Jan G. Bruhn

Adhatoda vasica : a critical review of ethnopharmacological and toxicological data

Adhatoda vasica (L.) Nees is a well-known plant drug in Ayurvedic and Unani medicine. It has been used for the treatment of various diseases and disorders, particularly for the respiratory tract ailments. During the last 20 years, several scientific reports on oxytocic and abortifacient effects of vasicine and alkaloid derived from the plant have appeared. This leads to questions concerning the safety of A. vasica as a herbal medicine. In this article, the major data on traditional uses as well as ethnopharmacological and toxicological studies, both published and unpublished, are reviewed and commented upon. The data have been evaluated from the point of view of correctness, reliability, relevance and importance for the overall evaluation of the safety of A. vasica.

Gynostemma pentaphyllum : identification of major sapogenins and differentiation from Panax species

Four main dammarane-type aglycones of gypenosides, extracted from the aerial parts of Gynostemma pentaphyllum were identified by gas chromatography-mass spectrometry. By detecting these aglycones as well as the aglycones of ginsenosides, a difference in sapogenin composition between Gynostemma pentaphyllum and Panax species was observed, which can be used in the differentiation of these plant drugs.

Mescaline use for 5700 years

Archaeological investigations in northeast Mexico and Trans-Pecos, Texas have shown that the use of psychotropic drugs in this region goes back to around 8500 BC. The aboriginal inhabitants of this region used the mescal bean, Sophora secundiflora, and buttons from the peyote cactus, Lophophora williamsii1. From an archaeological site in Coahuila, Mexico, several peyote buttons were retrieved and radiocarbon-dated to AD 810–1070. Alkaloid analysis revealed the presence of mescaline and four related tetrahydroisoquinoline alkaloids2. We have, however, analysed two much older samples of peyote buttons. These samples are thought to have been found in Shumla Cave number five on the Rio Grande, TX, USA, and are in the collection of the Witte Museum in San Antonio3. Radiocarbon dating showed a mean age of 5700 years. Standard alkaloid extraction procedures done on the samples gave residues that were analysed by thin-layer chromatography and gas chromatography-mass spectrometry. We were able to identify mescaline in both samples, based on identical retention times and Rf values, and similar mass-to-charge ratios and fragmentation pattern. The detection of mescaline in two different samples, both analysed by two methods based on different principles, is reliable evidence for the presence of this psychotropic drug. Freshly prepared peyote buttons can contain up to 8% of total alkaloids. The previously studied 1000-year-old sample had a lower content, around 2·25%. In our analysis, alkaloid content had fallen to 2%, and mescaline was the only peyote alkaloid we could identify. There was no trace of any of the other tetrahydroisoquinoline alkaloids typical for peyote. Earlier, nicotine and caffeine had been identified in plant remains from a medicine mans tomb in Bolivia, aged 1600 years4. Morphine has been found in a 3500 year old ceramic container from Cyprus5. From a scientific perspective, the studied peyote material seems to be the oldest plant drug that yielded a major bioactive compound on chemical analysis. From a cultural point of view, our identification of mescaline strengthens the evidence that Native Americans already recognised and valued the psychotropic properties of peyote as long as 5700 years ago.

Bioassay methods in natural product research and drug development

Bioassay methods in natural product research and drug development : proceedings of the international symposium on Bioassay Methods in Natural Product Research and Drug Development, held at the Biomedical Centre of Uppsala University, Sweden, from 24-27 August 1997

Alkaloids and ethnobotany of Mexican peyote cacti and related species

Some Mexican cacti of the genera Ariocarpus, Mammillaria, Obregonia, Pelecyphora, Solisia and Turbinicarpus have been studied with respect to their alkaloids and ethnobotany. Seven previously known cactus alkaloids were identified. N,N-Dimethyl-4-hydroxy-3-methoxyphenethylamine was found to occur in Ariocarpus agavoides. In Pelecyphora aselliformis N,N-dimethyl-3-hydroxy-4, 5-dimethoxyphenethylamine was identified as the major alkaloid. The possible relationship between the vernacular names of these plants and their alkaloid content is discusse.

Early peyote research an interdisciplinary study

Summary1.The first person to draw the attention of the scientific world to peyote was doubtless Dr. J. R. Briggs, and not Mrs. A. B. Nickels as is often stated.2.The first report of alkaloids in peyote seems to be the laboratory report by F. A. Thompson at Parke-Davis, although Louis Lewin was the first to publish.3.The variability ofLophophora williamsii and imperfect knowledge of the species laid the foundation for the controversy over botanical names. Only recently have field studies in Mexico indicated that there are two species,Lophophora williamsii andL. diffusa, differing in distribution and chemical characters.Anhalonium lewinii is now referred toL. williamsii.4.Present and earlier studies of the Querétaro peyote,Lophophora diffusa, show that this species differs considerably in its alkaloid set-up fromL. williamsii. L. diffusa produces predominantly (>90%) phenolic tetrahydroisoquinoline alkaloids (mainly pellotine) and almost no mescaline. This lends support to the earlier postulation of an independent metabolic pathway to pellotine and anhalidine.5.In our opinion, Heffter’s results withAnhalonium williamsii can be explained if we assume that his plant material was collected in Querétaro and was in factL. diffusa. The alkaloid analysis ofL. diffusa also provides an explanation of other controversial points in the history of peyote research.22 It seems especially appropriate here to recall that Kauder (p. 23) said: “The circumstances seem to me to call for further clarification, which will only be possible when we succeed in obtaining that cactus, which only contains pellotine.”6.An 80-year old sample of “mescal buttons” has been shown to still contain identifiable alkaloids, most notably mescaline.

Alkaline cleavage of gypenosides and characterization of dammarane-type aglycones by gas chromatography–mass spectrometry

Five dammarane-type aglycones, released from gypenosides following an alkaline cleavage procedure previously developed for ginsenosides, were separated and characterized by gas chromatography-mass spectrometry (GC-MS) after trimethylsilylation. A satisfactory identification among isomers of 20(S)-protopanaxadiol or 20(S)-protopanaxatriol was obtained.

Molecular Pharmacognosy : an explanatory model

Increased interest in the study of natural products as potential drugs and rapidly changing research strategies are driving us to reassess the role of pharmacognosy in the wider context of pharmaceutical research. The authors propose a new definition and an explanatory model of modern pharmacognosy that can be used as a theoretical foundation for future development of this classical branch of the life sciences.

Was opium known in 18th dynasty ancient Egypt? An examination of materials from the tomb of the chief royal architect Kha

Examination by microscopy, thin-layer chromatography, gas-liquid chromatography alone and combined with mass spectrometry, and radioimmunoassay methods of materials from the tomb of the ancient Egyptian chief royal architect Kha, who is believed to have died about 1405 BC, has shown that there is no morphine--and hence no opium--present. This finding casts doubt on the results of an earlier analysis. Tropane alkaloids are likewise absent. The significance of the present findings for the history of the opium poppy, Papaver somniferum L., in the eastern Mediterranean region is discussed. Evidence (chemical, botanical, artefactual, and linguistic) for the supposed presence of the opium poppy and opium in Egypt in the Late Bronze Age is briefly reviewed. These considerations and the negative outcome of the present analyses mean that the earlier reported finding can no longer be accepted as evidence.

A Cactus-Derived Toxin-Like Cystine Knot Peptide with Selective Antimicrobial Activity

Naturally occurring cystine knot peptides show a wide range of biological activity, and as they have inherent stability they represent potential scaffolds for peptide‐based drug design and biomolecular engineering. Here we report the discovery, sequencing, chemical synthesis, three‐dimensional solution structure determination and bioactivity of the first cystine knot peptide from Cactaceae (cactus) family: Ep‐AMP1 from Echinopsis pachanoi. The structure of Ep‐AMP1 (35 amino acids) conforms to that of the inhibitor cystine knot (or knottin) family but represents a novel diverse sequence; its activity was more than 500 times higher against bacterial than against eukaryotic cells. Rapid bactericidal action and liposome leakage implicate membrane permeabilisation as the mechanism of action. Sequence homology places Ec‐AMP1 in the plant C6‐type of antimicrobial peptides, but the three dimensional structure is highly similar to that of a spider neurotoxin.