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An Andrographolide from Helichrysum caespitium (DC.) Sond. Ex Harv., (Asteraceae) and Its Antimicrobial, Antiquorum Sensing, and Antibiofilm Potentials.

ABSTRACT: Helichrysum caespititium (DC.) Sond. Ex Harv., (Asteraceae) is a medicinal plant indigenous to South Africa. Its non-polar extracts exhibit significant antimicrobial and, in particular, antigonorrheal activity. This study aimed at isolating and purifying the active antigonorrheal compound from its chloroform extract and validating its inhibition potential on quorum sensing (QS) and biofilm formation of multi-drug resistant (MDR) pathogens. Phytochemical investigation of aerial parts of H. caespititium afforded a diterpene lactone (CF6). The effect of CF6 on violacein production and biofilm formation was studied using in vitro quantitative violacein inhibition (Chromobacterium violaceum) and biofilm formation (Streptococcus pyogenes, Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Neisseria gonorrhoeae, and Pseudomonas aeruginosa). The structure of CF6 was characterized using FTIR, NMR, and UPLC-MS data accordingly, as 10-methyl-8-(propan-17-ylidene)naphthalen-9-yl)-11-vinyl-14-hydroxyfuran-16-one. The susceptibility testing of the pathogens against CF6 revealed Neisseria gonorrhoeae was noticeably susceptible with a MIC value of 60 µg/mL, while Streptococcus pyogenes and Staphylococcus aureus showed MIC of 125 µg/mL. All gram-negative pathogens, Escherichia coli, Klebsiella pneumonia and Pseudomonas aeruginosa were inhibited at 250 µg/mL. CF6 also inhibited the production of violacein by 51.88% at 250 µg/mL and prevented cell attachment by 40.76-81.18%, with N. gonorrhoeae being highly prohibited from forming biofilm. In conclusion, 10-methyl-8-(propan-17-ylidene)naphthalen-9-yl)-11-vinyl-14-hydroxyfuran-16-one is the first of its kind to be isolated from the non-polar (chloroform) extract of South African Helichrysum caespititium with antigonorrheal, antimicrobial, antiquorum sensing, and antibiofilm properties. The compound may serve as a drug candidate against MDR pathogens.

SUBMITTER: Bassey K

PROVIDER: S-EPMC8698270 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:Quorum sensing (QS) and biofilm inhibition are recognized as the novel drug targets for the broad-spectrum anti-infective strategy to combat the infections caused by drug-resistant bacterial pathogens. Many compounds from medicinal plants have been found to demonstrate anti-infective activity. However, broad-spectrum anti-QS and antibiofilm efficacy and their mode of action are poorly studied. In this study, the efficacy of coumarin was tested against QS-regulated virulent traits of Gram-negative bacteria. Coumarin inhibited the production of violacein pigment in Chromobacterium violaceum 12472 by 64.21%. Similarly, there was 87.25, 70.05, 76.07, 58.64, 48.94, and 81.20% inhibition of pyocyanin, pyoverdin, and proteolytic activity, lasB elastase activity, swimming motility, and rhamnolipid production, respectively, in Pseudomonas aeruginosa PAO1. All tested virulence factors of Serratia marcescens MTCC 97 were also suppressed by more than 50% at the highest sub-minimum inhibitory concentration. Moreover, the biofilms of bacterial pathogens were also inhibited in a dose-dependent manner. Molecular docking and molecular dynamics (MD) simulation gave insights into the possible mode of action. The binding energy obtained by docking studies ranged from -5.7 to -8.1 kcal mol-1. Coumarin was found to be docked in the active site of acylhomoserine lactone (AHL) synthases and regulatory proteins of QS. MD simulations further supported the in vitro studies where coumarin formed a stable complex with the tested proteins. The secondary structure of all proteins showed a negligible change in the presence of coumarin. Computational studies showed that the possible mechanisms of anti-QS activity were the inhibition of AHL synthesis, antagonization of QS-regulatory proteins, and blocking of the receptor proteins. The findings of this study clearly highlight the potency of coumarin against the virulence factors of Gram-negative bacterial pathogens that may be developed as an effective inhibitor of QS and biofilms.

Project description:Baccharis dracunculifolia DC (Lamiaceae) (Asteraceae) is found in South America, mainly in Argentina, Brazil, Bolivia, Paraguay and Uruguay. Folk medicine is used as a sedative, hypotensive, bronchodilator, cardiovascular disorders, anti-flu, and also in skin wounds. Considered the main source of green propolis, which increases the pharmacological interest in this species. It is also known as a "benefactor" plant facilitating the development of other plant species around it, being indicated for the recovery of degraded areas. This species has been studied for decades in order to isolate and identify the active principles present in the aerial parts (leaves and flowers) and roots. The present study consists of a review of the scientific literature addressing the ethnobotanical, ethnomedicinal, phytochemical, pharmacological and potential cytotoxic effects of the B. dracunculifolia species. In this survey, we sought to investigate issues related to the botanical and geographic description of the species, the ethnobotanical uses, as well as the phytochemical studies of the essential oil, extracts and green propolis obtained from the aerial parts and roots of B. dracunculifolia. Using high precision analytical tools, numerous compounds have already been isolated and identified from leaves and flowers such as the flavonoids: naringenin, acacetin, dihydrokaempferol, isosakuranetin and kaempferide; phenolic acids: p-coumaric, dihydrocoumaric, ferulic (E)-cinnamic, hydroxycinnamic, gallic, caffeic, and several caffeoylquinic acids derivatives; phenolic acids prenylated: artepillin C, baccharin, drupanin; the glycosides dracuculifosides and the pentacyclic triterpenoids: Baccharis oxide and friedelanol. The predominant class in the essential oil of leaves and flowers are terpenoids comprising oxygenated monoterpenes and sesquiterpenes, highlighting the compounds nerolidol, spathulenol, germacrene D and bicyclogermacrene. These compounds give the species high antimicrobial, antioxidant, antitumor, analgesic, immunomodulatory and antiparasitic potential, making this species a promising herbal medicine. In vitro toxicity assays with B. dracunculifolia extract showed low or no cytotoxicity. However, in vivo analyses with high doses of the aqueous extract resulted in genotoxic effects, which leads us to conclude that the toxicity of this plant is dose-dependent.

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An Andrographolide from Helichrysum caespitium (DC.) Sond. Ex Harv., (Asteraceae) and Its Antimicrobial, Antiquorum Sensing, and Antibiofilm Potentials.

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