Ursolic acid derivatives are potent inhibitors against porcine reproductive and respiratory syndrome virus

Yang, Chen; Li, Hui; Wu, Li; Zhang, Mingxin; Gao, Yarou; Wang, Heng; Xu, Dan; Chen, Weisan; Song, Gaopeng; Chen, Jianxin

doi:10.1039/d0ra04070c

Cited by 10 publications

(5 citation statements)

References 37 publications

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“…Atractylodinol and ethoxysanguinarine were reported to have anti-PRRSV activity with an inhibitory concentration of 50% (IC 50 ) of 7.9 and 39.4 μM, respectively ( 58 ). 3-O-b-chacotriosyl ursolic acid and its ester analogs exhibited potent anti-PRRSV activity in vitro with minimal cytotoxicity ( 59 ). Nevertheless, there is still a long time before these compounds are further developed into approved drugs since novel drug development is of high cost and risk.…”

Section: Discussionmentioning

confidence: 99%

Therapeutic efficacy of tylvalosin combined with Poria cocos polysaccharides against porcine reproductive and respiratory syndrome

et al. 2023

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Porcine reproductive and respiratory syndrome (PRRS) is one of the most economically important infectious diseases of pigs worldwide. Vaccination and various management measures have been implemented to control PRRS. However, due to high genetic diversity and insufficient understanding of the pathogenesis and immunological mechanisms, PRRS is still a challenge to the pig industry. Therefore, it is important to develop novel strategies to combat PRRS virus (PRRSV) infection. In this study, our data show that tylvalosin, a third-generation animal-specific macrolide, could inhibit PRRSV replication in MARC-145 cells, and suppress the PRRSV-induced NF-κB activation and cytokines expression. The pig infection experiment further demonstrated that tylvalosin could significantly reduce the virus loads in serum and tissues, and alleviate lung lesions of pigs infected with highly pathogenic PRRSV strains. The fever and loss of daily gain (LoDG) of the pigs were decreased as well. Considering the feature of immune suppression of PRRSV, a combination of tylvalosin with the immunopotentiator Poria cocos polysaccharides (PCP) was developed. Pig experiment showed this combination had a better therapeutic efficacy against PRRSV infection than tylvalosin and PCP alone in attenuating lung lesions, alleviating fever, and suppressing cytokines production. This study suggests that tylvalosin has significant antiviral and anti-inflammatory effects against PRRSV infection, and the combination of tylvalosin and PCP provides a promising strategy for PRRS treatment.

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Section: Discussionmentioning

confidence: 99%

Therapeutic efficacy of tylvalosin combined with Poria cocos polysaccharides against porcine reproductive and respiratory syndrome

et al. 2023

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“…The favorable structure of UA over OA probably contributes to the better antimicrobial activity of UA. A negative effect on the antimicrobial activity was confirmed when the methyl group was replaced by a -CH 2 OH, a -CHO, or a -COOH group [25], indicating that the methyl group appears to be necessary and sufficient for antibacterial activity. This further proves our deduction that a methyl group may be an important group that plays an antibacterial role.…”

Section: Discussionmentioning

confidence: 99%

Metabolomic Profile and Antibacterial Bioactivity of Akebia trifoliata (Thunb.) Koidz Pericarp Extract

et al. 2022

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Akebia trifoliata (A. trifoliata) is a significant medicinal and edible fruit crop and has some important bioactivities. However, there are few studies on the bacteriostatic activity of A. trifoliata, and the underlying mechanism of A. trifoliata for antibacterial activity is still unknown. Therefore, the bacteriostatic activity and antibacterial mechanism of A. trifoliata were investigated by a combination of chemical assays, using the UHPLC-TOF-MS/MS technique. The results indicated that alkaloids, triterpenoids, and flavonoids are the major secondary bioactive compounds in A. trifoliata that play a crucial role in antibacterial activity. We found that EEPA exhibited both bacteriostatic and bactericidal effects against all Gram-positive and Gram-negative bacteria tested, with IZDs ranging from 13.80 ± 0.79 to 17.00 ± 0.58 mm. Significant differences in terms of sensitivity between Gram-positive and Gram-negative bacteria were not observed. In contrast, both antibiotics (kanamycin sulfate and ampicillin sodium salt) exhibited much better antimicrobial activity against Gram-positive bacteria than Gram-negative bacteria. In addition, the primary antimicrobial mechanism was that EEPA increased cellular content leakage, altered the cell morphology, and destroyed the internal cell structure. Meanwhile, MA, UA, and OA, as the common triterpenoid components existing in plants, were used to analyze the relationships between the structures and the antimicrobial activities among homologous compounds, to determine the key functional group that plays an antibacterial role in MA, UA, and OA. As result, it was found that both the hydroxide and methyl groups present are important for their antibacterial activity. These findings suggested that EEPA exerted significant antimicrobial activity against S. aureus, E. coli, B. subtilis, and P. aeruginosa and might be a potential natural antibacterial.

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“…In vitro study revealed that UA reduces expression of human papilloma virus À18 (HPV-18) E6/E7 genes in HeLa cells; however expression of p53 did not change [25]. Similarly, a recent study by Chen et al, revealed that UA derivatives are effective against porcine reproductive and respiratory syndrome virus through direct inactivation of viral virion and replication [26].…”

Section: Antiviral Effects Of Ursolic Acidmentioning

confidence: 97%

The possible role of ursolic acid in Covid-19: A real game changer

Al-Kuraishy

Al-Gareeb

Batiha

2022

Clinical Nutrition ESPEN

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Ursolic acid (UA) is a pentacyclic terpenoid is usually found in the fruit peels and stem bark as secondary metabolites. UA has antiviral, antibacterial, and antiparasitic properties. UA has a wide spectrum of pharmacological activities against different infections. Because of the greatest antiviral and anti-inflammatory properties of UA, so it could be a plausible therapeutic herbal medicine in Covid-19 treatment. Covid-19 is a recent worldwide virulent disease pandemic due to severe acute respiratory coronavirus disease 2 (SARS-CoV-2). The pathogenesis of SARS-CoV-2 infection is related to the direct cytopathic effect and exaggerated immune response by which acute lung injury (ALI) and/or acute respiratory distress syndrome might be developed in critical cases. UA may inhibit main protease of SARS-CoV-2, and inhibits the interface flanked by SARS-CoV-2 viral proteins and its entry point commonly recognized as angiotensin converting enzyme 2 (ACE2). In addition, UA attenuates SARS-CoV-2-induced inflammatory reactions and oxidative stress. Therefore, UA could avert SARS-CoV-2 infection from causing ALI. This opinion proposed that UA might be a potential candidate therapy against Covid-19 and can mitigate post-Covid-19 complications such as lung fibrosis. In this regards, forthcoming studies are reasonable to substantiate the therapeutic role of UA in Covid-19. However, taken into account that Covid-19 is yet to be investigating for further evaluations, therefore, clinical trials are recommended regarding use and dose of UA in Covid-19 treatment, as well as secondary effects.

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Ursolic acid derivatives are potent inhibitors against porcine reproductive and respiratory syndrome virus

Abstract: Porcine reproductive and respiratory syndrome virus (PRRSV) is one of the most devastating viral pathogens of swine and has a substantial economic impact on the global pork industry.

Cited by 10 publications

References 37 publications

Therapeutic efficacy of tylvalosin combined with Poria cocos polysaccharides against porcine reproductive and respiratory syndrome

Therapeutic efficacy of tylvalosin combined with Poria cocos polysaccharides against porcine reproductive and respiratory syndrome

Metabolomic Profile and Antibacterial Bioactivity of Akebia trifoliata (Thunb.) Koidz Pericarp Extract

The possible role of ursolic acid in Covid-19: A real game changer

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