Abstract:Formyl-phloroglucinol meroterpenoids (FPMs) are important types of natural products with various bioactivities. Our antifungal susceptibility assay showed that one of the Eucalyptus robusta-derived FPMs, eucarobustol E (EE), exerted a strong inhibitory effect against Candida albicans biofilms at a concentration of 16 g/ml. EE was found to block the yeast-to-hypha transition and reduce the cellular surface hydrophobicity of the biofilm cells. RNA sequencing and real-time reverse transcription-PCR analysis showe… Show more
“…The MIC 80 values of KPA against different Candida species were measured by the broth microdilution method. The results showed that KPA exerted a moderate antifungal effect (based on the previous reports [6,10,13,17]) against the five most common Candida species, including C. albicans, C. glabrata, C. parapsilosis, C. tropicalis and C. krusei, the MIC 80 value of which was all 16 μg/mL. The MIC 80 values of the positive control AMB were 0.5 or 1 μg/mL, respectively ( Table 1).…”
Section: Antifungal Activity Of Kpa On Candida Species (Mics)mentioning
Candidiasis causes high morbidity and mortality among immunocompromised patients. Antifungal drug resistance and cytotoxicity highlight the need of effective antifungal therapeutics. In this study, we found that kalopanaxsaponin A (KPA), a triterpenoid saponin natural product, could inhibit the proliferation of various Candida species, and exerted a fungicidal effect against C. albicans. To further explore its antifungal action mode, spectrofluorophotometer, fluorescence microscopy and transmission electron microscopy were performed, showing that KPA treatment induced the accumulation of intracellular reactive oxygen species (ROS), resulting in mitochondrial dysfunction. Meanwhile, KPA treatment also broke down the membrane barrier of C. albicans causing the leakage of intracellular trehalose, the entrance of extracellular impermeable substance and the decrease of ergosterol content. Both ROS accumulation and membrane destruction contributed to the death of C. albicans cells. Our work preliminarily elucidated the potential mechanisms of KPA against C. albicans on a cellular level, and might provide a potential option for the treatment of clinical candidiasis.
“…The MIC 80 values of KPA against different Candida species were measured by the broth microdilution method. The results showed that KPA exerted a moderate antifungal effect (based on the previous reports [6,10,13,17]) against the five most common Candida species, including C. albicans, C. glabrata, C. parapsilosis, C. tropicalis and C. krusei, the MIC 80 value of which was all 16 μg/mL. The MIC 80 values of the positive control AMB were 0.5 or 1 μg/mL, respectively ( Table 1).…”
Section: Antifungal Activity Of Kpa On Candida Species (Mics)mentioning
Candidiasis causes high morbidity and mortality among immunocompromised patients. Antifungal drug resistance and cytotoxicity highlight the need of effective antifungal therapeutics. In this study, we found that kalopanaxsaponin A (KPA), a triterpenoid saponin natural product, could inhibit the proliferation of various Candida species, and exerted a fungicidal effect against C. albicans. To further explore its antifungal action mode, spectrofluorophotometer, fluorescence microscopy and transmission electron microscopy were performed, showing that KPA treatment induced the accumulation of intracellular reactive oxygen species (ROS), resulting in mitochondrial dysfunction. Meanwhile, KPA treatment also broke down the membrane barrier of C. albicans causing the leakage of intracellular trehalose, the entrance of extracellular impermeable substance and the decrease of ergosterol content. Both ROS accumulation and membrane destruction contributed to the death of C. albicans cells. Our work preliminarily elucidated the potential mechanisms of KPA against C. albicans on a cellular level, and might provide a potential option for the treatment of clinical candidiasis.
“…For example, mixed polymicrobial infections due to the presence of bacteria and pathogenic fungi, commonly found in patients with chronic infections, constitute a noteworthy health care burden. Citrus EOs are capable of preventing the polymicrobial biofilm formed by Pseudomonas aeruginosa and pathogenic fungi, in particular A. fumigatus and Scedosporium apiospermum , at concentration between 50 mg/L and 250 mg/L [ 120 ].These EOs showed a potential of inhibiting fungal growth with MIC in concentrations of 50 mg/L and 250 mg/L. Furthermore, Citrus EOs impeded formation of bacterial and fungal monomicrobial biofilms in concentrations of 50 mg/L.…”
Since ancient times, folk medicine and agro-food science have benefitted from the use of plant derivatives, such as essential oils, to combat different diseases, as well as to preserve food. In Nature, essential oils play a fundamental role in protecting the plant from biotic and abiotic attacks to which it may be subjected. Many researchers have analyzed in detail the modes of action of essential oils and most of their components. The purpose of this brief review is to describe the properties of essential oils, principally as antifungal agents, and their role in blocking cell communication mechanisms, fungal biofilm formation, and mycotoxin production.
“…Our previous research also demonstrated that several novel FPMs exerted antifungal and antibiofilm activities against Candida spp. (Liu R. H. et al, 2017). Further investigations on FPMs showed that those FPMs with weak or without antifungal effects demonstrated enhanced activities when combined with other antifungal FPMs or azoles (data not shown).…”
The frequent emergence of azole-resistant strains has increasingly led azoles to fail in treating candidiasis. Combination with other drugs is a good option to effectively reduce or retard its incidence of resistance. Natural products are a promising synergist source to assist azoles in treating resistant candidiasis. Eucalyptal D (ED), a formyl-phloroglucinol meroterpenoid, is one of the natural synergists, which could significantly enhance the anticandidal activity of fluconazole (FLC) in treating FLC resistant
C. albicans
. The checkerboard microdilution assay showed their synergistic effect. The agar disk diffusion test illustrated the key role of ED in synergy. The rhodamine 6G (R6G) efflux assay reflected ED could reduce drug efflux, but quantitative reverse transcription PCR analysis revealed the upregulation of
CDR1
and
CDR2
genes in ED treating group. Efflux pump-deficient strains were hyper-susceptible to ED, thus ED was speculated to be the substrate of efflux pump Cdr1p and Cdr2p to competitively inhibit the excretion of FLC or R6G, which mainly contributed to its synergistic effect.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.