ArticleOncotarget2016
Octreotide-periplocymarin conjugate prodrug for improving targetability and anti-tumor efficiency: synthesis, in vitro and in vivo evaluation.
Article in Oncotarget, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
13 citing papers in PubMed, 21 citations in OpenAlex.
- SSTR-Mediated Precision Delivery: Overcoming Triptolide's Limitations through Octreotide Conjugation in Pancreatic Cancer Treatment.ACS medicinal chemistry letters · 2025Article
- Mechanisms of action of Fu Fang Gang Liu liquid in treating condyloma acuminatum by network pharmacology and experimental validation.BMC complementary medicine and therapies · 2023Article
- Dual targets of lethal apoptosis and protective autophagy in liver cancer with periplocymarin elicit a limited therapeutic effect.International journal of oncology · 2023Article
- Improving cellular uptake and bioavailability of periplocymarin-linoleic acid prodrug by combining PEGylated liposome.Drug delivery · 2022Article
- The Anti-Inflammatory Effect of a γ-Lactone Isolated from Ostrich Oil ofMolecules (Basel, Switzerland) · 2021Article
- Review
- Periplocymarin Induced Colorectal Cancer Cells ApoptosisFrontiers in oncology · 2021Article
- Cetuximab Conjugated with Octreotide and Entrapped Calcium Alginate-beads for Targeting Somatostatin Receptors.Scientific reports · 2020Article
- Periplocymarin Plays an Efficacious Cardiotonic RoleFrontiers in pharmacology · 2020Article
- Octreotide Conjugates for Tumor Targeting and Imaging.Pharmaceutics · 2019Article
- Enhanced Oral Bioavailability, Anti-Tumor Activity and Hepatoprotective Effect of 6-Shogaol Loaded in a Type of Novel Micelles of Polyethylene Glycol and Linoleic Acid Conjugate.Pharmaceutics · 2019Article
- Anticancer and Immunogenic Properties of Cardiac Glycosides.Molecules (Basel, Switzerland) · 2017Review
- Redox-responsive PEGylated self-assembled prodrug-nanoparticles formed by single disulfide bond bridge periplocymarin-vitamin E conjugate for liver cancer chemotherapy.Drug delivery · 2017Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cardiac glycosides could increase intracellular Ca2+ ion by inhibiting the Na+/K+ATPase to induce apoptosis in many tumor cells. However, narrow therapeutic index, poor tumor selectivity and severe cardiovascular toxicity hinder their applications in cancer treatment. To improve the safety profile and tumor targetablility of cardiac glycosides, we designed octreotide conjugated periplocymarin, a cardiac glycoside isolated from Cortex periplocae. The conjugate showed higher cytotoxicity on MCF-7 cells and HepG2 tumor cells (SSTRs overexpression) but much less toxicity in L-02 normal cells. Tissue distribution studies of the conjugate using H22 tumor model in mice showed higher accumulation in tumor and lower distribution in heart and liver than periplocymarin. Furthermore, in vivo anticancer effects of the conjugate on mice bearing H22 cancer xenografts confirmed enhanced anti-tumor efficacy and decreased systemic toxicity. Altogether, octreotide-conjugated periplocymarin demonstrated tumor selectivity and may be useful as a targeting agent to improve the safety profile of cardiac glycosides for cancer therapy.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.