The unique properties of nanodiamonds (NDs) such as chemical stability, surface modifiability and remarkable biocompatibility impart them with a great opportunity to be versatile platforms for drug delivery. In this study, chemotherapeutic doxorubicin (DOX) and cell penetrating peptide TAT were conjugated to the surface of NDs in sequence through carbodiimide coupling in order to avoid premature release and enhance the intracellular delivery of DOX. The cytotoxicity, intracellular location and cellular uptake of DOX-conjugated NDs with or without TAT were evaluated in C6 glioma cells. Our results revealed that conjugation of TAT to ND-DOX could enhance the translocation across the cell membrane and exhibit a higher cytotoxicity effect than free DOX. This antitumor drug and penetrating peptide-conjugated ND drug delivery system therefore represents a novel delivery system with promoted antineoplastic activity of therapeutics and minimized side effects.
Rhein, an active ingredient extensively found in plants such as Aloe, Cassitora L., rhubarb and so on, has been used for a long time in China. Pharmacological tests revealed that rhein not only had a strong antibacterial action, but also may be useful in cancer chemotherapy as a biochemical modulator. Its therapeutic action and toxicity is still the subject of considerable research. With microsome incubation assays in vitro and HPLC methods, the inhibition of rat liver CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A enzymes by rhein were studied kinetically. The results showed the most inhibition of CYP2E1 by rhein (K(i) = 10 microm, mixed); CYP3A and CYP2C9 were also inhibited by rhein, K(i) = 30 microm (mixed) and K(i) = 38 microm (mixed), respectively; rhein revealed some inhibition of CYP1A2 (K(i) = 62 microm, uncompetitive) and CYP2D6 (K(i) = 74 microm, mixed). Drug-drug interactions, especially cytochrome P450 (CYP)-mediated interactions, cause an enhancement or attenuation in the efficacy of co-administered drugs. Inhibition of the five major CYP enzymes observed for rhein suggested that changes in pharmacokinetics of co-administered drugs were likely to occur. Therefore, caution should be paid to the possible drug interaction of medicinal plants containing rhein and CYP substrates.
Herein we report on metallization of Cu on to surface-modified polyimide resin, the method of which relies on potassium hydroxide-induced modification of the polyimide surface to introduce carboxylic acid groups and incorporation of gold colloids as a seed layer through reduction of chloroauric acid. The contact angle of modified polyimide surface with water changed from 70 to 35 due to the hydrolysis of polyimide. Secondary amine group on the surface was detected with attenuated total reflection (ATR) Fourier transform infrared (FTIR) spectrophotometry, suggesting that tertiary amine group has turned into secondary group. In addition, on the basis of hydrophilic behavior, we succeeded in depositing gold colloids on the chemically modified surface. SEM image of copper electroless plated on polyimide surface indicated that copper particles were compact and about $ 300 nm in diameter. It showed that gold colloids provide an excellent conductive layer to catalyze the electroless plating of Cu on polyimide surface.
Through modular ROMP (ring-opening metathesis polymerization), biofunctional polynorbornenes are designed and fabricated from panchromatic fluorophores, bioactive peptides, and polyethylene glycol solubilizer for organelle-specific multicolor imaging. Attributed to the free permutation and combination of highly fluorescent red rhodamine B, green dichlorofluorescein and blue 9,10-diphenylanthracene fluorophores as well as signaling peptide sequences of F rFK and TAT, we successfully realize simultaneous multicolor imaging toward lysosomes and mitochondria in living cells first utilizing polymeric scaffolds. If more biofunctions could be incorporated, modularly designed copolymer would provide a promising opportunity to facilitate multitasking application to monitoring intracellular alterations and elucidating complex biological processes.
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