and baicalin) related to the anti-UC/inflammation were screened out. The contents of the components in BXD-AED were higher than those in BXD-MED. The joint results of the study indicated that BXD, an ancient TCM compound prescription, is an effective drug candidate for the modern treatment of UC.

Effects of Paeonol and Gastroretention Tablets of Paeonol on Experimental Gastric Ulcers and Intestinal Flora in Rats.

Paeonol, a major ingredient isolated from Moutan Cort, has various pharmacological effects. Our previous studies have shown that paeonol can exert antioxidant and anti-inflammatory therapeutic effects on ethanol-induced experimental gastric ulcer (GU). Therefore, in this study, we designed two GU models in rats induced by pyloric ligation (PL) and acetic acid and evaluated the protective effects of paeonol and gastroretention tablets of paeonol (GRT-Ps; 24, 48, and 96 mg/kg) on GU in rats and the effect of paeonol (48 mg/kg) on the intestinal flora. In vivo experiments showed that paeonol or GRT-Ps remarkably reduced gastric mucosal damage in a dose-dependent manner in the different types of models and improved the superoxide dismutase (SOD) activity and the malondialdehyde (MDA) content. And in fact, the sustained-release effect of GRT-Ps is more conducive to the improvement of GU compared with the rapid clearance of free drugs. In the PL-induced model, gastric secretion parameters, that is, pH and total acid, showed significant differences compared with the model group. In addition, paeonol treatment can improve the richness and diversity of the intestinal flora and increase the amount of beneficial bacteria, such as Lactobacillus. Paeonol and its stable sustained-release tablet GRT-Ps can promote ulcer healing by inhibiting oxidative stress and regulating the intestinal flora. This study can provide basis for the clinical treatment of GU with paeonol. Graphical Abstract.

Patchouli Alcohol: a Natural Sesquiterpene Against Both Inflammation and Intestinal Barrier Damage of Ulcerative Colitis.

Ulcerative colitis (UC) is a chronic and relapsing inflammatory disorder of the gastrointestinal tract, characterized by diarrhea, hematochezia, abdominal distension, and abdominal pain. The perpetuation of inflammation and the impairment of the intestinal barrier are part of the main courses of UC, responsible for the deteriorating inflammatory condition. Patchouli alcohol (PA), extracted from Pogostemon cablin Benth., is employed to treat both inflammation and intestinal barrier damage. Its curative effect on UC was testified firstly by TNBS-induced UC, a chemically induced colitis, and further tested by DSS-induced UC, an acute attack stage of UC in which the clinical course of human UC occurs frequently. PA reduced the levels of TNF-α, IFN-γ, IL-1ß, IL-6, and IL-17 in serum and decreased the mRNA expression of pro-inflammatory cytokines (e.g., iNOS, COX-2, TNF-α, IL-1ß, and IL-6). Concurrently, PA upregulated the expression of tight junction protein (e.g., ZO-1, ZO-2, claudin-1, and occludin) and the mRNA of mucin-1 and mucin-2 in both animal models. Further, PA ameliorated both histological damage and clinical parameters. Thus, PA could credibly reduce the expression of pro-inflammatory cytokines, protect the integrity of intestinal epithelial barrier, and repair the macroscopic colon lesions in both colitis models.

Fast and non-derivative method based on high-performance liquid chromatography-charged aerosol detection for the determination of fatty acids from Agastache rugosa (Fisch. et Mey.) O. Ktze. seeds.

This study utilised response surface methodology to optimise the conditions for the extraction of A. rugosa seeds oil (ARO). Single-factor experiment and response surface methodology (RSM) were performed to identify the extraction time, liquid-solid ratio and extraction temperature that provided the highest yield of ARO. The optimal extraction time, liquid-solid ratio and extraction temperature were 8 h, 4:1 mL/g and 55 °C. The fatty acids (FAs) content and oil yield obtained through the optimised impregnation-extraction process were 19.67 mg/g and 32.1%. These values matched well with the predicted values. Linolenic acid was identified to be the main active ingredient of ARO. The high-performance liquid chromatography-charged aerosol detection method presented here is fast and does not require derivatisation. Therefore, it could be used to quantitatively analyse the FAs present in ARO and applied to detect compounds with low or no ultraviolet response.

Analytical methods and biological activities of Panax notoginseng saponins: Recent trends.

ETHNOPHARMACOLOGICAL RELEVANCE: Panax notoginseng (Burk.) F. H. Chen, also called Sanqi, is a widely used traditional Chinese medicine, which has long history used as herbal medicines. It is currently an important medicinal material in China, holding the first place in the sale volume of the whole patent medicines market in China, and the market size of the single species has exceeded 10 billion yuan. In addition, P. notoginseng is an important constituent part of many famous Chinese patent medicines, such as Compound Danshen Dripping Pills and Yunnan Baiyao. P. notoginseng saponins (PNSs), which are the major active components of P. notoginseng, are a kind of chemical mixture containing different dammarane-type saponins. Many studies show that PNSs have been extensively used in medical research or applications, such as atherosclerosis, diabetes, acute lung injury, cancer, and cardiovascular diseases. In addition, various PNS preparations, such as injections and capsules, have been made commercially available and are widely applied in clinical practice. AIM OF THE REVIEW: Since the safety and efficacy of compounds are related to their qualitative and quantitative analyses, this review briefly summarizes the analytic approaches for PNSs and their biological effects developed in the last decade. METHODOLOGY: This review conducted a systematic search in electronic databases, such as Pubmed, Google Scholar, SciFinder, ISI Web of Science, and CNKI, since 2009. The information provided in this review is based on peer-reviewed papers and patents in either English or Chinese. RESULTS: At present, the chromatographic technique remains the most extensively used approach for the identification or quantitation of PNSs, coupled with different detectors, among which the difference mainly lies in their sensitivity and specificity for analyzing various compounds. It is well-known that PNSs have traditionally strong activity on cardiovascular diseases, such as atherosclerosis, intracerebral hemorrhage, or brain injury. The recent studies showed that PNSs also responded to osteoporosis, cancers, diabetes, and drug toxicity. However, some other studies also showed that some PNSs injections and special PNS components might lead to some biological toxicity under certain dosages. CONCLUSION: This review may be used as a basis for further research in the field of quantitative and qualitative analyses, and is expected to provide updated and valuable insights into the potential medicinal applications of PNSs.