천연 젖산 탈수소 효소(LDH) 억제제-2021

https://www.sciencedirect.com/science/article/abs/pii/S0021967321006786?dgcid=rss_sd_all 

Screening of lactate dehydrogenase inhibitor from bioactive compounds in natural products by electrophoretically mediated microa

Screening of lactate dehydrogenase inhibitor from bioactive compounds in natural products by electrophoretically mediated microanalysis

 

 

Abstract

젖산 탈수소효소(LDH)는 해당 작용의 핵심 효소로, 다양한 암 유형에서 LDH의 발현이 증가하여 종양 침입과 전이를 촉진할 수 있다고 보고되었습니다.

따라서 LDH는 암의 새로운 치료 표적으로 떠오르고 있습니다.

알려진 양성 억제제인 고시폴의 반 최대 억제 농도(IC50)는 9.269 μM으로 기존 문헌과 비슷한 수준으로 측정되었습니다.

그런 다음 개발된 방법을 사용하여 천연물에서 추출한 12가지 생리활성 화합물의 LDH에 대한 억제 활성을 조사했습니다.

케르세틴, 루테올린, 우르솔산 등 세 가지 화합물이 LDH에 대한 잠재적 억제 효과를 나타냈습니다. 

 

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https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3903096/

High-Throughput Screening to Identify Plant Derived Human LDH-A Inhibitors

 

High-Throughput Screening to Identify Plant Derived Human LDH-A Inhibitors

1-10위 까지만

1 - Wu Bei Zi Melaphis chinensis gallnut 0.00009 0.09-붉나무, 오배자
4 - Babul Chall Bark Acacia arabica 0.00075 0.75-아라비아 아카시아?
2 - Bladderwrack Fucus vesiculosus 0.00100 1.00-후코이단?
3 - Kelp Powder Laminaria Japonica 0.00134 1.34-다시마
5 - Bayberry Root bark Morella cerifera 0.00158 1.58
6 - CraneSbill Root Geranium maculatum 0.00173 1.73
7 - Arjun Terminalia arjuna 0.00183 1.83
8 - Ye Jiao Ten Polygonum multiflorum vine 0.00288 2.88
9 - Mu Dan Pi Paeonia suffructicose root - bark 0.00298 2.98
10 - Witch Hazel Root Hamamelis virginiana 0.00321 3.21

 

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https://onlinelibrary.wiley.com/doi/10.1002/cam4.1820

Lactate dehydrogenase A: A key player in carcinogenesis and potential target in cancer therapy

4 LDHA IN CANCER BIOLOGY

In cancers, enhanced LDHA promotes diverse malignant bio-characteristics. (Figure 2).

 

Figure 2

 

LDHA plays critical roles in hallmarks of cancer.

LDHA is closely related to malignant bio-characteristics of cancer via various mechanisms.

LDHA can promote cancer cell proliferation and maintain cell survival;

LDHA helps enhance cancer cell invasion and metastasis;

LDHA can also trigger angiogenesis;

LDHA can assist cancer cells in immune escape. ATP, adenosine triphosphate;

CSCs, cancer stem cells;

EMT, epithelial-to-mesenchymal;

IL-8, interleukin-8;

MDSCs, myeloid-derived suppressor cells;

ROS, reactive oxygen species; VEGF, vascular endothelial growth factor

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