Antitumor and Antibacterial Derivatives of Oridonin: A Main Composition of Dong-Ling-Cao

Abstract

Isodon rubescens has been used as a traditional green tea for more than 1000 years and many medicinal functions of I. rubescens are also very useful, such as its well-known antitumor and antibacterial activities. Oridonin, a bioactive ent-kaurane diterpenoid, is the major ingredient of this medicinal tea. Herein, 22 novel oridonin derivatives were designed and synthesized. The antibacterial activity was evaluated for the first time. Compound 12 was the most promising one with MIC of 2.0 µg/mL against B. subtilis, which was nearly 3-fold stronger than positive control chloromycetin. The antiproliferative property was also assayed and compound 19 showed stronger activity than taxol. The apoptosis-inducing ability, cell cycle arrest effect at S phase and influence of mitochondrial membrane potential by 19 in CaEs-17 cancer cells were first disclosed. Based on the above results, the cell apoptosis induced by compound 19 in CaEs-17 cells was most probably involved in the intrinsic apoptotic pathway.

Structural characterization of Momordica charantia L. (Cucurbitaceae) oligopeptides and the detection of their capability in non-small cell lung cancer A549 cells: induction of apoptosis

“…27 Previous studies have reported that the collapse of Dj m is correlated to the events of the apoptotic process. 28 The apoptotic changes of mitochondria include Dj m loss, transient swelling of the mitochondrial matrix, mechanical rupture of the membrane and/or its nonspecic permeabilization by giant protein permeant pores, and release of soluble intermembrane proteins through the outer membrane. 29 When the concentration of ROS and oxygen stress reach a certain level, the mitochondrial membrane permeability will be changed, resulting in the release of apoptosis factors.…”

The antibacterial mechanism of oridonin against methicillin-resistant Staphylococcus aureus (MRSA)

“…In modern medicine, oridonin is known for its potent antimicrobial, antioxidative, anti-inflammatory and pharmacological activities (Weiyan et al 2017). Oridonin was shown to inhibit the growth of several bacteria, including Salmonella typhi, Streptococcus pneumonia, Shigella castellani and S. aureus (Li et al 2016). In addition, a pilot experiment revealed the antibacterial activity of oridonin against MRSA.…”

NLRP1 and NLRP3 inflammasomes as a new approach to skin carcinogenesis (Review)

“…Great hope for revolutions in treatment rest on oridonin (ORI), one of the most important active Chinese medicinal components isolated from Rabdosia rubescens, which has been shown to be a potent anti-metastatic agent. Notably, oridonin shows a broad-spectrum of anti-proliferative and anti-cancer activities in various types of tumor (63)(64)(65)(66)(67)(68) as well as in melanoma (69,70). Wang et al (69) indicated that ORI induces human melanoma A375-S2 cell death (69).…”

“…As the mechanisms underlying the inhibiting effects of ORI in the metastasis of melanoma cells remain unclear, many authors have investigated this topic. Li et al (63,64) proposed that ORI could effectively inhibit migration as well as invasion and adhesion by inhibiting epithelial-mesenchymal transition (EMT) in melanoma cells through inhibiting the phosphorylation of phosphoiniositide-3 kinase (PI3K), Protein kinase B (Akt), and glycogen synthase kinase 3β (GSK-3β) in the presence of transforming growth factor β1 (TGF-β1). Recent studies have also indicated that oridonin is a specific inhibitor for the NLRP3 inflammasome which forms a covalent bond with the NACHT domain of NLRP3, thereby inhibiting NLRP3 inflammasome assembly and activation (71).…”