Arteriosclerosis ; drug therapy ; Coumaric Acids ; therapeutic use ; Drugs, Chinese Herbal ; therapeutic use ; Flavonoids ; Humans ; Phenols ; therapeutic use ; Phytotherapy ; Polymers ; therapeutic use ; Polyphenols ; Pyrazines ; therapeutic use

Research has demonstrated that many chemical constituents dominated by piperidine alkaloids and flavonoids, such as lobelanidine, lobeline, and lobelanine, have been obtained from Lobelia chinensis Lour. Experimental studies and clinical applications have also indicated that L. chinensis possesses a number of pharmacological activities (e.g., diuretic, choleretic, breathing excitement, anti-venom, anti-bacterial, and anticancer). This paper focuses on the properties, chemical constituents, and anticancer activity of L. chinensis to clarify the connection among them, and identify the active anticancer compounds. This work serves as the foundation for further research and development of L. chinensis.
Alkaloids ; pharmacology ; therapeutic use ; Animals ; Antineoplastic Agents, Phytogenic ; pharmacology ; therapeutic use ; Flavonoids ; pharmacology ; therapeutic use ; Humans ; Lobelia ; chemistry ; Neoplasms ; drug therapy ; Phytotherapy ; Plant Extracts ; pharmacology ; therapeutic use

OBJECTIVETo observe the protective effect of baicalin on mouse with Parkinson's disease induced by 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP).

METHODSThe mouse model of Parkinson's disease was established by intraperitoneal injection of MPTP at the daily dose of 30 mg/kg for 3 days to the aged (ten months old) C57BL mouse. And to the model mice in the tested group, baicalin (100 mg/kg) was given via gastric perfusion per day for 15 days. The motor function of limbs in mice was tested through hanging and swimming tests; the dopamine content of striatum was measured by HPLC; and the contents of malondialdehyde (MDA), glutathione (GSH) and glutathione peroxidase (GSH-Px) in the brain tissue were measured by spectrophotography. Besides, the freezing section of mouse brain was made through immunohistochemical stain with tyrosine hydroxylase (TH) to determine the condition of dopaminergic neuron damage in mesencephalon.

RESULTS(1) The decreased score in the hanging test and swimming test, the reduced DA contents of striatum and lessening of TH positive neurons in substantial nigra illustrated the model of Parkinson's disease was successfully established. (2) Medication of baicalin could prevent the loss of TH positive neurons in substantial nigra and the decrease of dopamine content of striatum in Parkinson mouse, and significantly raise the content of GSH in the brain, but MPTP induced motor dysfunction in model mouse was not significantly improved by a short-time medication.

CONCLUSIONThe preventive medication of baicalin shows a protective effect on C57 BL mouse with Parkinson's disease induced by MPTP.

Animals ; Antioxidants ; therapeutic use ; Drugs, Chinese Herbal ; therapeutic use ; Flavonoids ; therapeutic use ; Male ; Mice ; Mice, Inbred C57BL ; Parkinsonian Disorders ; drug therapy ; Phytotherapy ; Random Allocation

Hippophae rhamnoides is one of the most representative economy crops for its wide uses of biological diversity and abundance of resource. As the key healthy food development and ecology protection, H. rhamnoides has been developed widely. Meanwhile, the development of H. rhamnoides has obtained great achievements. Nowadays, H. rhamnoides is still a necessary economy crop, while it has great influence on ecology protection. This paper discussed the phytochemistry, pharmacology, clinical application and product development, and propounded some suggestions for future research and economy development to get comprehensive benefit of H. rhamnoides and to serve for well-off society.
Biomedical Research ; methods ; trends ; Drugs, Chinese Herbal ; chemistry ; therapeutic use ; Flavonoids ; chemistry ; therapeutic use ; Hippophae ; chemistry ; Humans ; Molecular Structure ; Phytotherapy ; methods ; trends ; Polyphenols ; chemistry ; therapeutic use

The present study optimized the extraction of flavonoids from Lonicera rupicola Hook. f. et Thoms(LRH) and explored its pharmacological effects, such as resisting inflammation, relieving pain, enhancing immunity, and inhibiting pyroptosis, aiming to provide data support and scientific basis for the development and utilization of LRH. Response surface methodology(RSM) was applied to optimize the extraction of flavonoids from LRH based on the results of single-factor experiments. Anti-inflammatory and analgesic effects of LRH flavonoids were evaluated via inflammation and pain models in mice, such as xylene-induced ear swelling, carrageenan-induced footpad swelling, writhing caused by acetic acid, and paw licking. The effect of LRH flavonoids on the carbon clearance index of monocytes and serum immunoglobulin A(IgA) and IgM levels was analyzed on the immunosuppression model induced by cyclophosphamide in mice. The anti-oxidative effect in vivo of LRH flavonoids on liver superoxide dismutase(SOD), catalase(CAT), and malondialdehyde(MDA) levels was determined based on the chronic/subacute aging model in mice induced by D-galactose. The levels of cysteinyl aspartate specific proteinase-1(caspase-1), interleukin-1β(IL-1β), and IL-18 in the supernatant of J774 A.1 mononuclear phagocytes were detected to evaluate the effect of LRH flavonoids on the pyroptosis of mononuclear phagocytes in mice induced by the combination of lipopolysaccharide(LPS) and adenosine triphosphate(ATP). Meanwhile, the effect of LRH flavonoids on the cAMP-PKA signaling pathway was also explored. The optimum conditions for the extraction of LRH flavonoids are listed below: extraction temperature of 65 ℃, the ethanol concentration of 50%, extraction time of 60 min, a material-liquid ratio at 1∶25, and the yield of LRH flavonoids of 0.553%. RSM determined the multiple quadratic regression equation model of response value and variables as follows: the yield of LRH flavonoids=0.61-0.48A+0.1B+0.029C-0.014D+0.32AB+0.04AC-0.012AD-0.02BC+0.037BD-0.031CD-0.058A~2-0.068B~2-0.069C~2-0.057D~2. LRH flavonoids could effectively inhibit ear swelling and footpad swelling, reduced acetic acid-induced writhing, and delayed the paw licking response time in mice. Additionally, LRH flavonoids could improve the carbon clearance index in immunosuppressed mice, potentiate the activities of SOD and CAT and reduce MDA levels in the liver of aging mice induced by D-galactose, and effectively inhibit macrophage pyroptosis by decreasing the levels of caspase-1, IL-1β, and IL-18. The results reveal that LRH flavonoids possess excellent pharmacological activities such as resisting inflammation and oxidation, relieving pain, and enhancing immunity. They can inhibit pyroptosis by enhancing the cAMP-PKA signaling pathway. The results of this study can underpin the pharmacological research, development, and utilization of LRH.
Analgesics/therapeutic use* ; Animals ; Edema/drug therapy* ; Flavonoids/therapeutic use* ; Inflammation/drug therapy* ; Lonicera ; Mice ; Mice, Inbred ICR ; Pain/drug therapy* ; Plant Extracts/therapeutic use* ; Pyroptosis

Flavonoids ; pharmacology ; therapeutic use ; Humans ; Osteogenesis ; drug effects ; Osteoporosis ; drug therapy

OBJECTIVEThe National Institutes of Health (NIH) category IIIa chronic prostatitis syndromes (non bacterial chronic prostatitis) were common disorders but with few effective therapies. Alpha-blockers and bioflavonoids had recently been reported in randomized controlled trials to improve the symptom of these disorders in a significant proportion of men. The aim of this study was to confirm these findings in a prospective randomized, placebo-controlled trial.

METHODSForty-five men with category IIIa chronic non bacterial protatitis were randomized into three groups as follows: (1) placebo; (2) phenoxybenzamine-hydrochloride:10 mg two times a day for one month; (3) flavoxate HCI-neptumus: 200 mg three times a day for one month. The NIH chronic prostatitis symptom score was used to grade symptoms at the beginning and conclusion of the study.

RESULTSAll the patients in three groups completed the study except three dropout patients in placebo group because of sever symptoms. The three groups were similar in age, duration of symptoms and initial symptom score. Patients taking placebo had a mean improvement in NIH-CPSI from 21.85 to 19.55 (not significant), while the phenoxybenzamine-hydrochloride group had a mean improvement from 21.95 to 13.75 (P < 0.01), and those taking flavoxate HCI-neptumus had a mean improvement from 21.75 to 16.95 (P < 0.05). The decrease in NIH-CPSI was associated with significant improvement in patients' clinical manifestations.

CONCLUSIONTherapy with alpha-blockers was well tolerated with significant symptomatic improvement in most men having chronic non-bacterial chronic protatitis while the bioflavonoids group had no significant improvement. Mechanism of both medicines needs further study.

Adrenergic alpha-Antagonists ; administration & dosage ; therapeutic use ; Adult ; Chronic Disease ; Flavonoids ; administration & dosage ; therapeutic use ; Flavoxate ; therapeutic use ; Humans ; Male ; Parasympatholytics ; therapeutic use ; Prospective Studies ; Prostatitis ; drug therapy ; Treatment Outcome

The antidepressant effects of the flavonoid-rich fraction of Monodora tenuifolia seed extract were examined by assessing the extent of attenuation of behavioural alterations and oxidative damage in the rats that were stressed by forced swim test. Compared with the model control group, the altered behavioural parameters were attenuated significantly (P < 0.05) in the group treated with the flavonoid-rich fraction (100 and 200 mg·kg(-1)), comparable to the group treated with the standard drug, fluoxetine (10 mg·kg(-1)). The flavonoid-rich fraction and fluoxetine improved significantly (P < 0.05) the activities of the antioxidant enzymes such as superoxide dismutase and catalase as well as other biochemical parameters such as reduced glutathione, protein, and nitrite in the brain of the stressed rats. These results suggested that the flavonoid-rich fraction of Monodora tenuifolia seed extract exerted the antidepressant-like effects which could be useful in the management of stress induced disease.
Animals ; Annonaceae ; chemistry ; Antidepressive Agents ; therapeutic use ; Antioxidants ; metabolism ; Behavior, Animal ; drug effects ; Brain ; metabolism ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Flavonoids ; therapeutic use ; Fluoxetine ; therapeutic use ; Male ; Oxidative Stress ; drug effects ; Rats ; Rats, Wistar ; Seeds ; chemistry ; Swimming

OBJECTIVETo reproduce an experimental model of alcoholic liver disease in rats and to investigate the preventive and treatment effects of tea polyphenols on alcoholic liver disease.

METHODS68 male Sprague-Dawley rats were randomly divided into 3 groups: alcohol group (gastrically infused with 56% of ethanol once a day with a dose of 7 g/kg body weight for 4, 12 and 24 weeks), tea polyphenols group (gastric infusion with alcohol same as in the alcohol group and with tea polyphenols at 0.25 g/kg bw) and control group (gastric infusion with normal saline). At the end of 4, 12 and 24 weeks, blood samples were collected and then the rats were sacrificed. Liver samples were obtained for routine histological examination and the degree of hepatic steatosis and alcoholic hepatitis were examined. Blood specimens were used for evaluation of alanine transaminase (ALT) and aspartate aminotransferase (AST).

RESULTS(1) The levels of the two transaminases were elevated with the increase of the duration of ethanol feeding and the difference is significant. TP significantly mitigated the increase of ALT and AST activities induced by the alcohol. (2) Histological changes of the liver injury indicated that piecemeal or focal necrosis of hepatocytes was present in the centrilobular area. As fibrosis advanced, broader septa were formed with central-central and centra-portal bridging necrosis. In the TP infusion group, the severity of the pathological changes was significantly milder.

CONCLUSIONThe results of this study revealed that TP mitigated the development of alcoholic liver disease, and TP may be a potential drug for treatment of alcoholic liver disease.

Animals ; Flavonoids ; therapeutic use ; Liver Diseases, Alcoholic ; drug therapy ; prevention & control ; Male ; Phenols ; therapeutic use ; Phytotherapy ; Polyphenols ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Tea ; chemistry

OBJECTIVETo study the therapeutic efficacy of baicalin and its effect on apoptosis of inflammatory cells in spinal cords in Wistar rats with autoimmune encephalomyelitis (EAE).

METHODSForty-four rats were randomly divided into four groups: normal control group (control, n=10), EAE group (n=12), and two intervention groups with dexamethasone (DXM) or baicalin. Seven days after immunization, the two intervention groups were injected intraperitoneally with DXM (1 mg/kg) and baicalin (200 mg/kg) for 1 week, respectively. The spinal cords were removed 14 days after immunization, and stained with hematoxylin and eosin. MBP expression in spinal cords was detected by immunohistochemistry. The apoptosis of inflammatory cells in spinal cords was detected by TUNEL.

RESULTSThe weight gain rate in the untreated EAE and the DXM or baicalin intervention groups were significantly lower than that in the control group (P<0.05). The weight gain rate in the baicalin intervention group was significantly higher than that in the untreated EAE and the DXM intervention groups (P<0.05). The scores of neurological function in the two intervention groups were significantly higher than that in the untreated EAE group (P<0.05). DXM or baicalin treatment significantly increased the MBP expression compared with the untreated EAE group (P<0.05). The apoptosis of inflammatory cells increased more in the DXM and the baicalin intervention groups compared with the untreated EAE groups (P<0.05).

CONCLUSIONSBaicalin has protective effects against EAE in rats. It can promote the apoptosis of inflammatory cells in spinal cords.

Animals ; Apoptosis ; drug effects ; Dexamethasone ; therapeutic use ; Encephalomyelitis, Autoimmune, Experimental ; drug therapy ; pathology ; Female ; Flavonoids ; pharmacology ; therapeutic use ; In Situ Nick-End Labeling ; Rats ; Rats, Wistar