Targeting the tubulin C-terminal tail by charged small molecules.

The disordered tubulin C-terminal tail (CTT), which possesses a higher degree of heterogeneity, is the target for the interaction of many proteins and cellular components. Compared to the seven well-described binding sites of microtubule-targeting agents (MTAs) that localize on the globular tubulin core, tubulin CTT is far less explored. Therefore, tubulin CTT can be regarded as a novel site for the development of MTAs with distinct biochemical and cell biological properties. Here, we designed and synthesized linear and cyclic peptides containing multiple arginines (RRR), which are complementary to multiple acidic residues in tubulin CTT. Some of them showed moderate induction and promotion of tubulin polymerization. The most potent macrocyclic compound 1f was found to bind to tubulin CTT and thus exert its bioactivity. Such RRR containing compounds represent a starting point for the discovery of tubulin CTT-targeting agents with therapeutic potential.

A review for discovering bioactive minor saponins and biotransformative metabolites in Panax quinquefolius L.

Panax quinquefolius L. has attracted extensive attention worldwide because of its prominent pharmacological properties on type 2 diabetes, cancers, central nervous system, and cardiovascular diseases. Ginsenosides are active phytochemicals of P. quinquefolius, which can be classified as propanaxdiol (PPD)-type, propanaxtriol (PPT)-type, oleanane-type, and ocotillol-type oligo-glycosides depending on the skeleton of aglycone. Recently, advanced analytical and isolated methods including ultra-performance liquid chromatography tandem with mass detector, preparative high-performance liquid chromatography, and high speed counter-current chromatography have been used to isolate and identify minor components in P. quinquefolius, which accelerates the clarification of the material basis. However, the poor bioavailability and undetermined bio-metabolism of most saponins have greatly hindered both the development of medicines and the identification of their real active constituents. Thus, it is essential to consider the bio-metabolism of constituents before and after absorption. In this review, we described the structures of minor ginsenosides in P. quinquefolius, including naturally occurring protype compounds and their in vivo metabolites. The preclinical and clinical pharmacological studies of the ginsenosides in the past few years were also summarized. The review will promote the reacquaint of minor saponins on the growing appreciation of their biological role in P. quinquefolius.

An environmental energy-enhanced solar steam evaporator derived from MXene-decorated cellulose acetate cigarette filter with ultrahigh solar steam generation efficiency.

Although solar energy is promising for water purification, there is still a room for further improving the solar steam generation efficiency. Herein, an environmental energy-enhanced solar steam evaporator is fabricated by immersing a cellulose acetate fiber-based cigarette filter (CF) in an aqueous solution of polyvinyl alcohol (PVA) followed by freeze-drying and decorating with MXene sheets. The presence of MXene is to absorb solar light and convert solar energy to thermal energy for efficient water evaporation, while the porous PVA network generated inside the pores of the filter during the freeze-drying process accommodates the dispersed MXene sheets and interconnects the CF and MXene. Because of the constructed PVA/MXene network inside the CF porous architecture and the hydrophilic feature of both MXene and PVA, the resultant MXene/PVA modified CF (MPCF) is highly hydrophilic and competent for rapid upward transfer of water. Interestingly, in addition to the normal energy input by the incident solar light, the large-area sidewall of MPCF gains thermal energy from the environment in the forms of heat convection and heat radiation to enhance the solar steam generation efficiency, resulting in an ultrahigh water evaporation rate of 3.38 kg m-2 h-1 with an outstanding evaporation efficiency of 132.9%.