Natural as well as synthetic coumarins have recently drawn much attention due to its broad pharmacological activities. Many coumarins and their derivatives exert anti-coagulant, anti-tumor, anti-viral, anti-inflammatory and anti-oxidant effects, as well as anti-microbial and enzyme inhibition properties. The recognition of key structural features within coumarin family is crucial for the design and development of new analogues with improved activity and for the characterization of their mechanism of action and potential side effects. The different substituents in the coumarin nucleus strongly influence the biological activity of the resulting derivatives. Although some coumarins have been already characterized to evoke a particular biological activity, the challenge would be the design and synthesis of new derivatives with high specific activity for other pharmacological targets and define their mechanism of action to achieve new therapeutic drugs. The present review highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anti-cancer agents. The major challenges about coumarins include the translation of current knowledge into new potential lead compounds and the repositioning of known compounds for the treatment of cancer.

Coumarins: old compounds with novel promising therapeutic perspectives.

Reversal of multidrug resistance in cancer cells by pyranocoumarins isolated from Radix Peucedani

In this study, the effects of Peucedanum praeruptorum DUNN methanolic extract (PPME) and its major constituents on SGC7901 human gastric cancer cells were evaluated. Two pyranocoumarins, namely, (±) praeruptorin A (PA) and (±) praeruptorin B (PB), were isolated from PPME. A high performance liquid chromatographic (HPLC) method was developed to determine the contents of PA and PB in PPME. The anti-proliferative and cytotoxic actions of PPME were observed using the 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and release of lactate dehydrogenase (LDH) assays. At 300 μg/mL, PPME inhibited cell growth by 51.2% (P < 0.01), probably linked to the high concentration of PA and PB. Both PA and PB exhibited antiproliferative and cytotoxic activities on the SGC7901 cells. Furthermore, the active principle compound, PA, also enhanced the actions of doxorubincin (DOX) on SGC7901 cells. Cell growth decreased higher with the combined treatment of PA and DOX than that with the chemotherapy agent applied alone, suggesting that PA could reduce the dose of DOX for the desired effects.

/pdf/chemopreventive-effects-of-peucedanum-praeruptorum-dunn-and-1t1bcj08z5.pdf

Chemopreventive effects of Peucedanum praeruptorum DUNN and its major constituents on SGC7901 gastric cancer cells.

As a commonly employed traditional Chinese medicine, Peucedani Radix (Qian-hu in Chinese), which consists of the dried roots of Peucedanum praeruptorum Dunn, has a long history of application for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper air-way infections in traditional medicinal practice. The current review aims to summarize the research progress on the botany, phytochemistry, chemical analysis, pharmacological assay, and pharmacokinetic profile of this famous herbal drug. All available information on this traditional medicine was obtained via electronic search (using ACS, PubMed, Web of Science, Google Scholar, Baidu Scholar, and CNKI). Phytochemical investigations revealed that angular-type pyranocoumarins (APs), mainly (±)-praeruptorin A (Pd-Ia), (+)-praeruptorin A, (±)-praeruptorin B, (+)-praeruptorin B (Pd-II) and (+)-praeruptorin E (Pd-III), were the main active components in Qian-hu, while some other types of ingredients were also identified from this herb. The crude extract and pure compounds from Peucedani Radix exhibited a wide spectrum of in vitro and in vivo pharmacological activities, including vasorelaxant, cardioprotective, hepatoprotective, anti-tumor and anti-platelet aggregative effects. Conversely to the well-defined chemical constituents and activities, the properties of absorption, pharmacokinetics, and metabolism were rarely characterized. However, further investigations are wistful for the development of new drugs and therapies for various diseases, especially cardiovascular disorders. Collectively, the present review on the phytochemistry, chemical analysis, pharmacological evaluation, and pharmacokinetic profile of Peucedani Radix will provide meaningful information for further studies and commercial exploitation of the herbal medicine.

/pdf/research-progress-of-the-studies-on-the-roots-of-peucedanum-eex8b668vb.pdf

Research progress of the studies on the roots of Peucedanum praeruptorum dunn (Peucedani radix).

Summary:This study was designed to investigate the effects of berberine on membrane currents forming the repolarization phase of action potentials in isolated guinea pig ventricular myocytes by using the patch-clamp technique. Application of berberine (3-30 μM) to the current-clamped myocytes produc

Ionic Mechanism Responsible for Prolongation of Cardiac Action-Potential Duration by Berberine

With patch clamp technic (whole cell recording), the effect of dl-praeruptorin A (Pra), an ingredient of Peucedanum praeruptorum Dunn on calcium current (ICa) in the single ventricular cells of guinea pig was studied. Results showed that under Cs/Cs condition, when the holding potential was -40 mV and in the presence of Pra (1, 10, 100 mumol.L-1), ICa was decreased dose-dependently from 2.02 +/- 0.24, 2.00 +/- 0.12, 2.12 +/- 0.33 nA (control) to 1.60 +/- 0.24, 1.32 +/- 0.08, 1.16 +/- 0.43 nA, respectively, and their inhibitory rates were 21%, 33.5%, 45%, respectively. The current-voltage relation curve showed that the reversal potential of ICa was +60 mV; the potential producing peak value of ICa was about 0 mV. The results indicated that Pra had a Ca2+ channel blocking effect.

Effect of dl-praeruptorin A on calcium current in ventricular cells of guinea pig

AIM: To study the effects of N-methyl berbamine (NMB) on the delayed outward potassium currents (Ik) in isolated rat hepatocytes. 
METHODS: With patch-clamp techniques and whole-cell recording method, holding potential -50 mV, command potential +30 to +140 mV, duration 900 ms. 
RESULTS: NMB reduced Ik in a concentration-dependent manner. When the concentrations of NMB were 20, 50, 400 nmol.L-1 and 50 mumol.L-1, the amplitude values of Ik were decreased to 3.6 +/- 0.4 (P > 0.05), 2.1 +/- 1.6 (P > 0.05), 3.7 +/- 1.6 (P < 0.05), 2.3 +/- 1.3 nA (P < 0.01) from 4.4 +/- 1.0 (n = 4), 2.5 +/- 1.8 (n = 4), 5.8 +/- 2.1 (n = 5), 4.6 +/- 1.3 (n = 6) nA of control, respectively. The inhibitory rates were 10%, 15%, 37%, and 51%, respectively. 
CONCLUSION: NMB was a K+ channel inhibitor.

Effects of N-methyl berbamine on delayed outward potassium current in isolated rat hepatocytes.

Effects of Pd-Ia,a Component of Chinese Traditional Herb Bai-Hua Qian-Hu,on Ca2+-Current and Action Potential Duration in Single Ventricular Cells of Guinea Pig Hearts

Using a single sucrose gap voltage clamp technique, it was found that berberine hydrochloride (Ber-HCl) had a dose-dependent biphasic effect on Isi of guinea pig papillary muscle. It was more difficult to wash out the inhibitory effect of Ber-HCl on Isi. In the initial stage of the experiment, Ber-HCl 72 mumol/L and 365 mumol/L greatly improved the influx of extracellular Ca2+ and increased the amplitude of Isi. As the drug perfusion was prolonged, however, Ber-HCl dramatically blocked Ca2+ channels and decreased the influx of extracellular Ca2+ consequently, Isi was reduced in amplitude and later disappeared. This experiment further revealed the mechanisms of action of Ber on cardiac contractility and for the treatment of arrhythmias.

Effect of berberine on slow inward ionic current in guinea pig ventricular papillary muscle

Single rabbit sinoatrial node (SAN) cells were isolated by means of an enzymatic dispersion procedure and used for the whole-cell patch clamp experiment. At a holding potential of -40 mV, a time- and voltage-dependent inward current, I(f), was activated at different hyperpolarization potentials from -60 mV to -110 mV. The current-voltage relation curve showed that I(f) was activated at potential more negative than -40 mV. Five min after treatment by CsCl 2 mmol.L-1-containing Tyrode solution, I(f) was almost completely blocked. At a hyperpolarization potential of -110 mV, I(f) was reduced from 1.7 +/- 0.2 nA of the control to 1.2 +/- 0.4 nA after superfusing with Tyrode solution containing berberine (Ber) 1 mumol.L-1 for 5 min. And it was difficult to wash out this action. Ber also had inhibitory effects on other currents to a certain extent. The results indicate that I(f) is a Cs(+)-sensitive current and that the negative chronotropic effect of Ber may be due to the inhibition of I(f) that functions as an important pacemaking modulator for the spontaneous depolarization of SAN tissue.

Whole-cell patch clamp measurements and berberine inhibition of hyperpolarization-activated inward current in rabbit sinoatrial node cells

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