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首页> 美国卫生研究院文献>International Journal of Molecular Sciences >Prodrugs for Skin Delivery of Menahydroquinone-4 an Active Form of Vitamin K2(20) Could Overcome the Photoinstability and Phototoxicity of Vitamin K2(20)
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Prodrugs for Skin Delivery of Menahydroquinone-4 an Active Form of Vitamin K2(20) Could Overcome the Photoinstability and Phototoxicity of Vitamin K2(20)

机译：维生素K2（20）的活性形式Menahydroquinone-4的皮肤递送前药可以克服维生素K2（20）的光不稳定性和光毒性

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摘要

The effective delivery of menahydroquinone-4 (MKH), an active form of menaquinone-4 (MK-4, vitamin K2(20)), to the skin is beneficial in the treatment of various skin pathologies. However, its delivery through the application of MK-4 to the skin is hampered due to the photoinstability and phototoxicity of MK-4. This study aimed to evaluate the potential of ester prodrugs of MKH for its delivery into the skin to avoid the abovementioned issues. The ester prodrugs, MKH 1,4-bis-N,N-dimethylglycinate hydrochloride (MKH-DMG) and MKH 1,4-bis-hemisuccinate (MKH-SUC), were prepared using our previously reported methods. Photostability was determined under artificial sunlight and multi-wavelength light irradiation, phototoxicity was determined by intracellular ROS formation and cell viability of UVA-irradiated human epidermal keratinocyte cells (HaCaT), and delivery of MKH into HaCaT cells was assessed by measuring menaquinone-4 epoxide (MKO) levels. MKH prodrugs showed higher photostability than MK-4. Although MK-4 induced cellular ROS and reduced cell viability after UVA irradiation, MKH prodrugs did not affect either ROS generation or cell viability. MKH prodrugs enhanced intracellular MKO, indicating effective delivery of MKH and subsequent carboxylation activity. In conclusion, these MKH prodrugs show potential for the delivery of MKH into the skin without photoinstability and phototoxicity.
机译：Menaquinone-4（MK-4，维生素K2（20））的活性形式Menahydroquinone-4（MKH）的有效递送对皮肤的各种疾病的治疗是有益的。然而，由于MK-4的光不稳定性和光毒性，其通过将MK-4施用到皮肤上的递送受到阻碍。这项研究旨在评估MKH的酯类前药向皮肤输送以避免上述问题的潜力。酯前药MKH 1,4-双-N，N-二甲基甘氨酸盐酸盐（MKH-DMG）和MKH 1,4-双-半琥珀酸酯（MKH-SUC）是使用我们先前报道的方法制备的。在人造阳光和多波长光照射下确定光稳定性，通过细胞内ROS形成和UVA照射的人表皮角质形成细胞（HaCaT）的细胞生存力来确定光毒性，并通过测量环戊烯酮-4环氧化物评估将MKH递送到HaCaT细胞中（MKO）级别。 MKH前药显示出比MK-4更高的光稳定性。尽管MK-4诱导细胞ROS并在UVA照射后降低细胞活力，但MKH前药既不影响ROS的产生，也不影响细胞活力。 MKH前药增强了细胞内MKO，表明MKH的有效传递和随后的羧化活性。总之，这些MKH前药显示出将MKH输送到皮肤中而没有光不稳定和光毒性的潜力。

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