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

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

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

The Use of natural Products in 3D Printing of Pharmaceutical Dosage Forms

Background Three-dimensional printing (3DP) has been investigated widely for applications in pharmaceutical sciences. Different 3DP techniques have been employed such as fused deposition modelling (FDM 3DP), powder bed 3DP, stereolithography 3DP (SLA 3DP), selective laser sintering (SLS 3DP), pates-extrusion 3DP and inkjet 3DP. Aim This article aims to explore the use of natural products as active ingredient or excipient. Methods Literature search was conduced for latest applications of 3DP for pharmaceutical dosage forms, and typical employed materials were identified. Results Polymeric materials form the main bulk of 3DP excipients such as polyvinyl alcohol or ploy lactic acid. Chemical stabilisers may be added to these polymers to increase their stability at high temperatures during hot melt extrusion for making filaments or printing. In addition, photoinitiators have been added such as diphenyl(2,4,6-trimethylbenzoyl) phosphine oxide in SLA 3DP, or candurin gold sheen in SLS 3DP. Presence of lead has been detected in FDM £DP, which originated from the nozzle. Currently, natural products have been employed only in paste extrusion 3DP of pharmaceutical dosage forms. We have identified a protentional natural thermoplastic polymer that may be used in 3DP FDM. Conclusion Natural products may be employed in 3DP of pharmaceutical dosage forms to improve the safety profile of printed objects.   Key words: Three-dimensional printing; polymers; thermoplastics; photoinitiators, natural polymer

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.&nbsp