跳至主要内容

Targeting the leptin receptor: To evaluate therapeutic efficacy and anti-tumor effects of Doxil, in vitro and in vivo in mice bearing C26 colon carcinoma tumor

Author：Shahrzad Amiri Darban, Sara Nikoofal-Sahlabadi, Nafise Amiri, Nafiseh Kiamanesh, Amin Mehrabian, Bamdad Zendehbad, Zahra Gholizadeh, Mahmoud Reza Jaafari   《Colloids and Surfaces B: Biointerfaces》

ABSTRACTS
Leptin is an appetite regulatory hormone that is secreted into the blood circulation by the adipose tissue and it functions via its over expressed receptors (Ob-R) in a wide variety of cancers. In the present study, the function of a leptin-derived peptide (LP16, 91–110 of Leptin) was investigated as a targeting ligand to decorate PEGylated liposomal doxorubicin (PLD, Doxil?) surface and the anti-tumor activity and therapeutic efficacy of Doxil in C26 (Colon Carcinoma) tumor model were also evaluated. As a result of this, Doxil with different LP16 peptide density (25, 50, 100 and 200 peptide on the surface of each liposome) was successfully prepared and characterized. In vitro results showed significant enhanced cytotoxicity and cellular binding and uptake of LP16-targeted Doxil formulations (LP16-Doxil) in C26 cells as compared to Doxil. In BALB/c mice bearing C26 murine carcinoma, at a dose of 15?mg/kg, LP16-Doxil groups (100 ligand) significantly suppressed the growth of the tumor and showed higher inclination to tumor as compared to non-targeted Doxil. This study revealed that the potential of LP16 peptide targeting increased the therapeutic efficacy of Doxil and highlighted the importance of optimizing the ligand density to maximize the targeting ability of the nanocarriers and merits further investigations.

Graphical abstract



KEY WORDS
Doxil; Targeting ligand; Leptin; LP16 peptide
SCREENSHOT

RELATED PRODUCTS
SRNVIQISNDLENLRDLLHVGGGC-Ac, >95% pure by HPLC and mass spectrographic analyses was purchased from China Peptides Co. (Shanghai, China).
CHAINING
https://www.sciencedirect.com/science/article/pii/S0927776518300419

标签

标签：

评论

发表评论

此博客中的热门博文

Mitochondria Targeted Peptide Attenuates Mitochondrial Dysfunction, Controls Inflammation and Protects Against Spinal Cord Injury-Induced Lung Injury

文献作者：Zhu L.-L. · Li M.-Q. · He F. · Zhou S.-B. · Jiang W.     《Cellular Physiology and Biochemistry》 ABSTRACTS Background/Aims:   Spinal cord injury (SCI) is a common and devastating disease, which results in systemic inflammatory response syndrome and secondary lung injury. Mitochondrial dysfunction and inflammation are closely related to lung injury in diverse disease models. No studies have demonstrated the effects of mitochondrial targeted peptide SS-31 in a mouse model of SCI-induced lung injury.  Methods:   Immediately after injury, mice in the treatment groups received a daily, single-dose intraperitoneal injection of SS-31 and for the next 2 days. The sham and SCI groups also received a daily single dose of vehicle (DMSO and 0.9% NaCl, 1: 3). The lung tissue of mice was examined after SCI, and tissue damage, apoptosis, inflammation, and mitochondrial dysfunction were recorded.  Results:   SS-31 treatment attenuated lung edema ...
发表评论
阅读全文

CAS:843782-19-4|Neuromedin S (rat)|LPRLLHTDSRMATIDFPKKDPTTSLGRPFFLFRPRN-NH2

Contact： Liven Qian(钱叶华)-Custom Peptide Mobile: 13761298676（微信） Email：cps037@chinapeptides.net QQ：2880526724 ChinaPeptides Co., Ltd./强耀生物科技有限公司 Name Neuromedin S (rat) Code [843782-19-4] The alias Neuromedin S (rat) Sequence (single letter abbreviation) LPRLLHTDSRMATIDFPKKDPTTS LGRPFFLFRPRN-NH2 Sequence (three-letter abbreviation) H-Leu-Pro-Arg-Leu-Leu-His-Thr-Asp-Ser-Arg-Met-Ala-Thr-Ile-Asp-Phe-Pro-Lys-Lys-Asp-Pro-Thr-Thr-Ser-Leu-Gly-Arg-Pro-Phe-Phe-Leu-Phe-Arg-Pro-Arg-Asn-NH2?(trifluoroacetate salt) A basic description Neuropeptide widely distributed in the gut and central nervous system that induces uterine contractile activity and may be a physiology regulator of food intake. IC50 values for the binding of neuromedin U-25 (human) to the human neuromedin U receptors NMU1R and NMU2R are 2.7nM and 1.8nM, respectively. solubility The molecular weight 4241.98 Chemical formula C193H307N57O49S1 The purity 80%，90%，95%，98%，99% Weight 1mg,5mg,10mg,50mg,100mg,1g Storage co...
发表评论
阅读全文

CAS:198483-36-2|Cholecystokinin Octapeptide (1-6) (desulfated)|DYMGWM

Contact： Liven Qian(钱叶华)-Custom Peptide Mobile: 13761298676（微信） Email：cps037@chinapeptides.net QQ：2880526724 ChinaPeptides Co., Ltd./强耀生物科技有限公司 Name Cholecystokinin Octapeptide (1-6) (desulfated) Code [198483-36-2] The alias Cholecystokinin Octapeptide (1-6) (desulfated) Sequence (single letter abbreviation) DYMGWM Sequence (three-letter abbreviation) Asp-Tyr-Met-Gly-Trp-Met A basic description solubility The molecular weight 801.94 Chemical formula C36H47N7O10S2 The purity 80%，90%，95%，98%，99% Weight 1mg,5mg,10mg,50mg,100mg,1g Storage conditions Store at -20°C. Keep tightly closed. Store in a cool dry place.
发表评论
阅读全文