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The Potential of Microbial Mediated Fermentation Products of Herbal Material in Anti-Aging Cosmetics
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
Biotransformation may also result in the conversion of an active compound to an equally active compound, as in the instance of the cardiac glycosides lanatoside C to digoxin by Penicillium vermiculatum and Arthrobacter citreus (Figure 2.4). In this two-step reaction, lanatoside C co-cultured with P. vermiculatum for 12–20 hours yields acetyldigoxin as the sole metabolite through deglycosylation, with a yield of 60%. Incubation of acetyldigoxin with A. citrus for a further 12 hours results in a deacetylation reaction which yields digoxin with approximately 60% efficiency. Alternatively, lanatoside C may be incubated with P. vermiculatum or A. citreus for 240 and 120 hours, respectively; however, in addition to the extended period required for the incubation, the reaction yields are low (Figure 2.4) (Fuska et al., 1987).
Clinical studies on Shengmai San
Published in Kam-Ming Ko, Shengmai San, 2002
Ye-Zhi Rong, Mei-Hua Zhao, Bao-Jing Lu, Xiang-Yang Zhu, Shang-Biao Lu, Ya-Chen Zhang, Jie Chen, Kam-Ming Ko
By the Differentiation of Signs and Symptoms in traditional Chinese medicine, dilated cardiomyopathy belongs to mild or severe ‘palpitation’, manifested by deficiencies of the Qi (vital energy) and Yin, and retention of dampness and anxiety (Zhang H. 1997). These symptoms should therefore be treated by invigorating the Qi and nourishing the Yin, eliminating dampness and diuresis, as well as tranquilizing the mind. Modern pharmacological studies have shown that SMS could improve heart function and enhance the myocardial contractility, with its positive ionotropic action being similar to that of lanatoside. SMS can also enhance the oxygen inhaling and carrying capacity of the body, thereby invigorating the Qi.
Efflux in Gram-negative bacteria: what are the latest opportunities for drug discovery?
Published in Expert Opinion on Drug Discovery, 2023
Teresa Gil-Gil, Pablo Laborda, Luz Edith Ochoa-Sánchez, José Luis Martínez, Sara Hernando-Amado
Given the clinical relevance of P. aeruginosa, different works, analyzing potential inhibitors of its efflux pumps, have been published. Lanatoside C, diadzein, conessine, curcumine, berberine, and palmatine from Digitalis lanata, Glycine max, Curcuma longa, Holarrhena antidysenterica, and Berveris bulgaris, respectively [147,151–153], are inhibitors of the intrinsic resistance element MexAB-OprM [41]. Diadzein and Lanatoside C also have inhibitory activity against the AcrAB-TolC efflux pump of E. coli [147]. In addition, the activity of this efflux pump is inhibited by ursolic acid from Eucalyptus tereticornis [149], lysergol from Ipomea muricata [148], gallotannin 1,2,6-tri-O-galloyl-β-d-glucopyranose from Terminalia chebula [150], 4-hydroxy-ά-tetralone combined with its semisynthetic derivatives from Ammannia spp. [154] and plumbagin, nordihydroguaretic acid and shikonin from Plumbago indica, Larrea tridentata, and Lithospermum erythrorhizon, respectively [155]. Altogether, these data indicate that phenolic and aromatic compounds, flavones, alkaloids, or tannins from plants are valuable sources of efflux pump inhibitors.
Efflux pump inhibitors as a promising adjunct therapy against drug resistant tuberculosis: a new strategy to revisit mycobacterial targets and repurpose old drugs
Published in Expert Review of Anti-infective Therapy, 2020
Liliana Rodrigues, Pedro Cravo, Miguel Viveiros
This strategy also identified several antiarrhythmic, antihypertensive drugs that potentially target a probable metal cation transporter P-type ATPase A CtpF (Rv1997) in M. tuberculosis. Deslanoside is a cardiac glycoside used to treat congestive heart failure, supraventricular arrhythmias and to control ventricular rate in the treatment of chronic atrial fibrillation. This compound inhibits the Na+/K+-ATPase pump, resulting in an increase in intracellular sodium and calcium concentrations that may promote activation of contractile proteins, such as actin and myosin [162]. Acetyldigitoxin is a cardioactive derivative of lanatoside A or of digitoxin used for fast digitalization in congestive heart failure. The proposed mode of action is similar to deslanoside: inhibition of the Na+/K+ pump that leads to increased amounts of calcium [163]. Ethacrynic acid is used in the treatment of high blood pressure and edema caused by diseases like congestive heart failure, liver failure, and kidney failure. It inhibits the symport of sodium, potassium, and chloride primarily in the ascending limb of Henle. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid [164]. Finally, the last drug in this group is bretylium, used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. The main mode of action for bretylium is thought to be inhibition of voltage-gated potassium channels and the Na+/K+-ATPase [165].
The development of efflux pump inhibitors to treat Gram-negative infections
Published in Expert Opinion on Drug Discovery, 2018
Paula Blanco, Fernando Sanz-García, Sara Hernando-Amado, José Luis Martínez, Manuel Alcalde-Rico
Some of the EPIs so far described are phenolic compounds able to increase the susceptibility of Gram-negative pathogens to antibiotics, as erythromycin or vancomycin, with poor activity against these microorganisms [32]. Besides increasing the bacterial susceptibility to antimicrobials, these compounds may have also antibiofilm activity, a property of some EPIs (including catechol) extracted from maple syrup [47]. Constituents of essential oils, such as the monoterpene (−)-α-pinene present in Alpinia Katsumadai seeds [48], also inhibit the activity of Gram-negative efflux pumps. Indeed, (−)-α-pinene inhibits the CmeABC and Cj1687 efflux pumps and consequently increases de susceptibility of Campylobater jejuni to ciprofloxacin, erythromycin, and triclosan [48]. Given its clinical relevance, different works have focused on the search of plant-derived inhibitors of P. aeruginosa efflux pumps. Among them, lanatoside C, diadzein, conessine, berberine, and palmatine present in Digitalis lanata, Glycine max, Holarrhena antidysenterica, and Berveris bulgaris, respectively [49–51], inhibit the activity of MexAB, an efflux pump with a relevant role in the intrinsic resistance to antibiotics of P. aeruginosa [36]. Lanatoside C and diadzein also have EPI activity against the E. coli AcrAB efflux pump, indicating that these inhibitors are not fully specific [49]. Other EPIs capable to inhibit the activity of E. coli efflux pumps are ursolic acid from Eucalyptus tereticornis [52], lysergol from Ipomea muricata [53], gallotannin 1,2,6-tri-O-galloyl-β-d-glucopyranose from Terminalia chebula [54], 4-hydroxy-α-tetralone combined with its semisynthetic derivatives from Ammannia spp. [55] and plumbagin, nordihydroguaretic acid, and shikonin from Plumbago indica, Larrea tridentata, and Lithospermum erythrorhizon, respectively [56]. Altogether, these findings indicate that plants can be a good source of EPIs that may belong, among others, to the groups of phenolic and aromatic compounds, flavones, alkaloids, or tannins.