Search results for "Natural product"
showing 10 items of 163 documents
3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin Analogues with antiproliferative activity
2015
A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (~60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunctio…
Indole Diterpenoids from an Endophytic Penicillium sp.
2019
A chemical investigation of the endophyte Penicillium sp. (strain ZO-R1-1), isolated from roots of the medicinal plant Zingiber officinale, yielded nine new indole diterpenoids (1-9), together with 13 known congeners (10-22). The structures of the new compounds were elucidated by 1D and 2D NMR analysis in combination with HRESIMS data. The absolute configuration of the new natural products 1, 3, and 7 was determined using the TDDFT-ECD approach and confirmed for 1 by single-crystal X-ray determination through anomalous dispersion. The isolated compounds were tested for cytotoxicity against L5178Y, A2780, J82, and HEK-293 cell lines. Compound 1 was the most active metabolite toward L5178Y ce…
Lemon post-harvest decay control by natural products
2008
Postharvest diseases of lemon fruits represent one of the most severe sources of loss production. They are controlled by imazalil (IMZ), thiabendazole (TBZ) and sodium ortho-phenil-phenate (SOPP) registered fungicides for postharvest treatments. Nowadays, the chemical use is becoming more restricted for environmental concerns and development of fungicide-tolerance strains of fungal pathogens. In the last few years a renewed interest in alternative methods of postharvest decay control has been increasing and the research for natural products has provided encouraging results. The aim of this research has been the in vitro and in vivo effectiveness evaluation of six essences (garlic, cloves, o…
Total synthesis and biological evaluation of seven new anti-inflammatory oxacyclododecindione-type macrolactones
2020
Through variation of our previously published total synthesis of two highly active anti-inflammatory macrolactones from the oxacyclododecindione family (J. Tauber, M. Rohr, T. Walter, G. Erkel and T. Opatz, Org. Biomol. Chem., 2015, 13, 7813-7821), seven new representatives of this compound class were prepared. Substitution of the 14-hydroxy group in oxacyclododecindione with a methyl substituent provided a readily accessible non-natural analogue which has similar pharmacological properties to the scarcely available natural product. Since the producible amount of substance is therefore no longer restricted by low fermentation yields, extensive in vivo studies become possible for the first t…
Marine molecular biology : An emerging field of biological sciences
2007
An appreciation of the potential applications of molecular biology is of growing importance in many areas of life sciences, including marine biology. During the past two decades, the development of sophisticated molecular technologies and instruments for biomedical research has resulted in significant advances in the biological sciences. However, the value of molecular techniques for addressing problems in marine biology has only recently begun to be cherished. It has been proven that the exploitation of molecular biological techniques will allow difficult research questions about marine organisms and ocean processes to be addressed. Marine molecular biology is a discipline, which strives t…
2018
Marine sponges are a very attractive and rich source in the production of novel bioactive compounds. The sponges exhibit a wide range of pharmacological activities. The genus Amphimedon consists of various species, such as viridis, compressa, complanata, and terpenensis, along with a handful of undescribed species. The Amphimedon genus is a rich source of secondary metabolites containing diverse chemical classes, including alkaloids, ceramides, cerebrososides, and terpenes, with various valuable biological activities. This review covers the literature from January 1983 until January 2018 and provides a complete survey of all the compounds isolated from the genus Amphimedon and the associate…
MAPs in Sicily: cultivation, uses, and potentiality
2013
In Sicily, MAPs have been used and cultivated for centuries, with many uses ranging from the preparation of fresh or stored food items, flavoring of foods and beverages, home-made human or animal therapy or even aesthetical purposes. Many of them grow spontaneously into such areas, and are claimed to play a significant role inside land biodiversity. The widespread belief that only under “natural” conditions MAPs find their optimum quality features has driven in many cases to their uncontrolled collection from the wild, and as a result many of them are nowadays at a risk of extinction. The field cropping of such spontaneous species could play an important role in safeguarding biodiversity, a…
Fungal Biofilms as a Valuable Target for the Discovery of Natural Products That Cope with the Resistance of Medically Important Fungi—Latest Findings
2021
The development of new antifungal agents that target biofilms is an urgent need. Natural products, mainly from the plant kingdom, represent an invaluable source of these entities. The present review provides an update (2017–May 2021) on the available information on essential oils, propolis, extracts from plants, algae, lichens and microorganisms, compounds from different natural sources and nanosystems containing natural products with the capacity to in vitro or in vivo modulate fungal biofilms. The search yielded 42 articles; seven involved essential oils, two Brazilian propolis, six plant extracts and one of each, extracts from lichens and algae/cyanobacteria. Twenty articles deal with th…
An enantioselective synthesis of the C(33)–C(37) fragment of Amphotericin B
2003
An enantioselective synthesis of the C(33)–C(37) tripropionate fragment of Amphotericin B has been developed in only 6 steps. Peer reviewed
A surprising switch in absolute configuration of anti-inflammatory macrolactones.
2016
Oxacyclododecindione-type macrolactones exhibit highly potent anti-inflammatory activities even at nanomolar concentration. After the determination of the relative configuration of the stereocenters at C14 and C15 by total synthesis of 4-dechloro-14-deoxyoxacyclododecindione and 14-deoxyoxacyclododecindione, the absolute configuration has now been assigned by X-ray crystallography. Surprisingly, the absolute configuration is (14S,15R) which differs for C15 from that of the well-known derivatives of (S)-curvularin. The biological activities of both enantiomers of 14-deoxyoxacyclododecindione, obtained by racemic synthesis and optical resolution, were investigated and the ring conformation of…