Journal of Natural Products Discovery (LJMU)
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Stability of Feverfew and its Active Principle Parthenolide: An Elusive Antimigraine Herbal Medicine
Background
Feverfew is a traditional herbal remedy for the relief of arthritis, migraine, toothache, and menstrual difficulties. It is widely accepted that parthenolide, a sesquiterpene lactone, is its main active principle. However, the decrease of parthenolide in commercial preparations is a well-known process with no technical solution so far.
Aims
To review the evidence for the mechanism of the degradation of parthenolide and similar sesquiterpene lactones.
Methods
Systematic review.
Results and Conclusion
In conclusion, and without discarding any degradation of parthenolide into non-identifiable fragments, the fate of this compound in dry, powdered feverfew is to undergo a covalent binding to plant proteins resulting in a biologically inactive adduct - in accordance with the direct and indirect data found in the literature. This process seems to be virtually unstoppable, and temperature and light do not seem to be playing a significant role under normal storage conditions according to some authors. In the presence of a high level of humidity, parthenolide may undergo an acid-induced cyclisation giving rise to a guaianolide-type sesquiterpene lactone, a class of compound that is commonly found in Feverfew. Microbial degradations are not likely to play an important role if the formulation complies with Pharmacopoeial microbiological quality requirements. The experimental and clinical data in the literature do not report on any increase in the toxicity of stored feverfew. 
Journal of Natural Products Discovery (JNPD): Covering Natural Products Research From A New Perspective
Natural products have long been utilized as a source of food, medicine and other commercially important materials and products, and because of this, natural products, from plants, microbes or animals, have been studied extensively in the ever-ending search for new products, particularly new drug candidates. Historically, several ‘block buster’ drugs like the anticancer drugs taxol, vincristine and vinblastine, antibiotics like penicillins and cephalosporins, and the narcotic analgesic morphine were discovered from natural sources, either from plants or microbes.
Over the last couple of decades, particularly since the appearance of the ‘open access’ platform, the number of journals that claim to cover research in the area of natural products has mushroomed. However, with the exception of a few reputed journals in this area, most of the other journals have become just a business venture, they charge large sum of money from the authors in the name of so called ‘page charge’, ‘processing charge’ or ‘publication charge’, and publish almost anything and everything without assessing the quality of publications. Most often, all these publications are repetitive, the same findings in a new package or even shamelessly plagiarised from previously published articles and have little or no applied scientific values. Moreover, most of the journals catering for natural products research cover mainly academic research without any tangible outcomes or discoveries that can lead to product development.
Journal of Natural Products Discovery (JNPD), which is the official journal of the Centre for Natural Products Discovery (CNPD) at Liverpool John Moores University (LJMU), will stand out from the crowd because of its product-discovery-focussed approach. The coverage will be focussed more to discoveries of new products or new applications of already known natural products in relation to food, pharmaceuticals, cosmetics and other commercial products.
The Centre for Natural Products Discovery (CNPD) was founded within the School of Pharmacy and Biomolecular Sciences at LJMU about three years ago with the aim to facilitate world-class research in natural products discovery impacting on societal, national and global needs. This centre has already organised successfully two international conferences in 2020 and 2021, and the third anniversary conference will be held in March 2022. A brand-new MSc programme in Natural Products Discovery was launched last year, as a part of the initiatives from CNPD to embed natural products research and to disseminate knowledge at various levels. Similarly, a monthly research newsletter was also launched a year ago to capture various activities of the centre. Publication of this new journal will further strengthen the activities of the centre and this journal will become one of the main outlets for communicating our research activities to a wider audience using the open access platform, sponsored by the LJMU Library.
In this connection, we gratefully acknowledge the outstanding support and assistance that we have received from Ms Catherine Dishman to establish this platform and set up the journal online submission system. We would also like to express our gratitude to our colleague Dr Jose Prieto Garcia (Executive Editor-in-Chief), who worked closely with Catherine, all other colleagues of the CNPD and us to establish this journal, and to make this very first issue possible. This journal is in open access, and there is no charge whatsoever levied to the authors, meaning the publication in this journal is completely free!
We hope this journal will grow rapidly as one of the leading journals in the field of natural products research and will attract the finest quality publications from researcher from all over the world
DICHLOROMETHANE EXTRACT OF THE LEAVES OF ARBUTUS PAVARII PAMP. EXHIBITS CYTOTOXICITY AGAINST THE PROSTATE CANCER CELL LINE PC3: A BIOASSAY-GUIDED ISOLATION AND IDENTIFICATION OF ARBUTIN AND BETULINIC ACID METHYL ESTER
Background: Arbutus pavarii Pamp. (fam. Ericaceae), commonly known as “Shmeri”, “Shmar” and “Libyan Strawberry”, is an endemic Libyan medicinal plant, growing almost exclusively in the Al-Jabel Al-Akhdar mountainous region in Libya.
Aims: To assess the cytotoxicity of A. pavarii against human cancer cell lines and to carry out bioassay-guided isolation and identification of compounds.
Materials and Methods: Shed-dried and ground leaves of A. pavarii were Soxhlet-extracted, successively, with n-hexane, dichloromethane (DCM) and methanol (MeOH), and assessed for cytotoxicity against several human cancer cell lines using the MTT assay. The cytotoxicity of the DCM extract against the normal human prostate cell line PNT2 was also assessed to determine the selectivity index (SI). The DCM extract was subjected to vacuum liquid chromatography (VLC) to produce eight fractions. A reversed-phase preparative HPLC analysis of the active VLC fraction was carried out to purify the major compounds present in the active fraction, and the structures of the compounds were elucidated by spectroscopic means.
Results: The DCM extract was more cytotoxic against the PC3 cell line (IC50= 26 mg/mL) but less to the normal human prostate cell line PNT2 (IC50 = 90 mg/mL) with a selectivity index of 3.5. VLC analysis produced 8 fractions, with fraction VLC-5 most active against PC3 cells. Prep-HPLC-based purification of VLC-5 afforded the isolation of arbutin (1) and betulinic acid methyl ester (2), the structures of which were elucidated by spectroscopic means.
Conclusion: The DCM extract of the leaves of A. pavarii exhibited significant cytotoxicity to PC3 cells, but much less cytotoxicity against normal human prostate cell line. The isolated compounds from the active fraction, arbutin (1) and betulinic acid methyl ester (2), which were previously shown to possess cytotoxic properties, could be responsible for the cytotoxicity of the DCM extract
Therapeutic potential of Leea indica (Vitaceae)
Background
Leea indica (Burm. f.) Merr. (fam. Vitaceae), commonly known as ‘bandicoot berry’, is a Thai medicinal plant, and distributed widely in the far-east and south-east Asian countries, and in some parts of northern Australia. In Thailand, this plant has traditionally been used for the treatment of diarrhoea, pain, gastric ulcer, viral infections and some forms of cancers.
Aims
To review published findings on medicinal properties of L. indica and to critically appraise its therapeutic potential.
Methods
A comprehensive literature search was performed utilizing several databases, notably, Web of Science, PubMed and Google Scholar, and other relevant published materials. The keywords used in the search, individually as well as in combinations, were Leea indica, Vitaceae and traditional medicine.
Results
In vitro assays and in vivo animal studies displayed efficacy of the extracts and fractions of L. indica as an analgesic, antidiabetic, anti-inflammatory, antimicrobial, antioxidant and antiproliferative agent and indicated their therapeutic potential. Phytochemical studies revealed the presence of alkaloids, flavonoids, polyphenolics and terpenoids as major bioactive components in L. indica.
Conclusion
Preliminary bioactivity studies on L. indica provided some scientific basis for its traditional therapeutic applications. The presence of certain bioactive compounds in this plant could further support its therapeutic potential and traditional medicinal uses
Natural Products Discovery: Caveats, Considerations, Collaboration, Creativy and Contemporary Technology
oai:openjournals.ljmu.ac.uk:article/599There exists an enormous global need for new, safe, and effective drugs for a broad range of chronic and acute diseases. Most of these exigencies will not be met by “big Pharma”, ever. Consequently, in many countries, for a healthier and more productive population this pharmaceutical “chasm” must be bridged through alternative discovery efforts. At a time when environmental consciousness is increasing, and oil and coal processing for solvents and chemicals will likely be diminished in the future, synthetic pharmaceuticals cannot be relied on to serve as that bridge for the long-term. Natural products have continued to be a steady source of pharmaceuticals in the past 30 years (Newman & Cragg, 2020). However, a more emphatic, structured, and sustainable return to nature, using the contemporary technologies now available, is by far the best option to address global needs (Daley et al., 2021). This brief letter offers some general thoughts on natural product drug discovery programs and their initiation, operation, and development. It is not an exhaustive assessment, neither are the issues raised fully discussed, thus only a few key references are cited. The intention is to offer a background framework for scientists interested in this vast area of natural product research as they consider conducting their programs and publishing in this new and exciting journal. Five general areas of research development are presented: Caveats, Considerations, Collaborations, Creativity, and Contemporary Technology. 
Acne vulgaris: the skin microbiome, antibiotics and whether natural products could be considered a suitable alternative treatment?
Acne vulgaris is a common, chronic inflammatory skin disease manifested as inflammatory and non-inflammatory lesions typically associated with Cutibacterium acnes. However, its pathogenesis is not fully understood nor is the complexity of the skin microbiome and how it contributes to the development of acne. Whilst acne is not a typical bacterial infection, antibiotics have been the mainstay of treatment for over 50 years. Now, with the development of multi-drug resistant organisms and the emergence of resistant C. acnes strains; the question is are antibiotics still an appropriate treatment method or could natural products provide a suitable alternative? Research into alternative treatments is a growing field due to the increase in resistant organisms, there is a multitude of research into natural products due to their antimicrobial potential and the multiple mechanisms of action. Melaleuca alternifolia is a key natural product of interest in the treatment of acne due to its documented use throughout history and its prevalence in over the counter treatments. Green Tea is a more recent natural product of interest due to its composition of polyphenols, which give rise to both antimicrobial and anti-inflammatory properties. However, research also suggests that a synergistic approach of natural products may be the way forward
PHYTOCHEMICAL FINGERPRINT AND BIOLOGICAL ACTIVITIES OF THREE MALAYSIAN FICUS DELTOIDEA CULTIVARS.
Background
Ficus deltoidea (Moraceae), is a Malay Traditional Medicine locally known as Mas Cotek. Three varieties (angustifolia, deltoidea and kunslerii) has been indictincty used.
Aims
We here aim to better understand their chemistry and bioactivities to inform future scientific and agronomic research.
Methods
We extracted and analyzed samples from these varieties by HPTLC and HPLC-UV. The in vitro screening looked up to the scavenging activities against both DPPH and NO radicals, inhibitory activity upon tyrosinase and cytotoxicity against human prostate cancer cells PC3, DU145 and LNCaP using the sulforhodamine B proliferation assay and the MTT mitochondrial viability assay.
Results
We achieved to analytically differentiate the three varieties in term of the presence of flavonoids, establishing that vitexin, orientin and isoorientin may act as intraspecific and interorgan phytomarkers Their biological activities point out to the antioxidant value of extracts from the deltoidea and kunslerii varieties whilst the inhibition of tyrosinase is only present in the roots extract of the var. deltoidea which here we show is also endowed with cytotoxic activity against prostate cancer cells.
Conclusion
We suggest that the three Malaysian Ficus deltoidea botanical varieties (angustifolia, deltoidea and kunslerii) can be also considered chemovars. The least bioactive chemovar was angustifolia. The most active extract was from the roots of var. deltoidea that shows antioxidant, antimelanogenic and cytotoxic potential.
Keywords: Chemotaxonomy; Prostate Cancer; Tyrosinase; Antioxidant; Ficus
OLAX SUBSCORPIOIDEA OLIV. (OLACACEAE): AN ETHNOMEDICINAL AND PHARMACOLOGICAL REVIEW
Background
Olax subscorpioidea Oliv. (Olacaceae) is a woody shrub that is widely distributed in Africa. It has trado-medicinal importance and is used in the treatment of asthma, cancer, convulsion, diabetes, intestinal worm infections, jaundice, mental illnesses, neurodegenerative disorders, sexually transmitted infections, swellings and rheumatism, and yellow fever.
Aims
To review available literature on the phytochemistry, ethnobotany, pharmacology and toxicity of Olax subscorpioidea Oliv.
Methods
Published findings were searched in online databases such as Web of Science, Scopus, Pubmed, Google Scholar and other relevant sources, and the data were sorted by relevance. Combinations of keywords used in the search include Olax subscorpioidea, Olacaceae, Olax, Ewe Ifon, and African medicinal plants.
Results
The presence of alkaloids, anthraquinones, cardiac glycosides, flavonoids, phenolic compounds, proanthocyanidins, saponins, tannins and triterpenes has been reported from O. subscorpioidea. Cytotoxic santalbic acid was isolated from the methanol extract of the seed of this plant, while GC-MS and HPLC analyses of the n-butanol and n-hexane extracts of the leaf revealed the presence of caffeic acid, quercetin, morin, rutin, n-hexadecanoic acid (palmitic acid), 7,10,13-hexadecatrienoic acid and methyl ester, hentriacontane, 9,17-octadecadienal (Z)-, 9,12-octadecadienoic acid (Z,Z)-, squalene, nonacosane, octadecanoic acid. Bioactivity studies on this plant demonstrated its medicinal potential mainly as an analgesic, anthelmintic, anti-arthritic, antidepressant, antihyperglycaemic, anti-inflammatory, antioxidant, antimalarial and antimicrobial agent. Oral acute toxicity of the leaf extracts in rats appeared to be greater than 5,000 mg/kg body weight.
Conclusion
Published literature available to date on O. subscorpioidea provides some preliminary scientific basis for the ethnomedicinal uses of this plant. However, some ethnomedicinal uses have not been scientifically validated yet, and similarly, only a limited amount of information is available on properly isolated and identified phytochemicals from this plant that link to its bioactivitie