A new invertebrate NPY-like polypeptide, ZoaNPY, from the Zoanthus sociatus, as a novel ligand of human NPY Y2 receptor rescues vascular insufficiency via PLC/PKC and Src- FAK-dependent signaling pathways.

Our recent multi-omics studies have revealed rich sources of novel bioactive proteins and polypeptides from marine organisms including cnidarians. In the present study, we initially conducted a transcriptomic analysis to review the composition profile of polypeptides from Zoanthus sociatus. Then, a newly discovered NPY-like polypeptide-ZoaNPY was selected for further in silico structural, binding and virtually pharmacological studies.

6-benzylaminopurine causes endothelial dysfunctions to human umbilical vein endothelial cells and exacerbates atorvastatin-induced cerebral hemorrhage in zebrafish.

6-benzylaminopurine (6-BA), a multifunctional plant growth regulator, which is frequently used worldwide to improve qualities of various crops, is an important ingredient in production of "toxic bean sprouts." Although there is no direct evidence of adverse effects, its hazardous effects, as well as joint toxicity with other chemicals, have received particular attention and aroused furious debate between proponents and environmental regulators. By use of human umbilical vein endothelial cells (HUVECs), adverse effects of 6-BA to human-derived cells were first demonstrated in this study.

6-Benzylaminopurine causes lipid dyshomeostasis via disruption of glycerophospholipid metabolism in zebrafish.

6-Benzylaminopurine (6-BA) is ubiquitous in agricultural production and is accessible to humans through diets. The modulation of lipid metabolism by 6-BA has been previously demonstrated in plants and oleaginous microorganisms. Therefore, whether it alters lipid homeostasis in other living organisms requires further investigation.

Role of endocrine disruption in toxicity of 6-benzylaminopurine (6-BA) to early-life stages of Zebrafish.

6-benzylaminopurine (6-BA), classified as a "plant hormone", is an important ingredient in production of "toxic bean sprouts". Although there is no direct evidence of adverse effects, its hazardous effects have received some attention and aroused furious debate between proponents and environmental regulators. In this study, potential adverse effects of 6-BA were investigated by exposing zebrafish in vivo to 0.

Toxic Peptide From Acting on the TRPV1 Channel Prevents Pentylenetetrazol-Induced Epilepsy in Zebrafish Larvae.

PcActx peptide, identified from the transcriptome of zoantharian was clustered into the phylogeny of analgesic polypeptides from sea anemone (known as APHC peptides). APHC peptides were considered as inhibitors of transient receptor potential cation channel subfamily V member 1 (TRPV1). TRPV1 is a calcium-permeable channel expressed in epileptic brain areas, serving as a potential target for preventing epileptic seizures.

Crocetin and Its Glycoside Crocin, Two Bioactive Constituents From L. (Saffron), Differentially Inhibit Angiogenesis by Inhibiting Endothelial Cytoskeleton Organization and Cell Migration Through VEGFR2/SRC/FAK and VEGFR2/MEK/ERK Signaling Pathways.

Crocetin and crocin are two important carotenoids isolated from saffron ( L.), which have been used as natural biomedicines with beneficial effects for improving the suboptimal health status associated with abnormal angiogenesis. However, the anti-angiogenic effects and underlying mechanisms of the effects of crocetin and crocin have not been investigated and compared.

Forchlorfenuron (CPPU) causes disorganization of the cytoskeleton and dysfunction of human umbilical vein endothelial cells, and abnormal vascular development in zebrafish embryos.

Forchlorfenuron (CPPU) has been used worldwide, to boost size and improve quality of various agricultural products. CPPU and its metabolites are persistent and have been detected frequently in fruits, water, sediments, and organisms in aquatic systems. Although the public became aware of CPPU through the exploding watermelon scandal of 2011 in Zhenjiang, China, little was known of its potential effects on the environment and wildlife.

Screening of Xanthones from Identified Oliganthin H as a Novel Natural Inhibitor of Convulsions.

Epilepsy is a chronic neurological disorder, characterized by recurrent, spontaneous, and transient seizures, and affects more than 70 million people worldwide. Although two dozen antiepileptic drugs (AEDs) are approved and available in the market, seizures remain poorly controlled in one-third of epileptic patients who are suffering from drug resistance or various adverse effects. Recently, the xanthone skeleton has been regarded as an attractive scaffold for the discovery and development of emerging anticonvulsants.

Cardiotoxicity of forchlorfenuron (CPPU) in zebrafish (Danio rerio) and H9c2 cardiomyocytes.

Forchlorfenuron (CPPU), as a plant growth regulator or herbicide/pesticide, is widely used in agriculture worldwide. It is adopted by most farmers due to its high efficacy for boosting size and improving the quality of fruit. However, CPPU was implicated in, and gained notoriety due to an incident of exploding watermelon that occurred in 2011.

Combined transcriptomic and proteomic analysis reveals a diversity of venom-related and toxin-like peptides expressed in the mat anemone Zoanthus natalensis (Cnidaria, Hexacorallia).

Venoms from marine animals have been recognized as a new emerging source of peptide-based therapeutics. Several peptide toxins from sea anemone have been investigated as therapeutic leads or pharmacological tools. Venom complexity should be further highlighted using combined strategies of large-scale sequencing and data analysis which integrated transcriptomics and proteomics to elucidate new proteins or peptides to be compared among species.

A new isoflavone with anti-inflammatory effect from the seeds of .

A new isoflavone, milletenol A (), along with four known flavonoids (-) were isolated from the seeds of . The structure of was established by extensive spectroscopic methods while known compounds were identified by comparisons with literature data. Compound and showed significant anti-inflammatory activities against nitric oxide production in LPS-induced RAW264.

EH-42: A Novel Small Molecule Induces Apoptosis and Inhibits Migration and Invasion of Human Hepatoma Cells through Suppressing STAT3 Signaling Pathway.

Background: Since signal transducer and activator of transcription 3 (STAT3) is aberrantly activated in hepatocellular carcinoma (HCC) and plays a key role in this tumor progression. Inhibition of the STAT3 signaling pathway has been considered as an effective therapeutic strategy for suppressing HCC development.

Objective: In this study, we investigated the anti-cancer effects of EH-42 on HCC cells and tried to explain the underlying mechanism.

Anti-angiogenic and anticancer effects of baicalein derivatives based on transgenic zebrafish model.

Angiogenesis leads to tumor neovascularization by promoting tumor growth and metastatic spread, therefore, angiogenesis is considered as an attractive target for potential small molecule anticancer drug discovery. Herein, we report the structural modification and biological evaluation of baicalein derivatives, among which compound 42 had potent in vivo anti-angiogenic activity and wide security treatment window in transgenic zebrafish model. Further, 42 exhibited the most potent inhibitory activity on HUVEC proliferation, migration and tube formation in vitro.

A Novel ShK-Like Toxic Peptide from the Transcriptome of the Cnidarian Displays Neuroprotection and Cardioprotection in Zebrafish.

(class Anthozoa) is a zoantharian which, together with other cnidarians, like jellyfishes, hydra, and sea anemones, possesses specialized structures in its tissues, the cnidocytes, which deliver an array of toxins in order to capture prey and deter predators. The whole transcriptome of was deep sequenced, and a diversity of toxin-related peptide sequences were identified, and some retrieved for functional analysis. In this work, a peptide precursor containing a ShK domain, named PcShK3, was analyzed by means of computational processing, comprising structural phylogenetic analysis, model prediction, and dynamics simulation of peptide-receptor interaction.

Rhodol Derivatives as Selective Fluorescent Probes for the Detection of Hg Ions and the Bioimaging of Hypochlorous Acid.

Two sensors, with a spirolactone group and with a spirolactam group containing a phenyl isothiocyanate moiety, based on rhodol, were designed and synthesized in order to obtain materials with excellent optical properties for the detection of environmentally and biologically important Hg and hypochlorous acid (HClO) ions. The crystal structure of revealed two moieties, a rhodamine-like portion with a spirolactone and a fluorescein-like portion without a spirolactone. In the absence of analyte, produced an optical output with a maximum absorption and emission at 475 and 570 nm, respectively, which was attributed to the fluorescein-like moiety without a spirolactone.

Rhodol Derivatives as Selective Fluorescent Probes for the Detection of Hg Ions and the Bioimaging of Hypochlorous Acid.

Invited for this month's cover picture is the group of Professor Keith Man-Chung Wong from the Southern University of Science and Technology (P.R. China).

In vivo toxic effects of 4-methoxy-5-hydroxy-canthin-6-one in zebrafish embryos via copper dyshomeostasis and oxidative stress.

Dysfunction of copper homeostasis can lead to a host of disorders, which might be toxic sometimes. 4-Methoxy-5-hydroxy-canthin-6-one (CAN) is one of the major constituents from Picrasma quassioides and responsible for its therapeutic effects. In this work, we evaluated the toxic effect of CAN (7.

pH-Responsive prodrug nanoparticles based on a sodium alginate derivative for selective co-release of doxorubicin and curcumin into tumor cells.

In order to realize a combination of chemotherapy and selective drug release into tumor cells, novel pH-sensitive prodrugnanoparticles were designed and prepared via the self-assembly of a synthetic amphiphilic macromolecular prodrug for the selective co-delivery of doxorubicin (Dox) and curcumin (Cur). Dox was covalently conjugated to the oxidized sodium alginate through a Schiff base reaction to produce an amphiphilic macromolecular prodrug, and the prodrug was subsequently self-assembled into nanoparticles (Dox-NPs) in an aqueous solution, which were responsive to the acidic environment in tumor cells. Additionally, a second chemotherapeutic agent, Cur, was encapsulated in the core of nanoparticles (Cur-Dox-NPs) via hydrophobic effects, with a significant drug loading capacity.