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ETHNOPHARMACOLOGICAL RELEVANCE: Geniposide (GE) is ubiquitous in nearly 40 species of plants, among which Gardenia jasminoides J. Ellis has the highest content, and has been used ethnopharmacologically to treat chronic inflammatory diseases. As a traditional Chinese medicine, Gardenia jasminoides J. Ellis has a long history of usage in detumescence and sedation, liver protection and cholestasis, hypotension and hemostasis. It is commonly used in the treatment of diabetes, hypertension, jaundice hepatitis, sprain and contusion. As a type of iridoid glycosides extracted from Gardenia jasminoides J. Ellis, GE has many pharmacological effects, such as anti-inflammatory, anti-angiogenesic, anti-oxidative, etc. AIM OF THE REVIEW: In this article, we reviewed the sources, traditional usage, pharmacokinetics, toxicity and therapeutic effect of GE on chronic inflammatory diseases, and discussed its potential regulatory mechanisms and clinical application. RESULTS: GE is a common iridoid glycoside in medicinal plants, which has strong activity in the treatment of chronic inflammatory diseases. A large number of in vivo and in vitro experiments confirmed that GE has certain therapeutic value for a variety of chronic inflammation disease. Its mechanism of function is mainly based on its anti-inflammatory, anti-oxidant, neuroprotective properties, as well as regulation of apoptotsis. GE plays a role in the treatment of chronic inflammatory diseases by regulating cell proliferation and apoptosis, realizing the dynamic balance of pro/anti-inflammatory factors, improving the state of oxidative stress, and restoring abnormally expressed inflammation-related pathways. CONCLUSION: According to its extensive pharmacological effects, GE is a promising drug for the treatment of chronic inflammatory diseases.
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Inflammation/drug therapy , Iridoids/therapeutic use , Animals , Chronic Disease , Humans , Iridoids/chemistry , Phytotherapy , Plants/chemistryABSTRACT
OBJECTIVETo study the neurological manifestations of patients with coronavirus disease 2019 (COVID-19). DESIGNRetrospective case series SETTINGThree designated COVID-19 care hospitals of the Union Hospital of Huazhong University of Science and Technology in Wuhan, China. PARTICIPANTSTwo hundred fourteen hospitalized patients with laboratory confirmed diagnosis of severe acute respiratory syndrome from coronavirus 2 (SARS-CoV-2) infection. Data were collected from 16 January 2020 to 19 February 2020. MAIN OUTCOME MEASURESClinical data were extracted from electronic medical records and reviewed by a trained team of physicians. Neurological symptoms fall into three categories: central nervous system (CNS) symptoms or diseases (headache, dizziness, impaired consciousness, ataxia, acute cerebrovascular disease, and epilepsy), peripheral nervous system (PNS) symptoms (hypogeusia, hyposmia, hypopsia, and neuralgia), and skeletal muscular symptoms. Data of all neurological symptoms were checked by two trained neurologists. RESULTSOf 214 patients studied, 88 (41.1%) were severe and 126 (58.9%) were non-severe patients. Compared with non-severe patients, severe patients were older (58.7 {+/-} 15.0 years vs 48.9 {+/-} 14.7 years), had more underlying disorders (42 [47.7%] vs 41 [32.5%]), especially hypertension (32 [36.4%] vs 19 [15.1%]), and showed less typical symptoms such as fever (40 [45.5%] vs 92 [73%]) and cough (30 [34.1%] vs 77 [61.1%]). Seventy-eight (36.4%) patients had neurologic manifestations. More severe patients were likely to have neurologic symptoms (40 [45.5%] vs 38 [30.2%]), such as acute cerebrovascular diseases (5 [5.7%] vs 1 [0.8%]), impaired consciousness (13 [14.8%] vs 3 [2.4%]) and skeletal muscle injury (17 [19.3%] vs 6 [4.8%]). CONCLUSIONCompared with non-severe patients with COVID-19, severe patients commonly had neurologic symptoms manifested as acute cerebrovascular diseases, consciousness impairment and skeletal muscle symptoms.
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Objective To compare the dissolution curves of metronidazole tablets from 38 national manufactures and original drugs of Britain in four dissolution mediums,and provide the reference for the quality and clinical effect consistency evaluation of metronidazole tablets.Methods Paddle method was adopted at 50 r · min-1 in four dissolution mediums with the volume of 900 mL.The dissolution profiles were determined by ultraviolet spectrophotometry.The cumulative dissolution percentages were calculated and the dissolution curves were drawn.Similarity factor (f2)was used for comparing of the differences between dissolution curves.Results The dissolution profiles of 4 manufactures in pH 1.2 and 9 manufactures in pH 4.5 were similar (f2 ≥ 50)to that of original drugs,only 1 and 3 were similar to original drugs in water and pH 6.8,respectively.There are no companies whose dissolution curve were similar to that of original drugs in 4 dissolution mediums.Conclusion Great difference exists between domestic manufactures and pharmaceutical enterprises of origin in dissolution behaviors of metronidazole tablets.In order to ensure the consistency between the metronidazole tablets generics and original drugs of Britain in quality and clinical effect.It is advisable for the relevant companies to improve their product quality by improving the formulation and preparation.
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Objective To investigate the effect of Exendin-4 (Ex-4) on ischemia/reperfusion (I/R) injury-induced apoptosis in primary rat cortical neurons and the possible underlying mechanisms.Methods Rat cortical neurons were cultured in vitro,identified by NES-immunohistological staining and immunofluorescence staining,and randomly divided into the following groups: control group,I/R group and Ex-4 group.RT-PCR was performed to establish the existence of active glucagon-like peptide-1 receptor (GLP-1R).ELISA was used to measure the neuronal cytoplasmic cAMP level. MTT was used to detect viability. Fluorescent DNA binding dye Hoechest 33258 was used to reveal apoptosis. C/EBP-homologous protein (CHOP) and growth arrest and DNA-damage-inducible gene 34 (GADD34) mRNAs were detected by real-time PCR. Results The apoptosis rate induced by ischemia 6 h/reperfusion 12 h was 77.0% ±5.3% and was decreased to 27.0% ± 3.5% after Ex-4 ( 0. 4 μg/ml ) treating ( t = 19. 462,P ＜ 0. 01 ).Levels of CHOP and GADD34 mRNA in cortical neurons increased since 4 h and peaked at 12 h after reperfusion. Ex-4 group showed a sharp elevation of levels of CHOP and GADD34 mRNA,peaking at 8 h reperfusion,and then tended to decrease.Conclusions Ex-4 has protective effect against rat cortical neurons injury induced by ischemia/reperfusion. The protective effect may be related to inhibition of ESR-related neuron apoptosis via regulation of unfolded protein response.
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Objective To observe the effects of passive movement on the functional outcome after occlusion of the middle artery in the brain and reperfusion, and to explore the molecular mechanisms involved. Methods Cerebral infarction models were established in rats using left middle cerebral artery occlusion ( MCAO). The survivors were randomly divided into a passive movement group and a natural recovery group. There was also a sham-operated group and a normal group. Passive movement treatment (twice a day, twenty min per time) was started at different times after reperfusion. The expression of brain-derived neurotrophic factor (BDNF) and B cell lymphoma/leukemia-2 gene (Bcl-2) were determined using real-time PCRs. Results Expression of BDNF and Bcl-2 was detected a-round the infarction area in both groups. The expression of BDNF and Bcl-2 was highest in the sub-groups where passive movement was begun 24 or 48 h after the operation. Conclusions The expression of BDNF and Bcl-2 in the brain peaks when daily, moderate intensity passive movement is administered beginning 24 to 48 h after reperfusion. Passive movement might have a protective and rehabilitative effect after cerebral infarction.
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Objective To study the effect of electroacupuncture (EA) combined with transcranial magnetic stimulation (TMS) on the expression of the B-cell lymphoma/leukemia-2 gene (Bcl-2) and brain derived neurotrophic factor (BDNF) after cerebral infarction. Methods One hundred Sprague-Dawley rats were randomly and equally divided into a normal group, a sham-operated control group, a model group and an EA plus TMS group. A cerebral infarction model was established in the latter two groups using left middle cerebral artery occlusion (MCAO). Five-member subgroups of the EA plus TMS group were then treated at 6, 12, 24,48 and 72 hours after reperfusion. Sham EA plus TMS was given to similar sub-groups from the other groups at the same time points. The expression of Bcl-2 mRNA and BDNF mRNA were measured using a RT-PCR at the 14th day. Results Positive expression of Bcl-2 mRNA and BDNF mRNA was detected around the infarction in all groups. The average expression of both was significantly higher in the EA plus TMS group than in the model group. Bcl-2 mRNA peaked when the therapy was administered at 24 hours and BDNF mRNA at 48 hours.Conclusions The expression of Bcl-2 mRNA and BDNF mRNA is maximized when EA plus TMS is administered 24-48 hours after cerebral infarction. EA plus TMS does have protective and rehabilitative effects on rats after cerebral infarction.
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Objective To study the effect of transcranial magnetic stimulation (TMS) on the rehabilitation of rats with cerebral infarction. Methods One hundred Sprague-Dawley rats were randomly divided into a normal group, a sham-operated control group, a model group and a TMS group with 25 rats in each group. A cerebral infarction model was established in the latter two groups by left middle cerebral artery occlusion (MCAO). TMS was started at either 12 or 24 hours after reperfusion, and sham-TMS was given to the first two groups at the same time points. The expression of Bcl-2 mRNA and BDNF mRNA were measured by RT-PCR after 14 days. Results Bcl-2 mRNA and BDNF mRNA were detected in all groups. The expression of Bcl-2 mRNA in the TMS-12 h group, and that of BDNF mRNA in the TMS-24 h group were significantly higher than in the other groups. Conclusions The expression of Bcl-2 mRNA and BDNF mRNA in the brains of rats after cerebral infarction peak when TMS is administered 12 h and 24 h after reperfusion, respectively. TMS might have protective and rehabilitative effects on rats after cere-bral infarct.
