Akt modulators(Proto-oncogene proteins c-akt modulators), NLRP3 inhibitors(NACHT, LRR and PYD domains-containing protein 3 inhibitors), PI3K family modulators(Phosphatidylinositol 3-kinase family modulators)

Therapeutic Areas

NeoplasmsImmune System DiseasesDigestive System Disorders+ [2]

Active Indication

Colitis, UlcerativeInflammationBreast Cancer

Inactive Indication-

Originator Organization

University of Science & Technology of China

Active Organization

University of Texas Medical Branch

Tianjin University of Traditional Chinese Medicine

University of Science & Technology of China

Inactive Organization

Second Affiliated Hospital of Soochow University

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC20H28O6

InChIKeySDHTXBWLVGWJFT-NACUCOKYSA-N

CAS Registry28957-04-2

100 Clinical Results associated with Oridonin

100 Translational Medicine associated with Oridonin

100 Patents (Medical) associated with Oridonin

758

Literatures (Medical) associated with Oridonin

01 Feb 2026·MOLECULAR IMMUNOLOGY

An H₂S-releasing oridonin derivative protects HaCaT cells against metabolic stress via PI3K/AKT/Nrf2 signaling

Article

Author: Xue, Rubing ; Lin, Lang ; Jia, Yuzhen ; Chu, Chun ; Shi, Yutong ; Xu, Fanxing ; Li, Dahong

The chronic hyperglycemia and its-associated metabolic changes often lead to impaired wound healing, which seriously affects the quality of life of diabetic patients. Oxidative stress and apoptosis are key factors that impede epidermal cell proliferation and migration and delay wound healing. The aim of this study was to investigate the protective effect of a novel hydrogen sulfide (H₂S)-releasing oridonin derivative (OAc-Ph-ADT) on epidermal HaCaT cells against a high-glucose and high-fat environment in vitro. Mechanistic studies showed that OAc-Ph-ADT exerted its antioxidant effects by activating the PI3K/AKT/Nrf2 signaling pathway. Specifically, it increased PI3K and phosphorylated-AKT expression, and promotes Nrf2 nuclear translocation, which in turn enhances the mRNA and protein expression of downstream antioxidant factors (HO-1, SOD2 and NQO1). In addition, OAc-Ph-ADT significantly reduced apoptosis by inhibiting the decrease in mitochondrial membrane potential and decreasing the expression of apoptosis-related proteins (Bax, Cleaved-Caspase 3/9). It was also observed that OAc-Ph-ADT up-regulated the expression of cystathionine β-synthase (CBS) via Nrf2, which further promoted the synthesis of endogenous H₂S, resulting in positive feedback regulation. In summary, this paper elucidated through systematic in vitro experiments that OAc-Ph-ADT has a protective effect against epidermal cell damage in a high-glucose and high-fat environment, revealing its potential as a candidate molecule for diabetic wound treatment, and this novel H₂S-releasing oridonin derivative has a potential application as a diabetic wound healing promoter.

01 Feb 2026·Translational Oncology

Mechanistic and translational insights into plant-derived natural products in preclinical multiple myeloma research: Current evidence

Review

Author: Li, Lulu ; Li, Changnian ; Yu, Liming ; Gu, Jiabao ; Cui, Siyuan ; Xu, Jie ; Shi, Jingbo ; Wang, Yaru

Multiple myeloma (MM) is a hematological malignancy characterized by the clonal proliferation of abnormal plasma cells, with marked heterogeneity and therapeutic refractoriness. Despite the introduction of proteasome inhibitors (PIs), immunomodulatory drugs (IMiDs), monoclonal antibodies (mAbs), and chimeric antigen receptor T-cell (CAR-T) therapy, relapse and drug resistance remain major challenges that urgently need to be addressed. Plant-derived natural products have attracted increasing attention in recent years due to their multi-target synergistic effects, demonstrating unique potential in inducing MM cell apoptosis, reversing drug resistance, and modulating the immune microenvironment-making them a rising focus in translational medicine research. In this structured narrative review, we systematically summarize the anti-myeloma mechanisms of fourteen plant-derived natural products, including plant-derived monomeric compounds (baicalein, artemisinin, curcumin, celastrol, gambogic acid, resveratrol, ginsenosides, icariin, oridonin, plumbagin, formononetin) and standardized plant extracts (Strychnos nux-vomica root extract, dandelion flavonoids, Hedyotis diffusa polysaccharides). This review highlights their multi-target regulatory effects on signaling pathways, cell cycle modulation, and immune regulation, and further discusses their potential translational value in overcoming drug resistance and optimizing combination treatment strategies. Literature was retrieved from PubMed, Web of Science, and CNKI databases, covering studies published up to January 2025. Although plant-derived natural products exhibit promising multi-target regulatory mechanisms in MM therapy, their clinical translation remains limited by poor bioavailability of single compounds and the lack of standardized extracts. Future research should integrate systems pharmacology with clinical studies to elucidate multi-component synergistic networks and develop novel targeted formulations, thereby accelerating the efficient translation of phytochemicals from bench to bedside.

01 Feb 2026·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Effect of stereochemistry at position C14 on the antiproliferative activity and selectivity of simplified oridonin O-acylated derivatives

Article

Author: Gao, Feng ; Song, Junying ; Xu, Jinbu ; Li, Xiaohuan ; Xie, Luyao ; He, Zhengyang ; Tan, Jiao ; Tian, Ailing

Oridonin is an ent-kaurane diterpenoid with broader antitumor properties. Much efforts have been devoted to develop methods for rational chemical modification of oridonin to obtain synthetic derivatives with higher anticancer activity than the native structure. However, no study has examined the effect of stereochemistry on antiproliferative activity of oridonin and its derivatives thus far. In this study, a novel oridonin analogue with C14α-OH (6) was first synthesized via a Retro-Aldol-Aldol cascade reaction based on a configuration inversion strategy. Its structure was unambiguously confirmed by single-crystal X-ray diffraction analysis. The C14α-OH analogue (6), along with its native counterpart 2 (C14β-OH), was transformed into a series of forty-six C14-O-acylated products (6a-6w and 2a-2w). In vitro antiproliferative activities screening revealed that the α-configured derivative 6 (IC₅₀ = 0.53 μM) exhibited 1.7-fold enhanced potency over its native β-form (2, IC₅₀ = 0.88 μM) specifically in SU-DHL-6 cell lines, despite similar activity against solid tumors. The C14α-configured compounds 6k (IC₅₀ = 0.12 μM) and 6l (IC₅₀ = 0.31 μM) exhibited superior activity compared to their C14β-configured counterparts with the same substituents, 2k (IC₅₀ = 0.71 μM) and 2l (IC₅₀ = 0.47 μM), respectively. On the other hand, the aliphatic derivatives of C14α-O- series generally demonstrated reduced solubility, underscoring the importance of synergistic optimization of the substituent and configuration. Overall, the most potent compound 6k with a C14α-acrylate substitution (IC₅₀ = 0.12 μM) demonstrated a 4.4-fold increase in potency compared to its parent compound 6 and was 16-fold more active than oridonin in the SU-DHL-6 cell lines. Mechanistic studies established that the most potent derivative 6k induces apoptosis and downregulates p-Akt in SU-DHL-6 cells without affecting cell cycle progression. Our study for the first time demonstrates that the stereochemistry at position C14 could affect the selectivity and antiproliferative activity of oridonin derivatives, providing novel natural product-derived lead compounds for further development of anti-cancer drugs.

News (Medical) associated with Oridonin

26 Jan 2024

·www.prnewswire.com

Three Journal of Pharmaceutical Analysis Studies Explore the Use of Traditional Chinese Medicine for Various Diseases

XI'AN, China, Jan. 26, 2024 /PRNewswire/ -- Despite demonstrating significant clinical efficacy against various diseases, the widespread use of Traditional Chinese Medicine (TCM) is still limited. This is mainly due to the complexity in their formulation and lack of sufficient pharmacological and safety-related data. To address this gap, a new issue of the Journal of Pharmaceutical Analysis presents three independent studies which assessed the potency of TCM-based compounds for various human diseases, along with their molecular mechanisms of action. Continue Reading Latest research unveils the potential of Traditional Chinese Medicine compounds for the treatment of human diseases The accumulation of excess fat in the liver leads to non-alcoholic fatty liver disease (NAFLD). Oridonin (ORI), a TCM derived from the Chinese herb Rabdosia rubescens, exhibits anti-inflammatory effects. An article available online on 21 August 2023 and published in Volume 13, Issue 11 of the journal in November 2023, now reveals that ORI regulates lipid homeostasis in the liver by maintaining the balance between triglyceride (TG) and phosphatidylethanolamine (PE), through modulation of adipose triglyceride lipase (ATGL) and ethanolamine phosphotransferase 1 (EPT1) expression via the liver X receptor alpha (LXRα) signaling pathway. "When the TG-PE lipid balance is disturbed, the seesaw tilts towards TG, increasing the risk of NAFLD. Restoring lipid homeostasis using compounds like oridonin can alleviate lipid accumulation and liver cytotoxicity," explains Professor Lan Tang. Tumor heterogeneity compromises the efficacy of radiotherapy for treating lung cancer. Radiosensitizers help prime tumor cells and improve their response to radiation. Now, in an article available online on 7 June 2023 and published in Volume 13, Issue 11 of the journal in November 2023, researchers found that ginsenoside Rg5 induced cell-cycle arrest and enhanced radiation-induced cell death. Ginsenoside Rg5 interacts with heat shock protein alpha (HSP90α) with high affinity and reduces the binding between HSP90 and cell division cycle 37 (CDC37), promoting HSP90-CDC37 client protein degradation. "Ginsenoside Rg5 can be potentially developed into a new drug for improving the sensitivity of lung cancer and other types of tumors to radiation therapy," the authors explain. Diabetic retinopathy (DR) is characterized by the activation of oxidative stress pathways in response to high glucose. In a study available online on 12 May 2023 and published in Volume 13, Issue 11 of the journal in November 2023, researchers synthesized a polymeric drug complex by combining a natural flavonoid antioxidant known as dihydromyricetin (DMY) with iron (Fe) ions in nano-coordinated polymer particles (NCPs). Fe-DMY NCPs can alleviate glucose-induced oxidative damage and reverse the pathological features of DR by decreasing the expression of key proteins involved in microvascular dysfunction. Fe-DMY NCPs could also inhibit the activation of Poldip2-Nox4-H2O2 signaling pathway and down-regulate important vascular function indicators such as VCAM-1, HIF-1α, and VEGF. Explaining its applications, the authors say, "We report for the first time the synthesis and validation of ultra-small Fe-DMY NCPs. Fe-DMY complexes bear the potential to alleviate the impact of DR on vision, thus improving the quality of life of affected individuals." These studies provide a scientific basis for the development of TCM-based compounds into effective targeted therapies for various diseases. Reference Titles of original papers: Oridonin restores hepatic lipid homeostasis in an LXRa-ATGL/EPT1 axis-dependent manner Ginsenoside Rg5 enhances the radiosensitivity of lung adenocarcinoma via reducing HSP90-CDC37 interaction and promoting client protein degradation Nanoscale coordination polymer Fe-DMY downregulating Poldip2-Nox4-H2O2 pathway and alleviating diabetic retinopathy Journal name: Journal of Pharmaceutical Analysis DOI: Media contact Mengjie Wang [email protected] Xi'an, China +86-(0)29-88960092 SOURCE Journal of Pharmaceutical Analysis

100 Deals associated with Oridonin

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Colitis, Ulcerative	Preclinical	China	Tianjin University of Traditional Chinese Medicine	01 Sep 2025
Inflammation	Preclinical	China	University of Science & Technology of China	29 Jun 2018
Breast Cancer	Preclinical	United States	University of Texas Medical Branch	31 Oct 2013
Breast Cancer	Preclinical	China	Second Affiliated Hospital of Soochow University	31 Oct 2013

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