Cancer is a preeminent threat to the human race, causing millions of deaths each year on the Earth. Traditionally, natural compounds are deemed promising agents for cancer treatment. Cantharidin (CTD)—a terpenoid isolated from blister beetles—has been used extensively in traditional Chinese medicines for healing various maladies and cancer. CTD has been proven to be protein phosphatase 2A (PP2A) and heat shock transcription factor 1 (HSF-1) inhibitor, which can be potential targets for its anticancer activity. Albeit, it harbors some toxicities, its immense anticancer potential cannot be overlooked, as the cancer-specific delivery of CTD could help to rescue its lethal effects. Furthermore, several derivatives have been designed to weaken its toxicity. In light of extensive research, the antitumor activity of CTD is evident in both in vitro as well as in vivo cancer models. CTD has also proven efficacious in combination with chemotherapy and radiotherapy and it can also target some drug-resistant cancer cells. This mini-review endeavors to interpret and summarize recent information about CTD anticancer potential and underlying molecular mechanisms. The pertinent anticancer strength of CTD could be employed to develop an effective anticarcinogenic drug.
A novel norsesquiterpene, named norcyperone (1), and three known compounds: (-)-clovane-2,9-diol (2), rosenonolactone (3), and 5a,8a-epidioxy-(20S,22E,24R)-ergosta-6,22-dien-3β-ol (4) were isolated from the rhizomes of Cyperus rotundus L. The structure of 1 was elucidated as 8,11,11-trimethylbicyclo[5.3.1]undecane-5a, 8a-epoxy-3-one on the basis of extensive spectroscopic analyses, including 1D- and 2D-NMR, MS experiments, and single-crystal X-ray diffraction. This is the first report of a 8,11,11-trimethyl- bicyclo[5.3.1]undecane-3-one type norsesquiterpene with a tetrahydrofuran ring at C-5 and C-8.
7 January 2022 in Frontiers in Bioengineering and Biotechnology
Polycaprolactone (PCL) has been widely used as a scaffold material for tissue engineering. Reliable applications of the PCL scaffolds require overcoming their native hydrophobicity and obtaining the sustained release of signaling factors to modulate cell growth and differentiation. Here, we report a surface modification strategy for electrospun PCL nanofibers using an azide-terminated amphiphilic graft polymer. With multiple alkylation and pegylation on the side chains of poly-L-lysine, stable coating of the graft polymer on the PCL nanofibers was achieved in one step. Using the azide-alkyne “click chemistry”, we functionalized the azide-pegylated PCL nanofibers with dibenzocyclooctyne-modified nanocapsules containing growth factor, which rendered the nanofiber scaffold with satisfied cell adhesion and growth property. Moreover, by specific immobilization of pH-responsive nanocapsules containing bone morphogenetic protein 2 (BMP-2), controlled release of active BMP-2 from the PCL nanofibers was achieved within 21 days. When bone mesenchyme stem cells were cultured on this nanofiber scaffold, enhanced ossification was observed in correlation with the time-dependent release of BMP-2. The established surface modification can be extended as a generic approach to hydrophobic nanomaterials for longtime sustainable release of multiplex signaling proteins for tissue engineering.