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Natural Products from the Amazon Region as Potential Antimicrobials
Published in Mahendra Rai, Chistiane M. Feitosa, Eco-Friendly Biobased Products Used in Microbial Diseases, 2022
Josiane E. A. Silva, Iasmin L. D. Paranatinga, Elaine C. P. Oliveira, Silvia K. S. Escher, Ananda S. Antonio, Leandro S. Nascimento, Patricia P. Orlandi, Valdir F. Veiga-Júnior
The diterpenoids are a chemical class comprising metabolites with a 20-carbon skeleton, formed by four isoprene units and derived from geranyl geranyl pyrophosphate. Their structure can be linear, bicyclic, tricyclic, tetracyclic, pentacyclic or macrocyclic with distinct functional groups. This chemical class is particularly interesting due to its antimicrobial activity.
Chemopreventive Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Diterpenes (also called diterpenoids) are a highly diverse C20-subclass of terpenoids comprised of four isoprene units. Diterpenes are biosynthesized by animals, plants, and fungi, and form the basis for biologically essential compounds including retinal, retinol, and phytol, as well as compounds with reported chemopreventive activity such as cafestol and kahweol (Figure 12.29), which are described below. Structures of the diterpenoids cafestol and kahweol.
Marine Natural Products for Human Health Care
Published in Hafiz Ansar Rasul Suleria, Megh R. Goyal, Health Benefits of Secondary Phytocompounds from Plant and Marine Sources, 2021
Marine corals with Eleutherobin from a small Australian soft coral of the genus Eleutherobia sp. [173] and sarcodictyin A from the Mediterranean stoloniferan coral (Sarcodictyon roseum) [61] are good sources of anticancer drugs. They are closely related diterpenoids that mimic Taxol by stabilizing microtubules. Eleutherobin showed selective cytotoxicity toward breast, renal, ovarian, and lung cancer cell lines and is generally more inhibitory than sarcodictyin A. Despite some difficulties in the beginning, soon after the reporting of its molecular structure and issuing of patent, these two biocompounds were successfully synthesized [48, 206, 207]. Eleutherobin underwent some preclinical trials at Bristol-Myers Squibb but is no longer being pursued, due to the difficulty in obtaining sufficient material.
Biogenic synthesis and characterization of silver nanoparticles using aqueous leaf extract of Scoparia dulcis L. and assessment of their antimicrobial property
Published in Drug and Chemical Toxicology, 2020
In summary, plant aqueous extract could be used as an efficient green material for rapid and reliable synthesis of nanoparticles. In the present study, silver nanoparticles were synthesized using S. dulcis aqueous leaf extract. By changing the quantity of plant extract, silver ion concentration, and reaction time at room temperature, the size of nanoparticles was varied. Aqueous plant mediated the structured patterning of nanoparticles into spheres. At optimum conditions, FCC structure with diameter range of 3 to 18 nm have been envisaged without chemical reagent and was stable for more than 3 months. Color change occurs due to Surface plasmon resonance during the reaction with the phytochemicals present in the leaf extract. The development of nanoparticles was monitored by UV-Vis spectroscopy and the particle size was measured by DLS. Characterization of silver nanoparticles was evaluated by TEM and XRD analysis at optimum conditions. FTIR analysis confirmed the bioreduction of Ag+ ions to AgNPs by various functional groups. Moreover, the synthesized nanoparticles exhibit a pronounced antibacterial activity against different tested microorganisms. It is already known that the isolated different types of biologically active diterpenoids from the aerial parts of S. dulcis showed cytotoxicity against different cancer cell lines. These AgNPs could be a potential candidates to target the cancer cells. In this study, the synthesized AgNPs using S. dulcis aqueous leaf extract, in nanoformulation could be a better approach to enhance the efficacy of plant extracts.
Recent progress in the development of small molecule Nrf2 activators: a patent review (2017-present)
Published in Expert Opinion on Therapeutic Patents, 2020
Haishan Zhou, Yan Wang, Qidong You, Zhengyu Jiang
Recently, Li et al. [76] had collected 66 diterpenoids and evaluated the effects of Nrf2 activation via a NAD(P)H: quinone reductase (QR) assay in murine hepatoma Hepa1c1c7 cells. 16 diterpenoids showed Nrf2-dependent protective response. Among them, sphaeropsidin A (SA, 17, Figure 8) was the most outstanding activator, and exhibited about 5-folds potency than that of SFN. Subsequent cell-based studies showed that SA could activate Nrf2 and its downstream cytoprotective genes (NQO1 and GCLM) via stabilizing Nrf2 in a process involving protein kinases phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K), protein kinase C (PKC), and protein kinase R-like endoplasmic reticulum kinase (PERK). Furthermore, SA prevented human lung epithelial cells against sodium arsenite [As(III)]- and cigarette smoke extract (CSE)-induced oxidative stress and cytotoxicity in vitro, and reduced metronidazole (MTZ)-induced oxidative damage in Tg (krt4: NTR-hKikGR)cy17 transgenic zebrafish and lipopolysaccharide (LPS)-induced oxidative injury in wild-type AB zebrafish.
Screening of in vitro antimicrobial activity of plants used in traditional Indonesian medicine
Published in Pharmaceutical Biology, 2018
Andreas Romulo, Ervizal A. M. Zuhud, Johana Rondevaldova, Ladislav Kokoska
In this study, leaf extract of O. aristatus exhibited inhibitory activity against C. albicans, E. faecalis, S. aureus and P. aeruginosa. This is in correspondence with previously published results showing the antimicrobial effect of methanol and ethanol leaf extract of O. aristatus against S. aureus, P. aeruginosa (Ho et al. 2010; Vijayan et al. 2013) and C. albicans (Neharkar and Laware 2013), as determined by disk and agar diffusion methods. In addition, the essential oil of O. aristatus leaf has also been reported as exhibiting antifungal properties against several plant pathogens such as Botrytis cinerea, Colletotricum capsici, Fusarium solani, Phytophthora capsici and Rhizoctonia solani (Hossain et al. 2008). Di et al. (2013) isolated several new diterpenoid compounds (orthoarisins) from an ethanol aerial extract of O. aristatus. Many reports have extensively shown that diterpenoids exert significant antimicrobial effects (Veneziani et al. 2017). Olah et al. (2003) reported the presence of polymethoxylated flavonoids and caffeic acid derivatives, mainly rosmarinic acid in an ethanol leaf extract of O. aristatus. This compound has been known to possess antimicrobial activity against a broad spectrum of bacteria and yeasts (Gohari et al. 2010; Salawu et al. 2011). It can be assumed that these compounds may contribute to the broad-spectrum antimicrobial potential of O. aristatus found in the present study.