Anoplin is an amphipathic, α-helical bioactive peptide from wasp venom. In recent years, pharmaceutical and organic chemists discovered that anoplin and its derivatives showed multiple pharmacological activities in antibacterial, antitumor, antifungal, and antimalarial activities. Owing to the simple and unique structure and diverse biological activities, anoplin has attracted considerable research interests. This review highlights the advances in structural modification, biological activities, and the outlook of anoplin in order to provide a basis for new drug design and delivery.
Allergic
rhinitis (AR) is a chronic inflammatory reaction by immunoglobulin
E (IgE) mediators after individual contact with allergens. It affects
10–40% of the world’s population and reduces the quality
of life. Long-term symptoms of rhinitis can cause inflammation to
spread and trigger asthma, which can harm human health. Herein, we
develop a Smart PeptIde defeNse (SPIN) web technique, which in situ constructs a peptide
web, trapping IgE against AR. Two candidate SPINs, SPIN-1 and SPIN-2,
are designed with different IgE-binding sequences. The SPIN-1 or SPIN-2
is able to bind to IgE and transform from nanoparticles into entangled
nanofibers. In turn, the web of SPIN-1 or SPIN-2 acts as a long-term
trap of IgE to prevent the IgE from binding to mast cells. SPIN-1
or SPIN-2 (10 mg/kg) is able to treat AR model Balb/c mice with high
efficiency and reduced symptoms of rhinitis and inflammatory factors,
even better than a first-line clinical drug, cetirizine (10 mg/kg).
For example, the amount of IL-4 released in the AR group (185.5 ±
6.8 pg/mL) is significantly reduced after the treatment with SPIN-1
(70.4 ± 14.1 pg/mL), SPIN-2 (86.0 ± 9.3 pg/mL), or cetirizine
(112.8 ± 19.3 pg/mL). More importantly, compared with the cetirizine
group (1 day), the SPIN-1 or SPIN-2 group shows long-term therapeutic
effects (1 week). The SPIN web technique shows the great potential
for blocking IgE binding to mast cells in vivo, attenuating AR or
other allergic reactions.
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