Graphene Oxide, prepared by the modified Hummer's method, was modified with a series of high polymers (polyethyleneimine, polyethylene glycol, chitosan) and Folic Acid for the delivery of platinum anticancer drugs including Cisplatin, Carboplatin, Oxaliplatin and Eptaplatin. Nanocarriers were successfully prepared and characterized by Fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscope. Measurement of drug loading efficiency showed that these nanocarriers had the ability for effective delivery of the platinum anticancer drugs. The Maximum loading ratios of Cisplatin, Carboplatin, Oxaliplatin and Eptaplatin were 25.72, 161.08, 345.21 and 67.80 μg/mg. Drug release experiments in the acid environment showed that the cumulative release rate of platinum anticancer drugs from nanocarriers was higher than that in the neutral environment. The cumulative release of all three nanocarriers in the acid environment reached above 60%. In vitro cytotoxicity assay showed that those nanocarriers had a low toxicity. The cell viability rates were above 80% for all three nanocarriers. Investigation of the anticancer activity in vitro showed that those drug delivery systems had the ability to inhibit the growth of the SKOV3 cell line. These results showed that those nanocarriers were suitable for the delivery of platinum anticancer drugs. Providing preliminary advice on the potential application of the combination of platinum anticancer drugs and the functionalized Graphene Oxide nanocarriers.

11 May 2021·LangmuirQ2 · CHEMISTRY

Supramolecular Chemotherapy: Host–Guest Complexes of Heptaplatin-Cucurbit[7]uril toward Colorectal Normal and Tumor Cells

Q2 · CHEMISTRY

Article

Author: Jiao, Rong ; Qin, Changfu ; Xu, Lixin ; Chen, Yueyue ; Huang, Xin ; Zhou, Hang ; Liu, Hanrui

Supramolecular chemotherapy is a strategy that is currently used to improve the therapeutic efficacy of traditional chemotherapy while mitigating side effects. Heptaplatin, a platinum chemotherapeutic antitumor drug in colorectal tumors, is traditionally used in the clinic. However, its side effects and low efficiency in killing tumors remain unresolved. Herein, a facile supramolecular chemotherapy platform on account of the host-guest chemistry between cucurbit[7]uril and the commercially available heptaplatin was studied. At pH 7.4, heptaplatin showed a strong binding to the cucurbit[7]uril nanocarrier by ¹H NMR, whose K_a was (1.38 ± 0.06) × 10⁶ M^-1 by isothermal titration calorimetry (ITC). At pH 6.0 in a tumor microenvironment, overexpressed spermine can exchange competitively heptaplatin from heptaplatin-CB[7]. This supramolecular complex achieved higher antitumor activity on colorectal tumor cells and lower cytotoxicity than the drug alone on colorectal normal cells. Furthermore, the antitumor mechanisms of supramolecular complex were investigated by apoptosis, cell cycle, and spermine synthase. It was found that heptaplatin-CB[7] consumed more colorectal tumorous intracellular spermine by the spermine synthase assay (413.85 ± 0.004 pg/mL); hepataplatin-CB[7] caused early apoptosis (87.73%) of colorectal tumor cells; heptaplatin-CB[7] induced an inhibitory response in the G₁ phase of the tumor cell cycle. These findings demonstrated that heptaplatin-CB[7] had higher antitumor activity toward human colorectal tumor cells but lower cytotoxicity toward human colorectal normal cells. It is expected to promote the supramolecular chemotherapy and translational development of the nanocomplex into the clinical field.

30 Aug 2018·The Journal of Physical Chemistry AQ3 · CHEMISTRY

Raman and Infrared Studies of Platinum-Based Drugs: Cisplatin, Carboplatin, Oxaliplatin, Nedaplatin, and Heptaplatin

Q3 · CHEMISTRY

Article

Author: Nguyen, Trang ; Mirsaleh-Kohan, Nasrin ; DeYonker, Nathan J. ; Torres, Marjorie ; Morris, Tyree J. ; Khan, Sidrah ; Rostovtsev, Yuri V. ; Lozano, Hannah C. ; Duplanty, Michael

This study reports the optimized structures and lowest-energy conformations/stereochemistry of five currently used platinum-based drugs: cisplatin, carboplatin, nedaplatin, oxaliplatin, and heptaplatin. Normal Raman and IR spectra of each drug are experimentally obtained and have been compared to various levels of density functional theory (DFT). Although some combination of structure, reactivity, or spectroscopy for these drugs has been studied by various groups, there are no known experimental normal Raman and IR spectra for nedaplatin, oxaliplatin, and heptaplatin in the literature. The detailed structural and vibration findings of these drugs are very important to understanding platinum behavior and drug dynamics. The following work explores the vibrational frequencies of these drugs particularly by focusing on the low-energy modes between 200 and 600 cm^-1, where anharmonicity effects will have less influence on the accuracy of computed frequencies. Ideally, the Pt-N stretching modes provide vibrational diagnostics for each drug. Interestingly, a vibrational energy decomposition analysis (VEDA) suggests that oxaliplatin and heptaplatin Pt-N stretching modes are not Raman or IR active. Instead, C-C and Pt-O stretching frequencies in the various bidentate dioxo ligands might be more useful in characterizing new cisplatin derivatives. Analysis of anharmonicity effects was compared against (and in tandem with) dimer computations of four of the five drugs. Harmonic vibrational computations of the dimeric cisplatin derivatives provided greater qualitative improvement than that of the monomeric derivatives. Satisfying agreement with experimental Raman spectra was obtained, even without resorting to linear scale factors for the harmonic dimer frequencies.

100 Deals associated with Eptaplatin

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KEGG	Wiki	ATC	Drug Bank
-	-	L01XA	-

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Indication	Country/Location	Organization	Date
Neoplasms	KR	SK-Pharma, Inc.	14 Nov 1999
Head and Neck Neoplasms	KR	SK Chemicals Co. Ltd.	01 Jul 1999
Lung Cancer	KR	SK Chemicals Co. Ltd.	01 Jul 1999
Uterine Cervical Cancer	KR	SK Chemicals Co. Ltd.	01 Jul 1999

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2005	Phase 1	Advanced Malignant Solid Neoplasm	30	Heptaplatin	(rofowbwsye) = G3 proteinuria unqidzbsel (rbwwysbavw )	-	01 Jun 2005
ASCO2005	Phase 1/2	Advanced Head and Neck Carcinoma	-	Heptaplatin and 5-FU combination treatment	(rtkonkpawf) = xxfvvsstrr kxmmmmrijh (bjosqhdufh ) View more	-	01 Jun 2005
ASCO2004	Phase 1	Advanced Malignant Solid Neoplasm	15	Heptaplatin	(zpghmalppv) = myelosuppression and hepatotoxicity gxmpvgkaan (fjalgnfgtp )	-	15 Jul 2004

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