Phenolics and Carotenoid Contents in the Leaves of Different Organic and Conventional Raspberry (Rubus idaeus L.) Cultivars and Their In Vitro Activity

: Raspberry leaves are a source of carotenoids and polyphenols, including ellagic acid and salicylic acid. The results of scientific research suggest that they have potential pro-health properties that contribute to human health. The aim of this study was to determine the polyphenolic and carotenoid profiles in the leaves of selected raspberry cultivars and their in vitro activity. The second aim was to determine the impact of organic and conventional farm management on the polyphenol, carotenoid, and chlorophyll contents in different raspberry cultivars: ‘Polana’, ‘Polka’, ‘Tulameen’, ‘Laszka’ and ‘Glen Ample’. Compared with conventional raspberry leaves, organic raspberry leaves were characterized by a significantly higher content of dry matter, total polyphenols, total phenolic acids, chlorogenic acid, caffeic acid, salicylic acid and quercetin-3-O-rutinoside; moreover, the organic leaves were characterized by higher antioxidant activity. Among examined cultivars, ‘Polka’ c. was characterized by the highest antioxidant status. However, raspberry leaves from conventional farms contained more total carotenoids, violaxanthin, alpha-carotene, beta-carotene, total chlorophyll and individual forms of chlorophylls: a and b.

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Impact of Human Serum Albumin on Oritavancin In Vitro Activity against Enterococci

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00197-09 ◽

2009 ◽

Vol 53 (6) ◽

pp. 2687-2689 ◽

Cited By ~ 13

Author(s):

Geoffrey A. McKay ◽

Sylvain Beaulieu ◽

Ingrid Sarmiento ◽

Francis F. Arhin ◽

Thomas R. Parr ◽

...

Keyword(s):

Human Serum Albumin ◽

Serum Albumin ◽

Human Serum ◽

Vitro Activity ◽

In Vitro Activity ◽

Vancomycin Resistant Enterococci ◽

Vancomycin Resistant ◽

Time Kill ◽

The Impact

ABSTRACT Oritavancin is a lipoglycopeptide with activity against gram-positive pathogens including vancomycin-resistant enterococci. The impact of human serum albumin (HSA) on oritavancin activity against enterococci was compared to those of vancomycin, daptomycin, teicoplanin, and linezolid in vitro using MIC and time-kill methods. Oritavancin MICs increased between 0- and 8-fold in the presence of HSA. In time-kill assays with HSA, oritavancin retained activity, killing or inhibiting enterococci more rapidly than did comparators when peak concentrations were simulated.

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1276. Evaluation of CD377, a Novel Antiviral Fc-Conjugate (AVC), In Vitro Activity and In Vivo Efficacy in Immune-Competent and -Deficient (SCID) Lethal Mouse Models

Open Forum Infectious Diseases ◽

10.1093/ofid/ofaa439.1460 ◽

2020 ◽

Vol 7 (Supplement_1) ◽

pp. S654-S654

Author(s):

James Levin ◽

Karin Amundson ◽

Allen Borchardt ◽

Thanh Lam ◽

Tom Brady ◽

...

Keyword(s):

Mouse Models ◽

Survival Data ◽

Scid Mice ◽

Vitro Activity ◽

In Vitro Activity ◽

Prevention And Treatment ◽

The Impact ◽

Efficacy Studies

Abstract Background Cidara’s AVCs are novel, potent, antiviral agents conjugated with the Fc domain of human IgG1. CD377 is an AVC development candidate being evaluated for prevention and treatment of seasonal and pandemic influenza, including in immune-deficient populations unable to benefit from vaccination. We evaluated CD377 in vitro and in SCID mice to determine the impact of compromised immune status on efficacy. Methods CD377 and comparators (oseltamivir [OS], zanamivir [ZA], baloxavir marboxil [BM]) were evaluated in vitro by neuraminidase inhibition (NAI), and cytopathic effect (CPE) assays. The pharmacokinetics (PK) and efficacy of CD377 were determined in immune-competent (IC; BALB/c) and immune-deficient (ID; BALB/c SCID) mice. Efficacy was assessed by intranasal challenge at 3x the LD95 of influenza A/Puerto Rico/8/1934 (H1N1), followed by a single subcutaneous (SC) dose of CD377, 2 hours post-challenge. The SCID study also evaluated the efficacy of BM at 3 mg/kg (BID x 1 day). Body weights (BW) were monitored for 21 days, with 20% BW loss recorded as mortality. Results In vitro evaluation by NAI showed CD377, OS, and ZA to be approximately equipotent, with IC50 values between 0.5 and 1.7 nM. However, by CPE, CD377 was ~4.5-fold more active than BM and >1,000-fold more active than OS and ZA. In vivo, the PK of CD377 was found to be comparable in IC and ID mice. In subsequent efficacy studies, CD377 was protective at 0.1 mg/kg in IC mice (P=0.0020 vs. vehicle), while control groups fully succumbed to infection by Day 7 (Fig. 1A). In a similar study with ID mice, CD377 dosed at 0.1 mg/kg was also fully protective (P=0.0020). In contrast, mice treated with 6 mg/kg (total dose) of BM were only partially protected until day 13 (40% mortality by study end) (Fig. 1B). The potency of CD377 was further supported by BW data, which mirrored the survival data in both studies. Conclusion CD377 exhibited potent in vitro activity and had similar PK in IC and ID mice. In efficacy studies, CD377 demonstrated robust potency in both IC and ID mouse models at equivalent doses (0.1 mg/kg, SC, single dose). These results support further development of CD377 as a novel antiviral for the prevention and treatment of influenza infection, including in people with immune deficiencies and higher risk of infection. Balb/c and Balb/c SCID Disclosures James Levin, PhD, Cidara Therapeutics (Shareholder) Karin Amundson, B.S., Cidara Therapeutics (Shareholder) Allen Borchardt, PhD, Cidara Therapeutics (Employee) Thanh Lam, PhD, Cidara Therapeutics (Shareholder) Tom Brady, PhD, Cidara Therapeutics (Shareholder) Elizabeth Abelovski, B.S., Cidara Therapeutics (Shareholder) Simon Döhrmann, PhD, Cidara Therapeutics (Shareholder) Jason Cole, PhD, Cidara Therapeutics (Shareholder) Voon Ong, PhD, Cidara Therapeutics, Inc. (Employee, Shareholder) Les Tari, PhD, Cidara Therapeutics (Shareholder)

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In vitro activity of the novel triazaacenaphthylene gepotidacin (GSK2140944) against MDR Neisseria gonorrhoeae

Journal of Antimicrobial Chemotherapy ◽

10.1093/jac/dky162 ◽

2018 ◽

Vol 73 (8) ◽

pp. 2072-2077 ◽

Cited By ~ 12

Author(s):

Susanne Jacobsson ◽

Daniel Golparian ◽

Nicole Scangarella-Oman ◽

Magnus Unemo

Keyword(s):

Antimicrobial Resistance ◽

Neisseria Gonorrhoeae ◽

Efflux Pump ◽

Resistance Mutation ◽

Vitro Activity ◽

Fluoroquinolone Resistance ◽

Cross Resistance ◽

In Vitro Activity ◽

The Impact

Abstract Objectives Increased antimicrobial resistance surveillance and new effective antimicrobials are crucial to maintain treatable gonorrhoea. We examined the in vitro activity of gepotidacin, a novel triazaacenaphthylene, and the effect of efflux pump inactivation on clinical Neisseria gonorrhoeae isolates and international reference strains (n = 252) and compared gepotidacin with antimicrobials currently or previously recommended for gonorrhoea treatment. Methods MICs (mg/L) were determined by agar dilution (gepotidacin) or by Etest (seven other antimicrobials). The gyrA and parC genes were sequenced and the impact of inactivation of the MtrCDE, MacAB and NorM efflux pumps on gepotidacin MICs was examined. Results Gepotidacin showed potent in vitro activity against all gonococcal isolates (n = 252; MIC ≤4 mg/L). The modal MIC, MIC50, MIC90 and MIC range of gepotidacin were 0.5, 0.5, 1 and 0.032–4 mg/L, respectively. Inactivation of the MtrCDE efflux pump, but not MacAB or NorM, decreased the gepotidacin MICs for most strains. No significant cross-resistance between gepotidacin and any other antimicrobials, including the fluoroquinolone ciprofloxacin, was identified. However, the ParC D86N mutation (possibly together with additional antimicrobial resistance mutation), which is associated with fluoroquinolone resistance, was associated with increased gepotidacin MICs. Conclusions Gepotidacin demonstrated high in vitro activity against gonococcal strains, indicating that gepotidacin could potentially be an effective option for gonorrhoea treatment, particularly in a dual antimicrobial therapy regimen and for patients with resistance or allergy to extended-spectrum cephalosporins. Nevertheless, elucidating in vitro and in vivo resistance emergence and mechanisms in detail, together with further gonorrhoea clinical studies, ideally also including chlamydia and Mycoplasma genitalium are essential.

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