Natural product as a source of prodrug

Padmavathy, J.; Saravanan, Devarajan

doi:10.3329/bjp.v12i2.31020

Cited by 8 publications

(5 citation statements)

References 44 publications

(46 reference statements)

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“…It is also conceivable that prodrugs in the milieu of DLA are activated by in-vivo metabolism. In-vivo transformation of prodrugs present in the material of plants into biologically active compounds has precedent [ 61 ] and would explain the discrepancy in the efficacies of in-vitro and in-vivo models. Future experiments should explore modulation of infected host immune systems, digestion systems, and DLA-ART human pharmacokinetics.…”

Section: Discussionmentioning

confidence: 99%

In vitro analyses of Artemisia extracts on Plasmodium falciparum suggest a complex antimalarial effect

Gruessner

Weathers

2021

PLoS ONE

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Dried-leaf Artemisia annua L. (DLA) antimalarial therapy was shown effective in prior animal and human studies, but little is known about its mechanism of action. Here IC50s and ring-stage assays (RSAs) were used to compare extracts of A. annua (DLAe) to artemisinin (ART) and its derivatives in their ability to inhibit and kill Plasmodium falciparum strains 3D7, MRA1252, MRA1240, Cam3.11 and Cam3.11rev in vitro. Strains were sorbitol and Percoll synchronized to enrich for ring-stage parasites that were treated with hot water, methanol and dichloromethane extracts of DLA, artemisinin, CoArtem™, and dihydroartemisinin. Extracts of A. afra SEN were also tested. There was a correlation between ART concentration and inhibition of parasite growth. Although at 6 hr drug incubation, the RSAs for Cam3.11rev showed DLA and ART were less effective than high dose CoArtem™, 8 and 24 hr incubations yielded equivalent antiparasitic results. For Cam3.11, drug incubation time had no effect. DLAe was more effective on resistant MRA-1240 than on the sensitive MRA-1252 strain. Because results were not as robust as observed in animal and human studies, a host interaction was suspected, so sera collected from adult and pediatric Kenyan malaria patients was used in RSA inhibition experiments and compared to sera from adults naïve to the disease. The sera from both age groups of malaria patients inhibited parasite growth ≥ 70% after treatment with DLAe and compared to malaria naïve subjects suggesting some host interaction with DLA. The discrepancy between these data and in-vivo reports suggested that DLA’s effects require an interaction with the host to unlock their potential as an antimalarial therapy. Although we showed there are serum-based host effects that can kill up to 95% of parasites in vitro, it remains unclear how or if they play a role in vivo. These results further our understanding of how DLAe works against the malaria parasite in vitro.

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Section: Discussionmentioning

confidence: 99%

In vitro analyses of Artemisia extracts on Plasmodium falciparum suggest a complex antimalarial effect

Gruessner

Weathers

2021

PLoS ONE

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“…Because of multiple pharmacological activities, natural products are being increasingly screened for agents to treat various diseases [ 16 , 17 ]. Sodium oligomannate, which is commercially named as GV-971, has been reported to treat mild-to-moderate AD by regulating neuroinflammation implicated by amino acids of the gut bacteria [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

The Neuroprotection of Verbascoside in Alzheimer’s Disease Mediated through Mitigation of Neuroinflammation via Blocking NF-κB-p65 Signaling

et al. 2022

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Verbascoside (VB) is a phenylethanoid glycoside extracted from the herbaceous plant Verbascum sinuatum and plays a neuroprotective role in Alzheimer’s disease (AD). The goal of this study was to explore the neuroprotective mechanism of VB. Based on the proteomics analysis, immunohistochemistry, immunofluorescence, Western blot, and ELISA were utilized to explore the neuroprotective mechanism of VB in context of neuroinflammation in APP/PS1 mice, LPS-induced BV2 cells, and/or Aβ1-42-stimulated N2a cells. Proteomic analysis demonstrated that the neuroprotection of VB correlated closely to its anti-inflammatory effect. VB significantly blocked microglia and astrocyte against activation in brains of APP/PS1 mice, suppressed the generation of IL-1β as well as IL-6, and boosted that of IL-4, IL-10 and TGF-β in vivo, which were analogous to results acquired in vitro. Furthermore, VB effectively restrained the phosphorylation of IKKα+β, IκBα, and NF-κB-p65 in APP/PS1 mice; LPS-induced BV2 cells, and Aβ1-42-stimulated N2a cells and lowered the tendency of NF-κB-p65 translocation towards nucleus in vitro. These results demonstrate that the neuroprotective effect of VB correlates to the modulation of neuroinflammation via NF-κB-p65 pathway, making VB as a hopeful candidate drug for the prevention and treatment of AD.

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“…Plants and their extracts are used by oral route. It is well known that many of the chemical constituents present in the extract undergo metabolism in the intestine or liver (first-pass effect) after oral administration ( Padmavathy and Saravanan, 2017 ). Hence, some of the phytoconstituents may be prodrugs that may get activated upon metabolism and may show anti-cancer effects in-vivo .…”

Section: Discussionmentioning

confidence: 99%

Assessment of the anti-cancer potential of Ephedra foeminea leaf extract on MDA-MB-231, MCF-7, 4 T1, and MCF-10 breast cancer cell lines: Cytotoxic, apoptotic and oxidative assays

Abdulkarim Alharbi,

Eldin Ahmed Abdelsalam,

Asad

et al. 2024

Saudi Pharmaceutical Journal

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Natural product as a source of prodrug

Cited by 8 publications

References 44 publications

In vitro analyses of Artemisia extracts on Plasmodium falciparum suggest a complex antimalarial effect

In vitro analyses of Artemisia extracts on Plasmodium falciparum suggest a complex antimalarial effect

The Neuroprotection of Verbascoside in Alzheimer’s Disease Mediated through Mitigation of Neuroinflammation via Blocking NF-κB-p65 Signaling

Assessment of the anti-cancer potential of Ephedra foeminea leaf extract on MDA-MB-231, MCF-7, 4 T1, and MCF-10 breast cancer cell lines: Cytotoxic, apoptotic and oxidative assays

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