Novel targeted lysosome ruthenium photocatalyst as well as preparation method and application thereof

A technology of photocatalysts and lysosomes, applied in the field of medicine, can solve problems such as the decline in the quality of life of patients and achieve high curative effect

Active Publication Date: 2021-03-12
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AI-Extracted Technical Summary

Problems solved by technology

[0003] Radiation therapy and chemical drug therapy are clinically commonly used tumor treatment methods, but while achieving therapeutic effects, radiotherapy and chemotherapy often cause varying degrees of toxic a...
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The invention relates to the field of medicine, in particular to a novel targeted lysosome ruthenium photocatalyst as well as a preparation method and application thereof. The novel targeted lysosomeruthenium photocatalyst has a high curative effect when applied to photodynamic therapy of liver cancer (HepG2 cells), can target lysosome in cells, has a photocatalytic oxidation effect on NADH and amino acid, is of great significance to research of efficient and low-toxicity ruthenium complex photosensitizers, and lays experimental and theoretical foundations for clinical development of novel metal antitumor drugs. The metal ruthenium (II) complex has no toxicity (IC50>100 [mu] M) to human liver cancer cell strains in the absence of illumination, but has very strong growth inhibition ability(IC50 = 0.51 [mu] M) to the human liver cancer cell strains under illumination, can target lysosome, and has photocatalytic oxidation ability to NADH in cancer cells.

Application Domain

Ruthenium organic compoundsPhotodynamic therapy +2

Technology Topic

PhotosensPhoto catalysis +13


  • Novel targeted lysosome ruthenium photocatalyst as well as preparation method and application thereof
  • Novel targeted lysosome ruthenium photocatalyst as well as preparation method and application thereof
  • Novel targeted lysosome ruthenium photocatalyst as well as preparation method and application thereof


  • Experimental program(6)

Example Embodiment

[0031] Example 1
[0032] A new type of targeting lysosomal catalyst, which is structurally in formula (I):
[0034] Preparation method of compound of formula (I):
[0035] Double (2,2'-dipyridine) dichloride (II) dihydrate (0.0520 g, 0.1 mmol) and 4,4'-diphenyl-2,2'-bond pyridine (0.0308 g, 0.1) Mmol) The mixture was heated to 80 ° C in ethanol (20 mL), and the reaction was reduced to room temperature after 24 hours, and the precipitates were washed with ethanol, and the orange red solid was obtained after drying in vacuo. The obtained crude product was purified by neutral alumina column chromatography (solvent: methanol / dichloromethane = 1/99), and was recrystallized by dichloromethane / diethyl ether to obtain an orange red crystal ruthenium (II) complex (0.0619 g, 0.078 mmol), yield 78%. By mass spectrometry and nuclear magnetic flaps, its molecular formula is C 42 Hide 32 CL 2 N 6 Ru, ESI-MS [CH3OH, M / Z]: 361 [M-2CL] 2+. 1 H NMR (400MHz, DMSO) 9.37 (D, J = 1.6Hz, 2H), 8.91 (D, J = 8.1 Hz, 4H), 8.20 (D, J = 1.7 Hz, 4H), 8.08 (D, J = 7.0 Hz, 4H), 7.92-7.86 (m, 4H), 7.77 (T, J = 6.2 Hz, 4H), 7.65-7.56 (m, 10h).
[0036] Reaction flowchart:

Example Embodiment

[0038] Experimental Example 1
[0039] Test the light stability of the compound of formula (I) obtained by the example
[0040] The luminescent quartz-containing tank of the PBS solution containing the ruthenium complex (10 m) was placed at 465 nm light source to radiate for 5 min (the optical dose was 11.7 J / cm) 2), Detect the absorbance of the solution. Effects of ruthenium (II) complex under 465 nm light radiation figure 2 As shown, the uviol (II) complex is substantially no change in ultraviolet-visible absorption map before and after photoelectric radiation, and the visible ruthenium (II) complex has strong light stability.

Example Embodiment

[0041] Experiment 2
[0042] The ability of ruthenium (II) complex light catalyzed NADH
[0043] Due to the photocatalysis, the metal complex can oxidize the reduced coenzyme I (NADH) into its oxidation state (NAD) + ), Thus containing ruthenium complex (2M) and NADH (A 339nm = 1.5) The luminescent quartz band is placed at 465 nm light source radiation 5min (11.7J / cm) 2 ), Detect the absorbance of the solution. Effect of ruthenium (II) complex on NADH oxidation under 465 nm light radiation image 3 As shown, the ruthenium (II) complex is photocatalytic oxidation capability for NADH.


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