Cytisine derivatives are a group of alkaloids containing the structural core of cytisine, which are mainly distributed in Fabaceae plants with a wide range of pharmacological activities, such as resisting inflammation, tumors, and viruses, and affecting the central nervous system. At present, a total of 193 natural cytisine and its derivatives have been reported, all of which are derived from L-lysine. In this study, natural cytisine derivatives were classified into eight types, namely cytisine type, sparteine type, albine type, angustifoline type, camoensidine type, cytisine-like type, tsukushinamine type, and lupanacosmine type. This study reviewed the research progress on the structures, plant sources, biosynthesis, and pharmacological activities of alkaloids of various types.
Alkaloids/chemistry* ; Quinolizines/pharmacology* ; Azocines/chemistry* ; Fabaceae

OBJECTIVETo study the effects of matrine on gamma-globin synthesis in K562 cells in vitro.

METHODSBenzidine staining was used to study the dose- and time-dependent effects of matrine on hemoglobin synthesis in K562 cells, and Western blotting was performed to determine the level of hemoglobin F(alpha(2)gamma(2)).

RESULTSBenzidine staining showed that K562 cells treated with matrine of 0.1 mg/ml had a positivity rate for benzidine (BZ%) of 15.67% at 96 h after the treatment, and Western blotting indicated increased synthesis of hemoglobin F.

CONCLUSIONMatrine can induce gamma-globin synthesis and increase hemoglobin F level in K562 cells, the effect of which resembles that of sodium butyrate.

Alkaloids ; pharmacology ; Blotting, Western ; Fetal Hemoglobin ; biosynthesis ; Globins ; biosynthesis ; Humans ; K562 Cells ; Quinolizines ; pharmacology

OBJECTIVETo study the inhibitory and inductive effect of matrine (MA) on human colorectal cancer HT29 cells.

METHODSMTT assay was used to determine the cell growth inhibitory rate in vitro . Changes of cell cycle and the apoptosis of HT29 cells before and after MA treatment were observed using flow cytometry and electron microscope.

RESULTSMTT showed that 2-32 mg/mL MA inhibited the proliferation of HT29 cells (P < 0.05) in a dose- and time-dependent manner. Cells treated by 4, 8, and 16 mg/mL MA at G0/G1 phase were obviously higher than those in the negative control group (P < 0.05), indicating that the cell cycle was arrested at G0/G1 phase. Morphological apoptosis of HT29 cells could be seen under transmission electron microscope.

CONCLUSIONMA inhibited the proliferation of HT29 cells, and its mechanism might be associated with stagnation at G0/G1 phase and inducing apoptosis of HT29 cells.

Alkaloids ; pharmacology ; Apoptosis ; drug effects ; Cell Proliferation ; drug effects ; HT29 Cells ; Humans ; Quinolizines ; pharmacology

Alkaloids ; pharmacology ; Cisplatin ; pharmacology ; Fluorouracil ; pharmacology ; Hep G2 Cells ; Humans ; Quinolizines ; pharmacology ; Tumor Necrosis Factor Ligand Superfamily Member 13 ; metabolism

Alkaloids ; pharmacology ; Animals ; Liver Neoplasms, Experimental ; enzymology ; prevention & control ; Quinolizines ; pharmacology ; Rats ; Selenium ; pharmacology ; Telomerase ; metabolism ; Yeast, Dried ; pharmacology

OBJECTIVETo study the anti-cancer effect of matrine (Mat) on U937 cell line and its possible molecular mechanism.

METHODThe cells were cultured in medium containing either 0.1, 0.2, 0.3, 0.4, or 0.5 g x L(-1) of Mat. The morphological alteration was observed by inverted microscopy and electron microscopy. Cell proliferation was analyzed by Try pan blue staining and MTT. The method of Western Blot was used to detect phosphorylation activity of MAPK.

RESULTMatrine had a significant inhibitory effect on proliferation of U937 cell line at the concentration of 0.2 g x L(-1). Treated with matrine of 0.2 g x L(-1) for 48 h, U937 cells became smaller and appeared more round than previously. The number of U937 cells showing apoptosis increased with elevation of the concentration of the matrine. Matrine had an ability of inhibiting the activity of ERK and increasing the activities of p38 and JNK to some degree in U937 cells.

CONCLUSIONMatrine can inhibit the proliferation of U937 cell line in vitro and induce its apoptosis possibly through inhibiting the activity of ERK and increasing the activities of p38 and JNK in U937 cells.

Alkaloids ; pharmacology ; Apoptosis ; drug effects ; Cell Proliferation ; drug effects ; Humans ; MAP Kinase Signaling System ; drug effects ; Quinolizines ; pharmacology ; U937 Cells

OBJECTIVETo observe the effect of matrine on human ether à go-go related gene (HERG) potassium channels expressed in Chinese hamster ovary (CHO) cells and investigate whether HERG channel is a new target of the pharmacological effect of matrine on arrhythmia and tumor

METHODSHERG channel potassium current in CHO cell was recorded using whole-cell patch-clamp technique, and the influence of matrine on the current was explored.

RESULTSMatrine inhibited HERG potassium current in a dose-dependent manner, and the 50% inhibitory concentration (IC IC(50)) was 411±23 μmol/L. Matrine had no significant effect on the activation kinetics, and mainly blocked HERG channels in their closed state.

CONCLUSIONSThe blocking effect of matrine on HERG channels might be one of the mechanisms against arrythmias and tumors. Unlike most other blockers exerting blocking effect at the intracellular sites by entering the cell with the opening of HERG channel, matrine blocked HERG channels at the extracellular sites.

Alkaloids ; pharmacology ; Animals ; CHO Cells ; Cricetinae ; Cricetulus ; ERG1 Potassium Channel ; Ether-A-Go-Go Potassium Channels ; genetics ; metabolism ; Humans ; Quinolizines ; pharmacology

OBJECTIVETo observe the effect of Oxymatrine on left cardiac function and ventricular remodeling in rabbits after acute myocardial infarction.

METHODSLigation of the left anterior descending artery was adopted to establish acute myocardial infarction model, forty eight rabbits were randomized into the sham operation group, model group and Oxymatrine group. Eight models were successfully established in each group. the sham operation group and model group were given conventional feed. Oxymatrine were gavage administration 0.5 ml/100 g, once a day, lasted for 4 weeks. Respectively in postoperative week, and three weeks, to observe the Oxymatrine on cardiac output (CO), left ventricular end systolic pressure (LVESP), left ventricular end-diastolic pressure (LVEDP), left indoor pressure change rate peak (dp/dtmax)), and left ventricular cavity internal diameter (D), ventricular weight index (VWI), ventricular weight (VW).

RESULTSLeft ventricular anterior wall was from red to deep purple, electrocardiogram showed II guide ST-segment camber up ≥ 0.25 mv. Postoperative week in Oxymatrine group compared with model group, LVESP increased significantly (P < 0.01), LVEDP decreased obviously (P < 0.01); After three weeks in Oxymatrine group compared with model group, VW, VWI decreased (P < 0.05), D significantly reduced (P < 0.01); LVESP increased significantly (P < 0.01), LVEDP decreased obviously (P <0.01); dp/dt(max), CO increased (P < 0.05).

CONCLUSIONAfter acute myocardial infarction in rabbit Oxymatrine can improve the left ventricular reconstruction parameters, increase cardiac output, and improve cardiac function.

Alkaloids ; pharmacology ; Animals ; Cardiac Output ; Heart ; drug effects ; Myocardial Infarction ; pathology ; Quinolizines ; pharmacology ; Rabbits ; Ventricular Remodeling ; drug effects

Alkaloids ; pharmacology ; Angiogenesis Inhibitors ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Drugs, Chinese Herbal ; chemistry ; Ginsenosides ; pharmacology ; Humans ; Lymphatic Metastasis ; prevention & control ; Pyrazines ; pharmacology ; Quinolizines

OBJECTIVEMatrine has an anti-fibrosis effect, such as hepatic cirrhosis and derma fibrosis, while its effect on glomerulosclerosis is unknown. The purpose of this study was to analyze the renoprotective effects of matrine on experimental glomerulosclerosis in rats and inquire into its mechanisms.

METHODSThe rats were randomly assigned to following groups: normal control group, model control group, benazepril treatment group, matrine 100 mg/kg treatment group and matrine 50 mg/kg treatment group. The rats of normal control group were subjected to sham operation and were injected with normal saline via the tail vein one week later. The rats of the other groups were uninephrectomized and injected with adriamycin (5 mg/kg) via the tail vein one week later. The dose of benazepril was 6 mg/kg. Both matrine and benazepril were given by gastric perfusion from the first day after the operation. The level of urinary protein was measured at the 2nd, 4th and 6th week after the operation. The serum total protein and albumin, serum creatinine, blood urea nitrogen (BUN) were tested only at the 6th week after operation. Renal pathology changes were evaluated at the 6th week as well. Immunohistochemistry was used to detect the expression of fibronectin (FN), laminin (LN), connective tissue growth factor (CTGF) and transforming growth factor-beta1 (TGF-beta1) in glomeruli.

RESULTSMatrine and benazepril not only reduced the excretion of urinary protein and the level of serum creatinine and BUN, but also significantly ameliorated glomerular mesangial proliferation and glomerular sclerosis (P < 0.05, respectively). Immunohistochemical staining indicated that there was an increasing FN, LN, CTGF and TGF-beta1 expression in model control group as compared to the three treatment groups (P < 0.05). Matrine 100 mg/kg treatment group and benazepril treatment group showed much more advantages than matrine 50 mg/kg treatment group (P < 0.05), but there was no significant difference between the former two groups (P > 0.05).

CONCLUSIONMatrine has a renoprotective effect on experimental glomerulosclerosis in rats, the possible mechanism might relate to the reduction of the TGF-beta1 negative function via CTGF, which will inhibit the activation and proliferation of glomerular intrinsic cells, decrease the secretion of ECM accordingly.

Alkaloids ; pharmacology ; Animals ; Benzazepines ; pharmacology ; Kidney ; drug effects ; Kidney Diseases ; prevention & control ; Kidney Glomerulus ; drug effects ; Protective Agents ; pharmacology ; Quinolizines ; pharmacology ; Rats ; Renal Agents ; pharmacology