Indole Alkaloids of <i>Haplophyton crooksii</i>

Mroue, M.A.; Euler, K. L.; Ghuman, M.A.; Alam, Maktoob

doi:10.1021/np960070c

Cited by 37 publications

(21 citation statements)

References 15 publications

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“…The most active of these alkaloids (16-decarbomethoxyvinervine, IC50 = 57 µM) was about 38 times less active than physostigmine (IC95 = 4.8 µM). This could be a partial explanation for the neurotoxicity of these compounds and of H. crooksii but the ganglion-blocking activity should still be tested [92].…”

Section: Other Familiesmentioning

confidence: 99%

Natural Product Inhibitors of Acetylcholinesterase

Hostettmann¹,

Borloz²,

Urbain³

et al. 2006

COC

135

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Various natural products, such as physostigmine, have long been recognized as inhibitors of the enzyme acetylcholinesterase. Since the recent approval of galanthamine for the treatment of Alzheimer's disease by the blockage of acetylcholine degradation, attempts to find other inhibitors of the enzyme have multiplied, leading to promising candidates such as huperzine A. In this review, a listing is presented of natural product inhibitors, both alkaloid and nonalkaloid in origin. These have been isolated from plant, animal and microbial sources. Details of current testing methods on cholinesterases are given, including solution assays and screening techniques by TLC and HPLC.

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Section: Other Familiesmentioning

confidence: 99%

Natural Product Inhibitors of Acetylcholinesterase

Hostettmann¹,

Borloz²,

Urbain³

et al. 2006

COC

135

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“…Each of them was tested at the concentration of 0.8 mg/mL, and both activities were considered moderate when compared to the 100.0 + 0.0% inhibition displayed by galantamine [44]. From Haplophyton crooksii (Apocynaceae) were isolated 15 indole alkaloids [45][46][47]. All these compounds showed in vitro inhibition of AChE in the Ellman's test, at different concentration levels, but the most active metabolites, 10-methoxy-N1-methylpericyclivine (54, IC 50 : 1.35 µM) and 16-decarbomethoxyvinervine (55, IC 50 : 0.57µM) (Fig.…”

Section: Commercial Drugs For Ad Treatmentmentioning

confidence: 99%

New Anti-Alzheimer Drugs from Biodiversity: The Role of the Natural Acetylcholinesterase Inhibitors

Viegas¹,

Bolzani²,

Barreiro³

et al. 2005

MRMC

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Alzheimer's disease (AD) is a progressive neurodegenerative pathology with severe economic and social impact. There is currently no cure, although cholinesterase inhibitors provide effective temporary relief of symptoms in some patients. Nowadays, drug research and development are based on the cholinergic hypothesis that supports the cognition improvement by regulation of the synthesis and release of acetylcholine in the brain. There are only four commercial medicines approved for treatment of AD, and natural products have played an important alternative role in the research for new acetylcholinesterase inhibitors, as exemplified through the discovery of galantamine. This profile conducts us to give in this paper an overview relating the several classes of natural products with anti-cholinesterasic activity as potential templates to the design of new selective and powerful anti-Alzheimer drugs.

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“…Compared to the standard inhibitor eserine, akuammiline alkaloid lanceomigine showed weak activity (IC 50 eserine = 0.0015 mM; IC 50 lanceomigine = 0.383 mM) [47].…”

Section: The Antimicrobial Activity Of the Extracts Of A M A C R O mentioning

confidence: 91%

Current Progress in the Chemistry and Pharmacology of Akuammiline Alkaloids

Ramı́rez

García-Rubio²

2003

CMC

224

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Akuammiline alkaloids are a family of monoterpene indole alkaloids of renewed medicinal interest. These bases act as ligands for a heterogeneous group of molecular targets and, consequently, display a wide variety of pharmacological activities. For example, pseudoakuammigine (2) exhibits opioid activity in vivo, echitamine (4) has been reported to have promising cytotoxic activity, and corymine (121) behaves as an antagonist of the glycine receptor. Oddly enough, these alkaloids have not raised enough interest in the organic synthesis community, remaining inaccessible; even the entry to their pentacyclic framework continues elusive. Recently, several akuammiline bases have been isolated and identified including bisindole alkaloids, such as vingramine (103) or rausutrine (110), which incorporate akuammiline-type subunits. This review covers the advances in the chemistry and pharmacology of akuammiline alkaloids reported within the last ten years.

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Indole Alkaloids of Haplophyton crooksii

Cited by 37 publications

References 15 publications

Natural Product Inhibitors of Acetylcholinesterase

Natural Product Inhibitors of Acetylcholinesterase

New Anti-Alzheimer Drugs from Biodiversity: The Role of the Natural Acetylcholinesterase Inhibitors

Current Progress in the Chemistry and Pharmacology of Akuammiline Alkaloids

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