Yuanhuacin and Related Anti-Inflammatory and Anticancer Daphnane Diterpenes from Genkwa Flos—An Overview

Bailly, Christian

doi:10.3390/biom12020192

Cited by 17 publications

(14 citation statements)

References 90 publications

(120 reference statements)

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“…Conventional cancer treatments commonly involve radiotherapy and chemotherapy but with several adverse effects and other critical disorders. Recently, natural products as potential anticancer agents are also used and studied in many cancer models [ 35 , 41 ]. One significant advantage of using natural extracts against cancer cells is their multitargeted modes of action, which provide potential synergistic behavior and polypharmacology approaches for cancer therapies.…”

Section: Discussionmentioning

confidence: 99%

Cytotoxic, Antibacterial, and Antioxidant Activities of the Leaf Extract of Sinningia bullata

Chen

Lin

et al. 2023

Plants

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Sinningia bullata is a tuberous member of the flowering plant family Gesneriaceae. Prior to this work, the antibacterial, antioxidant, and cytotoxic properties of S. bullata were undetermined. Here, we prepared different extracts from the leaf, stem, and tuber of S. bullata and investigated their pharmacological activities. The leaf extract of S. bullata, obtained by 100% acetone (Sb-L-A), had the highest total flavonoid content, antioxidation capacity, and cytotoxic and antibacterial activities. Sb-L-A displayed a broad range of antibacterial activities against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. The inhibition zones of Sb-L-A ranged from 8 to 30 mm and were in the following order: S. aureus > E. coli > P. aeruginosa. Incubation of B16F10 melanoma cells with Sb-L-A at a concentration of 80 μg/mL caused deaths at the rate of 96%, reduced migration by 100%, suppressed proliferation and colony formation by 99%, and induced apoptosis, which was observed in 96% of the B16F10 cells. In addition, the cytotoxic activities of Sb-L-A were synergistically enhanced when coacting with the antitumor drug epothilone B. Sb-L-A was also used to determine the cytotoxic effects against 4T1 mammary carcinoma cells. Sb-L-A of 60 μg/mL boosted the distribution of the G2 phase from 1.4% to 24.4% in the B16F10 cells. Accordingly, Sb-L-A might suppress melanoma cell proliferation by inducing G2 cell-cycle arrest. The most abundant compounds in Sb-L-A were identified using gas chromatography–mass spectrometry. The top two contents in this extract were adlupulone and villosin. Overall, the collective data in this study may indicate the pharmacological potentials of Sb-L-A for possible medical applications.

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Section: Discussionmentioning

confidence: 99%

Cytotoxic, Antibacterial, and Antioxidant Activities of the Leaf Extract of Sinningia bullata

Chen

Lin

et al. 2023

Plants

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“…[5,17] Yuanhuacine is an active component isolated from D. genkwa and has been proven to exert inhibitory efficacy in cell growth in several cancers, including lung cancer, breast cancer and colon carcinoma. [8] Nevertheless, its role in PCa remains elusive. Analogously, a previous study also corroborated the low toxicity of yuanhuacine to normal lung epithelial cells.…”

Section: Discussionmentioning

confidence: 99%

“…[5] Yuanhuacine is a daphnane diterpenoid (Figure 1A) traditional herbal medicine from the flowers of Daphne genkwa (Thymelaeaceae) and has a range of biological activities, including abortifacient, antivirus, and anti-inflammation. [6,7] In recent years, increasing interest has focused on the pharmacological activities of yuanhuacine, especially its antitumor activity, [8] including lung cancer, [9] colon cancer, [10] and breast cancer. [11] For instance, yuanhuacine inhibits human lung cancer cell proliferation and exhibits little cytotoxicity to normal lung epithelial cells.…”

Section: Introductionmentioning

confidence: 99%

Blockage of MDM2‐mediated p53 ubiquitination by yuanhuacine restrains the carcinogenesis of prostate carcinoma cells by suppressing LncRNA LINC00665

Yan

et al. 2022

J Biochem & Molecular Tox

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Prostate cancer (PCa) is known as a challenging issue for the global men health due to its uncontrolled proliferation and high metastatic potential. Increasing evidence has supported plant extracts and plantderived natural derivatives as a promising anti-tumor therapeutics as their less toxic side effects.Yuanhuacine is an active component isolated from Daphne genkwa and can effectively suppress tumorigenesis of several cancers. However, its role in PCa is still unclear. In this study, yuanhuacine dosedependently inhibited PCa cell proliferation and induced cell apoptosis. Moreover, yuanhuacine treatment also restrained PCa cell invasion and migration. Mechanically, yuanhuacine decreased p53 protein ubiquitination, degradation and ultimately increased p53 levels, which was regulated by inhibiting phosphorylation and total protein levels of Mouse Double Minute 2 (MDM2). Moreover, elevation of MDM2 reversed the suppressive e cacy of yuanhuacine in PCa cell viability, invasion and migration. The network pharmacology and bioinformatics analysis con rmed that MDM2 might be a common target of Daphne genkwa and LINC00665. Furthermore, yuanhuacine reduced LINC00665 expression. Upregulation of LINC00665 inversed yuanhuacine-mediated inhibition in MDM2 protein expression and suppressed p53 levels by enhancing its ubiquitination in yuanhuacine-treated cells. Importantly, the inhibitory effects of yuanhuacine on cell viability and metastatic potential were offset after LINC00665 elevation. Together, the current nding highlight that yuanhuacine may possess its tumor-suppressive e cacy by inhibiting LINC00665-mediated MDM2/p53 ubiquitination signaling. Therefore, this data indicate that yuanhuacine may be a promising candidate for the treatment of PCa.

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“…et Zucc. exhibit anti‐inflammatory and neuroprotective effects 5,6 ; triptolide isolated from Tripterygium wilfordii Hook. F. exhibits anti‐inflammatory, antitumor, and immunosuppressive effects 7,8 .…”

Section: Introductionmentioning

confidence: 99%

An improved strategy for identification and annotation of easily in‐sourced dissociation diterpene lactones from plant natural products: Taking Andrographis paniculata (Burm. f.) as an example

Ding

Zhang

et al. 2023

Rapid Comm Mass Spectrometry

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Rationale: Diterpene lactones (DL) in Andrographis paniculata (AP) are known as "natural antibiotics" for their excellent antibacterial activity. During mass spectrometry (MS) analysis, the hydroxyl groups in the AP DL skeleton are prone to neutral loss of H 2 O, producing high in-source fragment peaks and affecting the characterization of these components.Methods: Mass tags were applied during the MS data acquisition step, and special adduct ion form was used to guide the data processing and characterization steps.Besides, the total number of characterized AP DLs significantly increased when combining the number of neutrally lost H 2 O from AP DLs, incorporating information on the diagnostic ions, and adopting molecular networks generated with the Global Natural Products Social Molecular Networking database.Results: Ninety-nine DLs, comprising 6 monohydroxyl groups, 20 dihydroxyl groups, 27 trihydroxy groups, and 46 DLs with more than 3 hydroxyl groups, were characterized from AP. In addition, based on the characteristic fragments in the product ions (C 3 H 4 , Δm/z = 40.03 Da), it could be assumed that 90 DLs had the C19-OH structure among the identified DLs. The current study provides a new approach for collecting, processing, and characterizing MS analysis of natural DLs prone to in-source fragmentation.Conclusions: MS characterization of AP DLs was significantly improved, and many potential new compounds were identified in AP. This characterization provides new methods for the purification and identification of AP DLs.

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Yuanhuacin and Related Anti-Inflammatory and Anticancer Daphnane Diterpenes from Genkwa Flos—An Overview

Cited by 17 publications

References 90 publications

Cytotoxic, Antibacterial, and Antioxidant Activities of the Leaf Extract of Sinningia bullata

Cytotoxic, Antibacterial, and Antioxidant Activities of the Leaf Extract of Sinningia bullata

Blockage of MDM2‐mediated p53 ubiquitination by yuanhuacine restrains the carcinogenesis of prostate carcinoma cells by suppressing LncRNA LINC00665

An improved strategy for identification and annotation of easily in‐sourced dissociation diterpene lactones from plant natural products: Taking Andrographis paniculata (Burm. f.) as an example

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