Raloxifene, identified as a novel LSD1 inhibitor, suppresses the migration of renal cell carcinoma.

Aim: As an important epigenetic modulator, histone lysine-specific demethylase 1 (LSD1) has been proved to be associated with the progression of renal cell carcinoma (RCC). Discovering novel LSD1 inhibitors offers therapeutic potential for RCC treatment. Methods & Results: We identified raloxifene as a novel LSD1 inhibitor (IC50 = 2.08 µM) through small compound library screening. Molecular docking indicated raloxifene might bind LSD1 in the flavin adenine dinucleotide (FAD) binding cavity in a reversible manner. Cell viability and migration assays showed raloxifene could suppress the proliferation and migration of RCC cells bearing overexpressed LSD1. Conclusion: Our findings indicated that LSD1 might be a promising therapeutic target for RCC and that raloxifene could serve as a lead compound for further anti-RCC metastasis drug discovery.

Molybdenum sulfide-based electrochemical platform for high sensitive detection of taxifolin in Chinese medicine.

MoS2 and nitrogen doped active carbon composite (MoS2/ANC) is fabricated to detect taxifolin and exhibits superior redox current response and decreased redox potential difference. Further investigation reveals that the kinetic process of the redox reaction of taxifolin on MoS2/ANC electrode is controlled by both adsorption and diffusion process. Under the optimum conditions, the redox peak currents linearly relate with the concentration of taxifolin in the range of 1 × 10-9-1 × 10-6 mol L-1, accompanied by the low detection limit (3 × 10-10 mol L-1). Meanwhile, outstanding selectivity, stability and repeatability are also obtained at MoS2/ANC electrode. At last, the proposed method is applied to quantitatively detect taxifolin in fructus polygoni orientalis and satisfactory results have been achieved.

A voltammetry sensor platform for baicalein and baicalin simultaneous detection in vivo based on Ta2O5-Nb2O5@CTS composite.

Baicalein and baicalin are the major flavonoids found in Scutellariae Radix, an essential herb which has had a presence in traditional Chinese medicine (TCMs) for more than two thousands of years. Owing to their similar characteristics and physiochemical properties, sensitive, it is a great challenge to detect both of them simultaneously. In this work, a novel, facile and sensitive electrochemical method was proposed based on tantalum oxide (Ta2O5), niobium oxide (Nb2O5) particles and antiseptic chitosan modified carbon paste electrode (Ta2O5-Nb2O5@CTS-CPE). Scanning electron microscope (SEM), X-ray diffraction spectroscopy (XRD), Fourier transform infrared spectroscopy (FTIR), cyclic voltammetry (CV) and electrochemical impedance spectrum (EIS) were used to characterize the properties and investigate the electrochemical response of the sensor. The electrochemical behaviors and redox mechanisms of two analytes were investigated at the target electrode. Under the optimum conditions, the highly sensitive and simultaneous determination of baicalein and baicalin was successfully achieved with a linear response range of 0.08-8.0µM for both of them. The obtained detection limits for baicalein and baicalin were of 0.05 and 0.03µM (S/N=3), respectively. Furthermore, the proposed sensor displayed high sensitivity, excellent stability and satisfactory results in Scutellariae Radix samples analysis and hydrolysis process analysis of baicalin in vivo.

Facile synthesized SnO2 decorated functionalized graphene modified electrode for sensitive determination of daidzein.

A one-step and facile method using SnCl2·H2O as reducing agent to reduce graphene oxide (GO) was performed in the aid of poly(diallyldimethylammonium chloride) solution (PDDA). SnCl2·H2O is not only a reducing agent for graphene oxide (GO), but also a precursor of SnO2. SnO2-PDDA-GR composite was characterized by various surface, structural and electrochemical analysis techniques, such as transmission electron microscopy (TEM), UV spectrum (UV-vis), Infrared Spectrum (IR), X-ray diffraction (XRD), Cyclic voltammograms (CV) and electrochemical impedance (EIS). The SnO2-PDDA-GR composite was used to constructed electrochemical sensor (SnO2-PDDA-GR/GCE) for the determination of daidzein. Under the optimized experimental condition, it was found that the response of peak current is linear to the concentration of daidzein in the ranges of 2.0×10-8 -1.0×10-6molL-1, and the detection limit was estimated to be 6.7×10-9mol L-1 (S/N=3). Furthermore, this sensor was successfully applied for the determination of daidzein in traditional Chinese medicine (pueraria lobata) and Daidzein tablets.

Sensitive, simultaneous determination of chrysin and baicalein based on Ta2O5-chitosan composite modified carbon paste electrode.

Chrysin and baicalein are the major flavonoids found in oroxylum indicum, an essential herb in traditional Chinese medicine (TCM). Owing to their similar characteristics and physiochemical property, it is a great challenge to detect both of them simultaneously. In this work, tantalum oxide (Ta2O5) particles and chitosan modified carbon paste electrode (Ta2O5-CTS-CPE) was prepared and characterized by scanning electron microscope (SEM), X-ray diffraction spectroscopy (XRD), Fourier transform infrared spectroscopy (FTIR), cyclic voltammetry (CV) and electrochemical impedance spectrum(EIS). Under the optimum conditions, the prepared Ta2O5-CTS-CPE exhibited excellent electrocatalytic activity toward the oxidation of chrysin and baicalein, and it could serve as the sensor for highly sensitive and simultaneous determination both of them. The linear range is 0.08-4.0µM for both of them, and the detection limits were determined to be 0.03 and 0.05µM (S/N=3) for chrysin and baicalein, respectively. Furthermore, the proposed electrochemical sensor displayed high sensitivity, excellent stability and got satisfactory results in oroxylum indicum samples analysis.

The novel voltammetric method for determination of hesperetin based on a sensitive electrochemical sensor.

A highly sensitive voltammetric sensor, based on reduced graphene oxide on SWCNTs modified glassy carbon electrode (GCE), was constructed and used for sensitive detection of hesperetin. The electrochemical behavior of hesperetin at this sensor was investigated systematically and a novel voltammetric method for determination of hesperetin was proposed. The redox characters of hesperetin was discussed in detail and a reasonable reaction mechanism was proposed also. As the analytical method, the response currents were linear relationship with the hesperetin concentrations in the range of 5.0 × 10(-8) to 3.0 × 10(-6) mol L-(1), with a detection limit of 2.0 × 10(-8) mol L(-1) (S/N=3). The method was also applied successfully to detect hesperetin in biological samples and Chinese herbal medicine Flos buddlejae with satisfactory results.

Electrochemical behavior of tectoridin and its sensitive determination based on L-arginine modified electrode.

A simple, inexpensive and highly sensitive voltammetric method for the determination of tectoridin was developed using a poly(L-Arginine) modified electrode. The redox character of tectoridin at proposed electrode was studied systematically and some dynamic parameters were calculated for the first time. A reasonable reaction mechanism of tectoridin on the poly(L-Arginine)/GCE was also dicussed and proposed, which could be a reference for the pharmacological action of tectoridin in clinical study. And the electroanalytical method for determination of tectoridin was established by differential pulse voltammograms (DPV). Under optimum conditions, the response peak currents were linear relationship with tectoridin concentrations in the range of 5.0×10(-8)-2.0×10(-6) mol L(-1) with a detection limit of 4.0×10(-8) mol L(-1). Therefore, the high sensitivity for tectoridin sensing at the proposed electrode was achieved, and the proposed method could also be used to detect tectoridin in the Chinese medicinal herb Blackberrylily with satisfactory results.

Study of the voltammetric behavior of jatrorrhizine and its sensitive determination at electrochemical pretreatment glassy carbon electrode.

A simple, inexpensive and highly sensitive electrochemical method for the determination of jatrorrhizine was developed using an electrochemically pretreated glassy carbon electrode (EPGCE). The electrochemical behavior of jatrorrhizine was systematically investigated in detail and some kinetic parameters were calculated for the first time. A reasonable reaction mechanism of jatrorrhizine on the EPGCE was also discussed and proposed, which could be a reference for the pharmacological action of jatrorrhizine in clinical study. And the first electroanalytical method of jatrorrhizine was established with a wide linear range from 7.0×10(-8) to 2.0×10(-5)mol L(-1) and a low detection limit of 5.0×10(-8)mol L(-1). The proposed method was successfully applied in determination of jatrorrhizine in pharmaceutical sample, Tinospora capillipes Gagnep (a traditional Chinese medicine), with satisfactory results.

Interaction of anticancer herbal drug berberine with DNA immobilized on the glassy carbon electrode.

The interaction of anticancer herbal drug berberine with double-strand DNA (dsDNA) and single-strand DNA (ssDNA) in solution, dsDNA immobilized on the glassy carbon electrode prepared by Langmuir-Blodgett technique, were investigated by electrochemical techniques (cyclic voltammetry, differential pulse voltammetry) and UV spectroscopy. The presence of DNA results in a decrease of the currents and a negative shift of the electrode potentials from the DPV curves of berberine, indicating the dominance of electrostatic interactions. The spectroscopy data confirmed that the predominant interaction between berberine and DNA is electrostatic. The binding of berberine with DNA, when analyzed in terms of the cooperative Hill model, yields the binding constant K(a)=2.2(+/-0.2)x10(4) M(-1), corresponding to the dissociation equilibrium constant K(d)=4.6(+/-0.3)x10(-5) M, which in the range of the applied concentrations of DNA (bp) and berberine, and a Hill coefficient m=1.82(+/-0.08) in Britton-Robinson buffer solution (0.05 M, pH 5.72) at T=298 K (25 degrees C). Apparently, at least two molecules of berberine have to bind as a couple to cause, e.g., the "elementary event" of current change. The results are suggestive for further fruitful applications of this anticancer herbal drug and DNA-modified electrodes.

Electrochemical studies of the interaction of the anticancer herbal drug emodin with DNA.

The interaction between anticancer herbal drug emodin and DNA was studied with differential pulse voltammetry (DPV) and cyclic voltammetry (CV) at the bare or DNA modified GCE and ultraviolet-visible (UV) spectra. The DPV of emodin showed that peak potentials shifted to more positive value and peak currents decreased with the addition of DNA. UV spectra exhibited that the absorption of emodin at about 440nm decreased with red shift. The results showed that the herbal drug emodin interacted with DNA by intercalating into the double helix of DNA. Under our experiment conditions, the decrease of peak current was proportional to DNA concentration, which can be applied to determining DNA concentration. The combining constant (beta) and combing number (m) of DNA-mEM were determined too.