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

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

Progresses in the studies on chemical constituents and bioactivities of total flavonoids of Astragalus (TFA) were systemically reviewed in this article. The results of studies on their bioactivities show that TFA has antioxidant and antitumor activities, and strengthen the immune system. Further biological studies on the species in total flavonoids of Astragalus are needed for better medicinal utilization.
Animals ; Antineoplastic Agents, Phytogenic ; pharmacology ; therapeutic use ; Astragalus Plant ; chemistry ; Drug Therapy ; Drugs, Chinese Herbal ; pharmacology ; Flavonoids ; pharmacology ; therapeutic use ; Humans

OBJECTIVETo observe the effect of Tiangou Jiangya capsule (TJC) on blood pressure in renovascular hypertension rats and explore its possible mechanism.

METHODSeventy-two Wistar rats were randomly divided into normal control group, model group, captopril group, TJC small, medium and high dose groups. Non-invasive blood pressure measurement was used to detect the arterial blood pressure of rat tails. PRA, Ang II , ALD, 6-Keto-PGF1alpha, ET and TXB2 content in blood was measured by radioimmunoassay. NO content in blood was determined by method of nitrate reductase.

RESULTThe systolic, diastolic and mean pressure significantly increased, serum PRA, Ang II , ALD decreased, ET levels significantly increased in model group rats. TJC significantly reduced blood pressure, improved the plasma renin activity, decreased ET levels and increased NO content of model rats.

CONCLUSIONTJC can reduce blood pressure of renovascular hypertention rats, and the mechanism may be related to its regulating lower blood pressure regulation of the secretion of RAAS system and improving vascular endothelial function.

Angiotensin II ; blood ; Animals ; Antihypertensive Agents ; administration & dosage ; pharmacology ; therapeutic use ; Benzyl Alcohols ; pharmacology ; therapeutic use ; Blood Pressure ; drug effects ; Drugs, Chinese Herbal ; administration & dosage ; pharmacology ; therapeutic use ; Flavonoids ; pharmacology ; therapeutic use ; Furans ; pharmacology ; therapeutic use ; Glucosides ; pharmacology ; therapeutic use ; Hypertension, Renovascular ; blood ; drug therapy ; Lignans ; pharmacology ; therapeutic use ; Rats ; Rats, Wistar ; Renin ; blood ; Renin-Angiotensin System ; drug effects

Thyroid carcinogenesis is accompanied by loss of thyroid-specific functions and refractory to radioiodine and thyroid stimulating hormone (TSH) suppression therapy. Redifferentiating agents have been shown to inhibit tumor growth and improve the response to conventional therapy. Polyphenol phytochemicals (PPs) in fruits and vegetables have been reported to inhibit cancer initiation, promotion, progression and induce redifferentiation in selected types. In this study we examined PPs induce redifferentiation in thyroid cancer cell lines. We investigated the effects of genistein, resveratrol, quercetin, kaempferol, and resorcinol on the F9 embryonal carcinoma cell differentiation model. The thyroid cancer cell lines, TPC-1, FTC-133, NPA, FRO, and ARO, displayed growth inhibition in response to genistein, resveratrol, quercetin. We further demonstrated that genistein decreased the dedifferention marker CD97 in NPA cells and resveratrol decreased CD97 in FTC-133, NPA, FRO cells and quercetin decreased CD97 in all cell lines. We observed increased expression of differentiation marker NIS in FTC-133 cells in response to genistein, and resveratrol but no change in NPA, FRO, ARO cells. Quercetin increased or induced NIS in FTC-133, NPA, FRO cells. These findings suggest that PPs may provide a useful therapeutic intervention in thyroid cancer redifferentiation therapy.
Antigens, CD/metabolism ; Antineoplastic Agents/*pharmacology/therapeutic use ; Carcinoma, Embryonal/*drug therapy/metabolism ; Cell Differentiation/*drug effects ; Cell Line, Tumor ; Cell Proliferation/*drug effects ; Flavonoids/*pharmacology/therapeutic use ; Gene Expression Regulation, Neoplastic ; Genistein/pharmacology/therapeutic use ; Humans ; Kaempferols/pharmacology/therapeutic use ; Models, Biological ; Phenols/*pharmacology/therapeutic use ; Quercetin/pharmacology/therapeutic use ; Resorcinols/pharmacology/therapeutic use ; Stilbenes/pharmacology/therapeutic use ; Symporters/metabolism ; Thyroid Neoplasms/*drug therapy/metabolism

Flavanoids are important phytochemistry compositions in foods and traditional Chinese medicines (TCM) and are mainly oxidized by CYP1A family in vivo. Some methoxyflavones could also be metabolized through demethylation. Usually, flavanoids own one or more phenolic hydroxyl group in their molecular structures, which facilitate conjugation with glucuronic acid and sulphuric acid, forming metabolites with good water-solubility to excrete. Natural flavanoids mainly exist in glycoside, and after oral ,they would be easily metabolized to aglycone by hydratase in gut microflora and then absorbed into blood. Besides, many flavanoids have strong inhibitory actions on Cytochrome P450 enzymes, which are significant mechanisms in cancer precaution and tumor inhibition. In this paper, we reviewed lots of articles and summarized metabolism characteristics of flavanoids and metabolism interaction with Cytochrome P450 enzymes.
Animals ; Cytochrome P-450 Enzyme Inhibitors ; Cytochrome P-450 Enzyme System ; metabolism ; Drug Therapy ; Flavonoids ; metabolism ; pharmacology ; therapeutic use ; Humans

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

Animals ; Antineoplastic Agents ; pharmacology ; therapeutic use ; Cell Cycle ; drug effects ; physiology ; Cyclin-Dependent Kinases ; antagonists & inhibitors ; metabolism ; Cyclins ; metabolism ; Flavonoids ; pharmacology ; therapeutic use ; Humans ; Neoplasms ; drug therapy ; metabolism ; pathology ; Piperidines ; pharmacology ; therapeutic use ; Purines ; pharmacology ; therapeutic use ; Staurosporine ; analogs & derivatives ; pharmacology ; therapeutic use

OBJECTIVETo investigate the effects of Tiangou Jiangya capsule on blood pressure of spontaneous hypertensive rats.

METHODThe 13-14 week SPF rats were selected and randomly divided into model groups, the low, middle, high dose of Tiangou Jiangya capsule groups, positive control group administrated with captopril. Drugs were intragastric administrated once per day, lasting four weeks. The blood pressure, heart rate, heart ventricle indexes, urinary volume and the level of PRA,angiotensing II (Ang II), aldosterone (ALD) of rats were observed.

RESULTThe low, middle, high dose of Tiangou Jiangya capsule can remarkably reduce the systolic pressure, diastolic pressure and mean arterial pressure of spontaneous hypertensive rats (P < 0.05 or P < 0.01). The low, middle dose can reduce the heart rate of rats (P < 0.01). The low dose can effectively inhibit the left ventricle indexes (P < 0.05). The Tiangou Jiangya capsule has no markedly effects on the renin-angiotensin-aldosterone system (RAAS) activity and urinary output of rats.

CONCLUSIONThe results indicate that the Tiangou Jiangya capsule has evident effect of lowering blood pressure of rats, which is related to reducing heart rate, heart ventricle indexes, and has no effect on the RAAS and diuresis.

Animals ; Antihypertensive Agents ; pharmacology ; therapeutic use ; Benzyl Alcohols ; pharmacology ; therapeutic use ; Blood Pressure ; drug effects ; Disease Models, Animal ; Diuresis ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Flavonoids ; pharmacology ; therapeutic use ; Furans ; pharmacology ; therapeutic use ; Glucosides ; pharmacology ; therapeutic use ; Heart Rate ; drug effects ; Hypertension ; drug therapy ; Lignans ; pharmacology ; therapeutic use ; Male ; Rats ; Rats, Inbred SHR ; Renin-Angiotensin System ; drug effects ; Ventricular Function, Left ; drug effects

OBJECTIVETo evaluate the effects of Tiangou Jiangya capsule on blood pressure and hemodynamics in anesthetized Beagle dogs.

METHODAnesthetized dogs were divided into five groups: Tiangou Jiangya capsule 3-dose groups as 1.6, 3.2, 6.4 g x kg(-1), positive control group was giving captopril, negative control was giving 0.5% CMC-Na, duodenal administration. The blood pressure and hemodynamic changes were observed.

RESULTThe systolic blood pressure of middle-dose Tiangou Jiangya capsule group was significantly reduced at 30 min after administration. The systolic blood pressure (SAP) and diastolic blood pressure (DAP) of high-dose group of Tiangou Jiangya capsule was significantly reduced at 15 min to 90 min after administration. High-dose Tiangou Jiangya capsule can also significantly reduce cardiac work (LVW) and total peripheral resistance (TPR). Tiangou Jiangya capsule had no significant effect on the other hemodynamic parameters and myocardial oxygen consumption.

CONCLUSIONTiangou Jiangya capsule has a significant effect on reducing blood pressure, which is related to the reducing total peripheral resistance and reducing cardiac work. The result can provide a reference to further clarify the Tiangou Jiangya capsule mechanism on reducing blood pressure.

Animals ; Antihypertensive Agents ; administration & dosage ; pharmacology ; therapeutic use ; Benzyl Alcohols ; pharmacology ; therapeutic use ; Blood Pressure ; drug effects ; Disease Models, Animal ; Dogs ; Drugs, Chinese Herbal ; administration & dosage ; pharmacology ; therapeutic use ; Female ; Flavonoids ; pharmacology ; therapeutic use ; Furans ; pharmacology ; therapeutic use ; Glucosides ; pharmacology ; therapeutic use ; Heart Rate ; drug effects ; Hemodynamics ; drug effects ; Hypertension ; drug therapy ; Lignans ; pharmacology ; therapeutic use ; Male ; Oxygen Consumption ; drug effects ; Vascular Resistance ; drug effects