[Decocting kinetics of Moringa oleifera leaves: based on correlation of decocting factors and multiple components].

Content of multiple components (neochlorogenic acid,L-tryptophan,vicenin-2,isoquercitrin,and astragalin) in Moringa oleifera leaves was determined by high-performance liquid chromatography (HPLC),and the absolute content-time curves were plotted.Based on Fick's law of diffusion and Higbie's penetration theory,the parameters of the equations were calculated,and the measured results were substituted into the mathematical model to fit the equations.The n and a obtained from the equations on the decocting time factor and the solvent volume were close to each other.The dynamic models of the five components are as follows:■.The variation of the content of multiple components in M.oleifera leaves with time and solvent volume was explored.It was found that the content of the components was the highest when the leaves were decocted for 30 min with solvent volume 12 folds of the medicinal material.The dissolution and destruction of components and the diffusion movement of components are the main causes of the content change of M.oleifera leaves at different time and with different solvent volumes.The R~2of the linear equations on the content and the equations on the decocting process (5-30min and solvent volume 12-20 folds of the medicinal materials) was≥0.999 8 and≥0.9,respectively.Thus,the content determination and the decocting kinetic model had high accuracy,which can reflect the change law of the content of key components in M.oleifera leaves during the decoction.This study is expected to serve as a reference for optimizing the decocting technology.

Pharmacology, Toxicity, Bioavailability, and Formulation of Magnolol: An Update.

Magnolol (MG) is one of the primary active components of Magnoliae officinalis cortex, which has been widely used in traditional Chinese and Japanese herbal medicine and possesses a wide range of pharmacological activities. In recent years, attention has been drawn to this component due to its potential as an anti-inflammatory and antitumor drug. To summarize the new biological and pharmacological data on MG, we screened the literature from January 2011 to October 2020. In this review, we provide an actualization of already known anti-inflammatory, cardiovascular protection, antiangiogenesis, antidiabetes, hypoglycemic, antioxidation, neuroprotection, gastrointestinal protection, and antibacterial activities of MG. Besides, results from studies on antitumor activity are presented. We also summarized the molecular mechanisms, toxicity, bioavailability, and formulations of MG. Therefore, we provide a valid cognition of MG.

Pharmacokinetics, tissue distribution, bioavailability, and excretion of nuciferine, an alkaloid from lotus, in rats by LC/MS/MS.

OBJECTIVE: In order to characterize the pharmacokinetics, tissue distribution, bioavailability, and excretion of nuciferine, a reliable gradient LC/MS/MS-based method was developed and validated. METHODS: Sprague-Dawley rats were intravenously injected with a bolus of nuciferine (0.2 mg/kg) and orally given a single dose of nuciferine (10.0 mg/kg). Blood samples were withdrawn via the ocular vein at specific times. Organs, including the liver, kidney, brain, lung, heart, and spleen, were collected at specific times after oral administration of 10.0 mg/kg nuciferine. The plasma and tissue samples were assayed by LC/MS/MS. RESULTS: The results indicated that nuciferine had rapid distribution and poor absorption into systemic circulation. The value of absolute bioavailability was only 1.9 ± 0.8% after administration of 10.0 mg/kg nuciferine by oral and administration of 0.2 mg/kg nuciferine intravenously (IV) to rats. The AUC0→4 h values in tissues were in the order of kidney > lung > spleen > liver > brain > heart. The majority of excretion of nuciferine (50.7%) was excreted through kidneys with parent drug after oral administration without liver metabolism. CONCLUSION: This study may provide a meaningful basis for clinical application of such a bioactive compound of herbal medicines.

Zephycandidine A, the First Naturally Occurring Imidazo[1,2-f]phenanthridine Alkaloid from Zephyranthes candida, Exhibits Significant Anti-tumor and Anti-acetylcholinesterase Activities.

Zephycandidine A (1), the first naturally occurring imidazo[1,2-f]phenanthridine alkaloid, was isolated from Zephyranthes candida (Amaryllidaceae). The structure of 1 was elucidated by spectroscopic analyses and NMR calculation, and a plausible biogenetic pathway for zephycandidine A (1) was proposed. Zephycandidine A (1) exhibited significant cytotoxicity against five cancer cell lines with IC50 values ranging from 1.98 to 7.03 µM with selectivity indices as high as 10 when compared to the normal Beas-2B cell. Further studies suggested that zephycandidine A (1) induces apoptosis in leukemia cells by the activation of caspase-3, upregulation of Bax, downregulation of Bcl-2, and degradation of PARP expression. In addition, zephycandidine A (1) showed acetylcholinesterase (AChE) inhibitory activity, and the docking studies of zephycandidine A (1) and galanthamine (2) with AChE revealed that interactions with W286 and Y337 are necessary.

Binding of citreoviridin to human serum albumin: multispectroscopic and molecular docking.

Citreoviridin (CIT), a mycotoxin produced by Penicillium citreonigrum, is a common contaminant of wide range of agriproducts and detrimental to human and animal health. In this study, the interaction of CIT with human serum albumin (HSA) is researched by steady-state fluorescence, ultraviolet-visible (UV-Vis) absorption, circular dichroism (CD) methods, and molecular modeling. The association constants, binding site numbers, and corresponding thermodynamic parameters are used to investigate the quenching mechanism. The alternations of HSA secondary structure in the presence of CIT are demonstrated with UV-Vis, synchronous fluorescence, and CD spectra. The molecular modeling results reveal that CIT can bind with hydrophobic pocket of HSA with hydrophobic and hydrogen bond force. Moreover, an apparent distance of 3.25 nm between Trp214 and CIT is obtained via fluorescence resonance energy transfer method.

Effects of Yerba Mate tea (Ilex paraguariensis) on vascular endothelial function and liver lipoprotein receptor gene expression in hyperlipidemic rats.

Yerba Mate tea (Mate), an infusion made from the leaves of the tree Ilex paraguariensis, is a widely consumed beverage in South America. This study was performed to investigate the effect of Mate tea on vascular endothelial dysfunction and liver lipoprotein receptor gene expression in hyperlipidemic rats, with the aim of gaining insight into its known lipid-lowering protective mechanisms. Sixty male Sprague-Dawley rats were randomly divided into five groups: a normal control group (NC), a high-fat diet group (HC), and three Mate tea-treated groups. In the NC group, rats were fed with standard diet while in the other groups the rats were fed a high-fat diet for 8weeks. In the Mate tea-treated groups, the rats were fed a high-fat diet supplemented with low, moderate or high concentrations of aqueous Mate tea extract for the final 4weeks. Compared to the HC group, aqueous Mate tea extract significantly reduced endothelin (ET) and thromboxane B(2) (TXB(2)) levels and increased nitric oxide (NO) and 6-keto prostaglandin F(1α) (6-keto-PGF(1α)) levels in the blood, reduced the pathological damage of vascular endothelial cells, decreased intercellular adhesion molecule-1 (ICAM-1) protein expression in the thoracic aorta, and upregulated mRNA expression of hepatic low density lipoprotein receptor (LDLR) and scavenger receptor B1 (SR-B1). These findings indicate that Mate tea administration might have a regulatory effect on blood fat and endothelial function in hyperlipidemia rats. The mechanism may involve protecting vascular endothelial cell function and upregulating the expression of LDLR and SR-B1 genes, thereby inhibiting the occurrence of atherosclerosis.

Aqueous extract of Yerba Mate tea lowers atherosclerotic risk factors in a rat hyperlipidemia model.

Yerba Mate tea (Mate) is believed to be a natural source of cardioprotective lipid-lowering and antioxidant compounds. In this study, the antihyperlipidemic and antioxidant effects of Mate tea in a rat hyperlipidemia model were investigated. Male Sprague-Dawley rats were divided randomly into five groups and fed varying diets: standard diet, hyperlipidemic diet, and hyperlipidemic diet supplemented with low, moderate, or high concentrations of Mate tea aqueous extract (1%, 2%, and 4% w/v, respectively). Compared to the hyperlipidemic control group, Mate tea reduced significantly the total body weight and lowered serum levels of total cholesterol, triglyceride, and low-density lipoprotein-cholesterol, and caused the elevation of serum levels of high-density lipoprotein-cholesterol. Moreover, activities of superoxide dismutase and glutathione peroxidase in serum were elevated significantly, whereas the levels of malondialdehyde decreased. In addition, Mate tea treatment ameliorated significantly the severe fatty degeneration of liver cells that occurred in the hyperlipidemic groups. The relative levels of sterol regulatory element binding protein 1 and its target fatty acid synthase, as well as acetyl-CoA carboxylase mRNA transcripts were reduced, whereas peroxisome proliferator-activated receptor alpha mRNA transcripts were elevated in the Mate tea groups. Our results suggest that Mate tea exerts strong antioxidant and lipid-lowering effects, prevents hepatic fatty deposition, and regulates the expression of lipid metabolic regulators. It can therefore be used to reduce the risk of atherosclerosis.

In vitro evaluation of a Folate-bovine serum albumin-doxorubicin conjugate.

Doxorubicin (DOX) is one of the most effective anticancer drugs. However, its therapeutic effectiveness is greatly hampered by its dose limiting and cumulative cardiotoxic side effects. To overcome these limitations, bioconjugates of DOX were studied using bovine serum albumin (BSA) as a carrier to provide passive tumor targeting by the enhanced permeability and retention (EPR) effect. Folic acid, as an active targeting agent, was linked to BSA to increase the selectivity of the conjugate. In the present study, folate-targeted (Folate-BSA-DOX) conjugates were prepared. In the optimization process, we found that 30 mg of folic acid activated esters reacted with BSA at pH 9.8 for 1 h, the yield was maximum. The qualitative analysis of fluorescent experiments revealed that Folate-BSA-DOX can be specifically delivered to Hela cells and that this unique interaction can be blocked by 1 mM free folic acid. More importantly, the enhanced efficiency of uptake of Folate-BSA-DOX by Hela cells was coupled with the increase of the amount of the conjugate, the incubated time and the conjugated ratio of folic acid. Finally, the quantitative data obtained from the flow cytometry further verified the higher targeting and killing ability of Folate-BSA-DOX to folate receptor positive tumor cells than BSA-DOX.

Folate receptor-targeted quantum dot liposomes as fluorescence probes.

In this study, the preparation of the novel imaging agents, folate receptor (FR)-targeted liposomes encapsulating hydrophilic CdTe quantum dots (QDs), and their use as luminescence probes for live cell imaging are reported. Hydrophilic CdTe QDs were directly synthesized in the water phase, and FR-targeted QD liposomes were prepared by hydrating the lipid thin film with CdTe suspension. Formulations were characterized by UV-visible and fluorescent measurements, liposomal particle size, and zeta potential. The targeting and imaging ability of FR-targeted liposomes were investigated against the human uterine cervix cancer cell line (HeLa). Furthermore, the cytotoxicity of QD liposomes was evaluated by HeLa cells incubated with FR-targeted QD liposomes, nontargeted QD liposomes, and free QDs. The results showed that FR-targeted QD liposomes were spherically shaped with high fluorescence yield, excellent photochemical stability, good cancer targeting, and minimal cytotoxicity. The average size of FR-targeted fluorescence liposomes was ~105 nm, and their size distribution was rather narrow. After storage at 4 degrees C for 11 months, QD liposomes maintained similar size and did not show any leakage of QDs. FR-targeted CdTe QD liposomes, which can target tumor cells via FR-mediated endocytosis, would become an attractive probe for tumor cell or tissue imaging for a long-time monitoring.