Cortex Lycii Research Articles

Effect of "maccog" TCM tea on improving glucolipid metabolism and gut microbiota in patients with type 2 diabetes in community.

This work aimed to observe the effect of consuming Chinese herb tea on glucolipid metabolism and gut microbiota in patients with type 2 diabetes mellitus (T2DM). Ninety patients with T2DM were recruited from a community and randomly divided into the control group (CG) and intervention group (IG). CG maintained conventional treatment and lifestyle, and IG accepted additional "maccog" traditional Chinese medicine (TCM) tea (mulberry leaf, radix astragali, corn stigma, cortex lycii, radix ophiopogonis, and gynostemma) for 12 weeks. Glucolipid metabolism, hepatorenal function, and gut microbiota were then measured. After the intervention, the decreases in fasting plasma glucose (FPG) and total cholesterol (TC) were greater (P<0.05) in IG than in CG, and those in glycosylated serum protein (GSP) were almost significantly greater (P=0.066) in IG than in CG. The total protein (TP), albumin (ALB), and creatinine (CREA) levels in IG were significantly lower and their decreases were larger in IG than in CG (P<0.05) after the intervention. The Ace and Chao1 indices in IG were slightly higher after the intervention (P=0.056 and 0.052, respectively) than at baselines. The abundance of Actinobacteria, Lachnospiraceae, Bifidobacteriaceae, and Phascolarctobacterium increased significantly after the intervention in IG (P<0.05), and the abundance was higher in IG than in CG (P<0.05 or P<0.1). The abundance of Clostridiales and Lactobacillales was negatively correlated with FPG (P<0.05), Clostridiales and Lachnospiraceae was negatively correlated with GSP (P<0.05), and Bacteroides/Firmicutes was positively correlated with both (P<0.05). No adverse event was observed during the intervention. Administration of "maccog" TCM tea for 12 weeks slightly improved glucolipid metabolism and significantly increased the abundance of beneficial gut microbiota in community patients with T2DM. The increase in beneficial bacteria abundance may be involved in the improvement of glucose metabolism indicators. In addition, this intervention is safe and feasible. https://www.chictr.org.cn/showproj.aspx?proj=31281, identifier ChiCTR1800018566.

Optimization of extraction process of total flavonoids from Cortex Lycii and its biological activities

Optimization of extraction process of total flavonoids from Cortex Lycii and its biological activities

Exploring the therapeutic effects of Cortex Lycii on essential hypertension

Exploring the therapeutic effects of Cortex Lycii on essential hypertension

Action mechanism of hypoglycemic principle 9-(R)-HODE isolated from cortex lycii based on a metabolomics approach.

The 9-(R)-HODE is an active compound isolated from cortex lycii that showed significant hypoglycemic effects in our previous in vitro study. In this study, 9-(R)-HODE's in vivo hypoglycemic activity and effect on alleviating diabetic complications, together with its molecular mechanism, was investigated using a metabolomics approach. The monitored regulation on dynamic fasting blood glucose, postprandial glucose, body weight, biochemical parameters and histopathological analysis confirmed the hypoglycemic activity and attenuation effect, i.e., renal lesions, of 9-(R)-HODE. Subsequent metabolomic studies indicated that 9-(R)-HODE induced metabolomic alterations primarily by affecting the levels of amino acids, organic acids, alcohols and amines related to amino acid metabolism, glucose metabolism and energy metabolism. By mediating the related metabolism or single molecules related to insulin resistance, e.g., kynurenine, myo-inositol and the branched chain amino acids leucine, isoleucine and valine, 9-(R)-HODE achieved its therapeutic effect. Moreover, the mediation of kynurenine displayed a systematic effect on the liver, kidney, muscle, plasma and faeces. Lipidomic studies revealed that 9-(R)-HODE could reverse the lipid metabolism disorder in diabetic mice mainly by regulating phosphatidylinositols, lysophosphatidylcholines, lysophosphatidylcholines, phosphatidylserine, phosphatidylglycerols, lysophosphatidylglycerols and triglycerides in both tissues and plasma. Treatment with 9-(R)-HODE significantly modified the structure and composition of the gut microbiota. The SCFA-producing bacteria, including Rikenellaceae and Lactobacillaceae at the family level and Ruminiclostridium 6, Ruminococcaceae UCG 014, Mucispirillum, Lactobacillus, Alistipes and Roseburia at the genus level, were increased by 9-(R)-HODE treatment. These results were consistent with the increased SCFA levels in both the colon content and plasma of diabetic mice treated with 9-(R)-HODE. The tissue DESI‒MSI analysis strongly confirmed the validity of the metabolomics approach in illustrating the hypoglycemic and diabetic complications-alleviation effect of 9-(R)-HODE. The significant upregulation of liver glycogen in diabetic mice by 9-(R)-HODE treatment validated the interpretation of the metabolic pathways related to glycogen synthesis in the integrated pathway network. Altogether, 9-(R)-HODE has the potential to be further developed as a promising candidate for the treatment of diabetes.

Kukoamine A Improves Mycoplasma pneumoniae Pneumonia by Regulating miR-222-3p/Superoxide Dismutase 2.

Mycoplasma pneumoniae pneumonia (MPP) represents a common respiratory disease in children patients. Kukoamine A (KuA) is a spermine alkaloid found in the Chinese herb Cortex Lycii radices, which has a variety of pharmacological properties. However, no study has been reported on the role of KuA in MPP. Exosomes, a type of lipid bilayer-enclosed extracellular vesicles, can be delivered to the target cells, where they regulate function and physiology. With the use of human alveolar basal epithelial cells (HABECs) as an in vitro model, in this study, we sought to characterize the changes in levels of superoxide dismutase 2 (SOD2) and proinflammatory cytokines including IL-6 and TNF-α in HABECs in response to exosomes, which were isolated from peripheral blood serum of MPP patients. We found that, compared to normal, MPP patients exhibited a significant up-regulated miR-222-3p. Further, exosomal miR-222-3p downregulated SOD2 activity but promoted nuclear NF-κB activity and expression of IL-6 and TNF-α in HABECs, ultimately leading to an oxidative stress condition. Interestingly, such stimulating effects were attenuated by the pretreatment of KuA. This study suggests a critical role possessed by KuA in MPP by regulating the miR-222-3p/SOD2 axis, which represents a promising strategy for the treatment of MPP.

Study on the mechanism of Cortex Lycii on lung cancer based on network pharmacology combined with experimental validation

Ethnopharmacological relevanceXie Bai San is a Chinese medicine prescription that has been used to treat lung cancer in China for a long time. It has been proven to alleviate the symptoms and extend the survival time of lung cancer patients. Xie Bai San comprises Cortex Lycii, Cortex Mori, and Radix Glycyrrhizae Preparata. The effects and mechanisms of Cortex Mori and Glycyrrhizae on lung cancer have been reported, whereas the underlying mechanism of Cortex Lycii remains unknown. Material and methodsNetwork pharmacology was used to explore the unknown mechanisms underlying the effect of Cortex Lycii on lung cancer. Molecular docking was used to predict the binding of a compound to the protein. The fingerprint of Cortex Lycii was obtained by HPLC. Cell counting Kit-8 assay was used to determine the appropriate concentration of Cortex Lycii extract for human lung adenocarcinoma cells, A549 and H1299. Wound healing assay and Matrigel invasion assay were used to detect the influence of Cortex Lycii extract on the migration and invasion ability of A549 and H1299. The protein expression level was detected by western blot and immunohistochemical staining. ResultsUsing network pharmacology, 38 components of Cortex Lycii and 79 possible lung cancer-related target genes of Cortex Lycii were obtained. The targets were assigned to 35 Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways and the PI3K-AKT signaling pathway contained the most targets and had the second-lowest P-value. The molecular docking showed the components of Cortex Lycii bound to HSP90AB1. Among them, 6 components bound to HSP90AB1 in which HSP90AB1 binds to and phosphorylates AKT. The functional experiments showed that Cortex Lycii suppressed the migration and invasion of human lung cancer cells in a dose-dependent manner. Cortex Lycii up-regulated E-Cadherin and down-regulated N-Cadherin, Vimentin, and MMP2. Furthermore, Cortex Lycii made no change in the total AKT and mTOR protein levels, but caused the down-regulation of p-AKT and p-mTOR in human lung cancer cells, which was reversed by Terazosin, an agonist of HSP90. Moreover, acacetin and apigenin, two components of Cortex Lycii, reduced the protein level of p-AKT and p-mTOR, and the reduction was also inhibited by Terazosin. ConclusionCortex Lycii suppressed epithelial-mesenchymal transition (EMT) in lung cancer cells through the PI3K-AKT-mTOR signaling pathway, possibly by targeting HSP90AB1 and inhibiting HSP90AB1-AKT binding.

Advance on alkaloids of&amp;lt;italic&amp;gt; Lycium&amp;lt;/italic&amp;gt; genus

<p indent=0mm>Natural products derived from medicinal and edible plants, such as polysaccharides, polyphenols, flavonoids, and alkaloids, are a valuable source of potential drug candidates and have attracted interest for their rich structural motifs and diverse physiological activities. Therefore, the discovery of new natural products with unique structures and potential bioactivity from esculent resources has emerged as a promising approach for drug research. In the Solanaceae family, plants of the genus <italic>Lycium</italic> are relatively abundant, containing about 80 species of plants. Of these, seven species and three varieties are found in China where <italic>L</italic>. <italic>barbarum</italic> L., <italic>L</italic>. <italic>chinense</italic> Mill., and <italic>L</italic>. <italic>ruthenicum</italic> Murr. are most common. Among them, <italic>L</italic>. <italic>barbarum</italic> L. and <italic>L</italic>. <italic>ruthenicum</italic> Murr are also major medicinal and edible plant resources in Northwest China. “Gou Qi Zi”, also known as Goji or Goji berry, are fruit from <italic>L</italic>.<italic> barbarum </italic>L., which has been used as a valuable traditional Chinese herbal medicine and functional food for <sc>2500 years.</sc> The earliest recorded mention of these berries is found in the oracle bone script (Jiaguwen) of the Shang Dynasty (1600−1040 BE). Goji berries and Cortex Lycii, which is derived from the root bark of <italic>L</italic>.<italic> chinense</italic> and <italic>L</italic>.<italic> barbarum</italic>, have many pharmacological functions, such as hypoglycemic, hypolipidemic, immuno-modulatory, antioxidant, anti-aging, neuroprotective, and anti-Alzheimer’s disease properties. Medical and pharmaceutical knowledge regarding <italic>L</italic>.<italic> barbarum</italic> has been recorded and summarized in Shennong’s Root and Herbal Classic (Shennong bencao jing) and isolated products are highly desired medicines and contribute to longevity. Li Shizhen also summarized the health and tonic effects of Goji berries in the Compendium of Materia Medica. Many researchers have focused significant attention on the <italic>Lycium </italic>genus in recent years and various chemical components have been isolated. Phytochemical studies have revealed that the genus<italic> Lycium</italic> possesses an abundance of secondary metabolites, such as glycerogalactolipids, phenylpropanoids, coumarins, lignans, flavonoids, amides, alkaloids, anthraquinones, organic acids, terpenoids, sterols, steroids and other small molecules and trace elements. Of these, the alkaloids are considered to be one of the main active ingredients. The aim of this review is to focus on identification and biological activity of alkaloids derived from a variety of species in <italic>Lycium </italic>genus. Up to 2021, at least 124 alkaloids, including 42 amide alkaloids, 31 spermine alkaloids, 17 nortropane alkaloids, 16 pyrrole alkaloids, 4 piperidine alkaloids, 5 imidazole alkaloids, 3 quinoline alkaloids, 3 indole alkaloids, and 3 other alkaloids were reported from different species in the <italic>Lycium </italic>genus. These can be found in diverse plant structures, such as fruits, root bark, leaves, seeds, or flowers. This review lays a solid foundation for better understanding of pharmacological activities of <italic>Lycium-</italic>derived compounds and is systematically summarized on the basis of phytochemical studies. This information provides reference values that should facilitate further investigation on additional pharmacological properties and add to the development and utilization of the<italic> Lycium</italic>.

Identification of α-glucosidase inhibitors from Cortex Lycii based on a bioactivity-labeling high-resolution mass spectrometry–metabolomics investigation

Cortex Lycii, as a kind of traditional Chinese medicines, have shown prospects in the prevention of diabetes and its complications. However, there is comparatively little information regarding the characterization of potentially hypoglycemic compounds derived from Cortex Lycii. In this study, we performed a global non-selective investigation of α-glucosidase inhibitors in Cortex Lycii based on a bioactivity-labeling high-resolution mass spectrometry–metabolomics method. Samples of Cortex Lycii were collected from different Chinese provinces and their ethyl acetate extracts were analyzed using an in vitro α-glucosidase inhibition assay for bioactivity-labeling. The ethyl acetate extracts were also subjected to liquid chromatography-mass spectrometry analysis and multivariate data analysis was subsequently conducted to identify correlations between the bioactivity measured from the enzyme-involved test and the profiles obtained based on high-resolution mass spectrometry. The variables contributing significantly to the separation of the more-active from the less-active samples were considered to indicate the potential target ions of active compounds. MS/MS fragment patterns and nuclear magnetic resonance analyses were used to identify the potential target ions. The developed platform mentioned above facilitated rapid identification of four α-glucosidase inhibitors, namely, N-p-trans-coumaroyltyramine (1), N-trans-caffeoyl-tyramine (2), (9R,10E,12Z)-9-hydroxy-10,12-octadecadienoic acid (3a), and (9S,10E,12Z)-9-hydroxy-10,12-octadecadienoic acid (3b) from Cortex Lycii. The α-glucosidase inhibitory activities of compounds 3a and 3b with IC50 values of 1.0413±0.0551 and 1.0423±0.0049 mM, respectively, are reported here for the first time. Enzyme kinetics revealed that both 3a and 3b were non-competitive inhibitors of α-glucosidase, with Ki values of 2.20 and 2.24 mM, respectively. In short, the presented work identified compounds 3a and 3b as potential α-glucosidase inhibitors with higher inhibitory activity and a different mode of inhibition compared to the standard α-glucosidase inhibitor, acarbose. The integrated approach adopted in this study can be extended as a normalized procedure to rapidly identify active compounds, even from complex extracts, and can readily be adapted for the study of other natural products.

Complementary Chinese Herbal Medicine Therapy Improves Survival in Patients With Pemphigus: A Retrospective Study From a Taiwan-Based Registry.

Pemphigus is a life-threatening and skin-specific inflammatory autoimmune disease, characterized by intraepidermal blistering between the mucous membranes and skin. Chinese herbal medicine (CHM) has been used as an adjunct therapy for treating many diseases, including pemphigus. However, there are still limited studies in effects of CHM treatment in pemphigus, especially in Taiwan. To more comprehensively explore the effect of long-term CHM treatment on the overall mortality of pemphigus patients, we performed a retrospective analysis of 1,037 pemphigus patients identified from the Registry for Catastrophic Illness Patients database in Taiwan. Among them, 229 and 177 patients were defined as CHM users and non-users, respectively. CHM users were young, predominantly female, and had a lesser Charlson comorbidity index (CCI) than non-CHM users. After adjusting for age, sex, prednisolone use, and CCI, CHM users had a lower overall mortality risk than non-CHM users (multivariate model: hazard ratio (HR): 0.422, 95% confidence interval (CI): 0.242–0.735, p = 0.0023). The cumulative incidence of overall survival was significantly higher in CHM users than in non-users (p = 0.0025, log rank test). Association rule mining and network analysis showed that there was one main CHM cluster with Qi–Ju–Di–Huang–Wan (QJDHW), Dan–Shen (DanS; Radix Salviae miltiorrhizae; Salvia miltiorrhiza Bunge), Jia–Wei–Xiao–Yao-–San (JWXYS), Huang–Lian (HL; Rhizoma coptidis; Coptis chinensis Franch.), and Di–Gu–Pi (DGP; Cortex lycii; Lycium barbarum L.), while the second CHM cluster included Jin–Yin–Hua (JYH; Flos lonicerae; Lonicera hypoglauca Miq.) and Lian–Qiao (LQ; Fructus forsythiae; Forsythia suspensa (Thunb.) Vahl). In Taiwan, CHMs used as an adjunctive therapy reduced the overall mortality to approximately 20% among pemphigus patients after a follow-up of more than 6 years. A comprehensive CHM list may be useful in future clinical trials and further scientific investigations to improve the overall survival in these patients.

Evaluation of Antioxidant and α-glucosidase Inhibitory Activities of Codonopsisjavanica (Blume) Hook. f. Thoms’ Root Extract

Evaluation of Antioxidant and α-glucosidase Inhibitory Activities of Codonopsisjavanica (Blume) Hook. f. Thoms’ Root Extract

Kukoamine A Protects against NMDA-Induced Neurotoxicity Accompanied with Down-Regulation of GluN2B-Containing NMDA Receptors and Phosphorylation of PI3K/Akt/GSK-3β Signaling Pathway in Cultured Primary Cortical Neurons.

Kukoamine (KuA) is a spermine alkaloid present in traditional Chinese medicine Cortex Lycii radices, which possesses various pharmacological properties. Our previous studies have demonstrated that KuA exerts neuroprotective effects against H2O2-induced oxidative stress, radiation-induced neuroinflammation, oxidative stress and neuronal apoptosis, as well as neurotoxin-induced Parkinson's disease through apoptosis inhibition and autophagy enhancement. The present study aimed to investigate the neuroprotective effects of KuA against NMDA-induced neuronal injury in cultured primary cortical neurons and explore the underlying mechanism. Incubation with 200μM NMDA for 30min induced excitotoxicity in primary cultured cortical neurons. The results demonstrated that pretreatment with KuA attenuated NMDA induced cell injury, LDH leakage and neuronal apoptosis. KuA also regulated apoptosis-related proteins. Thus, incubation with the alkaloid decreased the ratio of Bax/Bcl-2, and inhibited the release of cytochrome C, the expression of p53 and the cleavage of caspase-3. Moreover, KuA prevented the upregulation of GluN2B-containing NMDA receptors (NMDAR). Additionally, pretreatment with KuA reversed NMDA-induced dephosphorylation of Akt and GSK-3β and the protective effect of KuA on NMDA-induced cytotoxicity was abolished by wortmannin, a PI3K inhibitor. Taken together, these results indicated that KuA exerted neuroprotective effects against NMDA-induced neurotoxicity in cultural primary cortical neurons and caused the down-regulation of GluN2B-containing NMDARs as well as the phosphorylation of proteins belonging to the PI3K/Akt/GSK-3β signaling pathway.

Changes of Anti-tuberculosis Herbs Formula During Past Three Decades in Contrast to Ancient Ones.

To investigate the evolution of herbal medicine in treating tuberculosis (TB) and encourage anti-TB drug discovery and development. In this study, 477 ancient traditional Chinese medicine formulae were collected from the Dictionary of Traditional Chinese Medicine Prescriptions and 172 modern Chinese medicine formulae (from 1986 to 2016) were collected by searching 4 databases: WanFang Data Knowledge Service Platform, China National Knowledge Infrastructure Database (CNKI), China Science and Technology Journal Database (VIP) and Chinese Bio-medical Literature and Retrieval System (SinoMed) in Chinese. We restricted the search to publications in Chinese. Further data analysis was done using the Traditional Chinese Medicine Inheritance Support System version 2 Software. There were 425 herbs in the 477 ancient formulae and 257 herbs in the 172 modern formulae. Half of the top 30 herbs were shared by both modern and ancient prescriptions. They are Radix Ophiopogonis, Astragalus membranaceus, Fritillaria cirrhosa, Dried rehmannia glutinosa, Poria cocos, Angelica sinensis, Prepared rehmannia glutinosa, Platycodon Root, Radix paeoniae alba, Schisandra chinensis, Bighead atractylodes rhizome, Rhizoma anemarrhenae, Cortex lycii radicis and Radix Scutellariae. Only two groups of herbs with a high correlation coefficient were found in both modern and ancient prescriptions, the Dried rehmannia glutinosa with Radix ophiopogonis, and Radix ophiopogonis with Prepared rehmannia glutinosa. There were 9 and 15 core herb combinations in modern and ancient prescriptions, respectively, but no one was found simutaniously in both modern and ancient prescriptions. Although there were wide variations in the herb groups and herb combinations in the formulae, half of the top 30 herbs were found in both modern and ancient prescriptions. The core herb combinations in modern and ancient prescriptions could help us to improve the priscription for treatment of TB.

Exploring Chemical Structures From Cortex Lycii, Based on Manual and Automatic Analysis of the HPLC-Q-TOF-MS Data

Cortex Lycii, the root barks of Lycium barbarum and L. chinense, known as “di gu pi” in traditional Chinese herbal drugs, is an important ingredient of formulations used for treating a variety of diseases. During the last 3 decades, more than 70 chemical entities have been separated and purified from either the aqueous or aqueous ethyl alcohol extracts of Cortex Lycii. In this study, high-performance liquid chromatography together with quadrupole-time-of-flight mass spectrometry (MS) was employed to explore new analog structures from aqueous ethyl alcohol extracts (50%, v/v), which led us to discover 4 new phenolic amides and a new cyclic peptide. The structure-based manual screening method, on the basis of the analysis of the fragmentation pathway of the previously known compounds, was used to make a preliminary analysis of the negative total ion chromatography and negative extract ion spectra. Three ions at m/ z 472.1, 314.1, and 445.2 were assigned to phenolic amides, and by further analysis of their MS/MS data, the structure of 1, corresponding to one of them ( m/ z 314.1), was illustrated as an analog of the known compound KN1. A parent ion at m/ z 856.1 was assigned to a cyclic peptide analog (2) in the manual analysis procedure. Furthermore, the MS/MS data were profiled on the Global Natural Product Social Molecular Networking (GNPS, https://gnps.ucsd.edu/ProteoSAFe/static/gnps-splash.jsp ) workflow to weave a visualization molecular network. Three more new analog ions ( m/ z 604.3 [3], 597.3 [4], and 611.3 [5]) were found in the aggregation of KN5 and KN7, and their structures were all determined by comparisons with known compounds. This manual and networking automatic screening method may provide a sensitive and efficient procedure to facilitate the mining of novel trace components.

Variation of Kukoamine A (KuA) and B (KuB) contents and related meteorological factors for Cortex Lycii radicis of different areas

Kukoamines are polyamine alkaloids present in Cortex Lycii (LyC), which is the root bark of Lycium chinense Mill. or L. barbarum L. Environmental conditions and geographical distribution influence the biosynthesis and accumulation of Kukoamines in Lycium species, thus directly affecting the quality of LyC. To identify the factors that influence Kukoamine A (KuA) and Kukoamine B (KuB) accumulation, the KuA and KuB contents of L. chinense and L. barbarum LyC collected from different areas or potted L. barbarum LyC with soil collected from different areas were measured, and the correlation of Kukoamine contents with meteorological factors and soil constituents were analyzed. In both L. barbarum and L. chinense, the KuA and KuB contents of LyC planted in Zhongning were significantly higher than those of LyC planted in other areas. Three L. barbarum species planted in soil collected from different areas presented significant difference in the KuA and KuB content of LyC. The contents of both KuA and KuB showed negative correlation with annual precipitation, mean temperature, and mean humidity, while positively correlated with soil pH, altitude, mean diurnal temperature difference, and annual sunshine hours, but there was no significant correlation with any soil compositions. It might be illustrated that soil pH and meteorological factors are important aspects affecting the quality of LyC.

The Effect of Cortex Lycii on Rattus norvegicus’ Blood Glucose Level Using a High Glucose Diet

One of the primary problems in the United States is diabetes. Cortex Lycii is an herb from Asia mostly used in traditional Chinese medicine. Although its main purpose is not for lowering blood glucose levels, there are studies on Cortex Lycii with other substances which have proven it can lower glucose level in type 2 diabetes rat. Unlike other experiments, this experiment only used Cortex Lycii as a single unit to see if there was any effect on blood glucose level. Also an observation was done on if Cortex Lycii could reduce blood glucose level after ingesting a high glucose diet. Rattus norvegicus was used in this project and in order for the subject to consume Cortex Lycii, the herb was boiled and the liquid was given for consumption. In order to increase the rats’ glucose levels, corn syrup and white sugar were added to the mixture. The data showed significant decrease of blood glucose when Cortex Lycii liquid was ingested. This research has shown that Cortex Lycii can be a potential treatment for hyperglycemia or diabetes. With further research, there can be an alternative treatment rather than injecting external hormones (Insulin).

Neuroprotective effect of trans-N-caffeoyltyramine from Lycium chinense against H2O2 induced cytotoxicity in PC12 cells by attenuating oxidative stress

Natural products play a critical role in the promotion of good health as regards the prevention and management of oxidative stress related and neurodegenerative disorders. Oxidative stress has been implicated in several apoptotic pathways associated with cell damages in neuronal disorders. The aim of this study was to investigate the antioxidant effect of trans-N-caffeoyltyramine (TNC) isolated from Cortex lycii against hydrogen peroxide (H2O2) induced cell damages in PC12 cells as well as its mechanism of action. The results obtained indicated that pretreatment with TNC before the exposure of cells to H2O2 toxicity lead to a significant increase in the cell viability and the antioxidant enzyme activities catalase (CAT), superoxide dismutase (SOD), glutathione (GSH) and reduced the level of malondialdehyde (MDA). Furthermore, TNC attenuated the influx of Ca2+, ROS formation and restored the impaired mitochondria membrane potential (MMP). Thus TNC may be used as an alternative therapy for the prevention and treatment of neuronal disorders elicited by oxidative stress.

Kukoamine A inhibits human glioblastoma cell growth and migration through apoptosis induction and epithelial-mesenchymal transition attenuation.

Cortex lycii radicis is the dried root bark of Lycium chinense, a traditional Chinese herb used in multiple ailments. The crude extract of Cortex lycii radicis has growth inhibition effect on GBM cells. Kukoamine A (KuA) is a spermine alkaloid derived from it. KuA possesses antioxidant, anti-inflammatory activities, but its anticancer activity is unknown. In this study, the growth and migration inhibition effect of KuA on human GBM cells and the possible mechanism of its activity were investigated. After KuA treatment, proliferation and colony formation of GBM cells were decreased significantly; apoptotic cells were increased; the cell cycle was arrested G0/G1 phase; the migration and invasion were decreased, the growth of tumors initiated from GBM cells was inhibited significantly; the expressions of 5-Lipoxygenase (5-LOX) were decreased, apoptotic proteins, Bax and caspase-3 were increased, and antiapoptotic protein Bcl-2 was decreased significantly; The expressions of CCAAT/enhancer binding protein β (C/EBPβ), N-cadherin, vimentin, twist and snail+slug were decreased significantly, while the expression of E-cadherin was increased significantly in KuA treated GBM cells and tumor tissues. KuA inhibited human glioblastoma cell growth and migration in vitro and in vivo through apoptosis induction and epithelial-mesenchymal transition attenuation by downregulating expressions of 5-LOX and C/EBPβ.

Cortex Lycii Radicis Extracts Protect Pancreatic Beta Cells Under High Glucose Conditions.

The normal function of pancreatic beta cells is vital to the control of blood glucose. Earlier research suggests that the traditional Chinese medicine Cortex Lycii Radicis may help protect pancreatic beta cells and improve insulin sensitivity. However, the specific effects and molecular mechanism of this herb have not been described. Thus, we investigated the role of Cortex Lycii Radicis in regulating the proliferation, apoptosis, and autophagy of INS-1 pancreatic beta cells. Our study revealed that Cortex Lycii Radicis extracts could promote INS-1 cell proliferation and inhibit cell apoptosis under high glucose conditions. We also evaluated the formation of autophagosomes and found that GFP-LC3 fusion protein was translocated to the autophagosome membrane. Autophagosomes increased in the group treated with Cortex Lycii Radicis compared with the no treatment control group, indicating that these extracts could promote the activation of autophagy in INS-1 cells. Our findings suggest a significant association of the Cortex Lycii Radicis extracts treatment with apoptosis and autophagy, which protects the function of pancreatic beta cells, providing evidence for the development of a new drug for diabetes treatment.

Binding mechanism of trans-N-caffeoyltyramine and human serum albumin: Investigation by multi-spectroscopy and docking simulation

trans-N-Caffeoyltyramine (TNC), which was isolated from the Cortex Lycii in our laboratory, is a phenolic amide compound with multiple pharmacological activities. The interaction between TNC and human serum albumin (HSA) was studied by Nuclear magnetic resonance (NMR) relaxation experiment, fluorescence spectroscopy, and docking simulation. NMR methodology is based on the analysis of selective and non-selective spin-lattice relaxation rate enhancements of TNC protons in the presence of the HSA. Result indicated that the interaction occurred between HSA and TNC, and changed the proton magnetic environment of TNC. Fluorescence spectroscopy confirmed that TNC displayed a strong capability to quench the fluorescence of HSA, and the acting forces for binding were hydrogen bonds and van der Waals forces. Furthermore, the circular dichroism, synchronous, and three-dimensional fluorescence spectra, which were employed to determine the conformation of protein, revealed that binding of TNC with HSA could induce conformational changes in HSA. In addition, the molecular modeling results exhibited that TNC mainly bonded to site I in sub-domain IIA of HSA.

Anti-oxidative, anti-secretory and anti-inflammatory activities of the extract from the root bark of Lycium chinense (Cortex Lycii) against gastric ulcer in mice.

The evaluation of the antioxidant, anti-secretory and anti-inflammatory potentials of the ethyl acetate fraction (ELC) from the root bark of Lycium chinense against ethanol-induced gastric ulcer in mice and the possible mechanisms underlying this action was performed. The results indicated that oral administration of ELC (50, 100, 200 and 400mg/kg) before ethanol-induced ulcer increased the gastric mucus content, restored the superoxide dismutase and glutathione levels, reduced malondialdehyde levels and inhibited the activity of myeloperoxidase. Furthermore, ELC displayed its anti-secretory activity by decreasing the gastric juice and increased the gastric pH and reduced pro-inflammatory markers and caspase-3 tissue levels. These results suggest that L. chinense displays gastroprotective properties as a result of its antioxidant, anti-inflammatory, anti-secretory and anti-apoptotic effects.