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Publikationen - Natur- und Wirkstoffchemie

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Publikation

Hussain, H.; Xiao, J.; Ali, A.; Green, I. R.; Westermann, B.; Unusually cyclized triterpenoids: occurrence, biosynthesis and chemical synthesis Nat. Prod. Rep. 40, 412-451, (2023) DOI: 10.1039/d2np00033d

Covering: 2009 to 2021Biosynthetically, most of the syntheses of triterpenes follow the cascade cyclization and rearrangement of the acyclic precursors viz., squalene (S) and 2,3-oxidosqualene (OS), which lead to the very well known tetra- and pentacyclic triterpene skeletons. Aside from these, numerous other triterpenoid molecules are also reported from various natural sources and their structures are derived from \"S\" and \"OS\" via some unusual cyclization operations which are different from the usual tetra- and pentacyclic frameworks. Numerous compelling advances have been made and reported in the identification of these unusual cyclized mono-, di-, tri- and tetracyclic triterpenes between 2009 and 2021. Besides a dramatic increase in the newly isolated uncommon cyclized triterpenoids, substantial progress in the (bio)-synthesis of these triterpenes has been published along with significant progress in their biological effects. In this review, 180 new unusual cyclized triterpenoids together with their demonstrated biogenetic pathways, syntheses and biological effects will be categorized and discussed.
Publikation

Hussain, A.; Bourguet-Kondracki, M.-L.; Majeed, M.; Ibrahim, M.; Imran, M.; Yang, X.-W.; Ahmed, I.; Altaf, A. A.; Khalil, A. A.; Rauf, A.; Wilairatana, P.; Hemeg, H. A.; Ullah, R.; Green, I. R.; Ali, I.; Shah, S. T. A.; Hussain, H.; Marine life as a source for breast cancer treatment: A comprehensive review Biomedicine & Pharmacotherapy 159, 114165, (2023) DOI: 10.1016/j.biopha.2022.114165

Breast cancer, one of the most significant tumors among all cancer cells, still has deficiencies for effective treatment. Moreover, substitute treatments employing natural products as bioactive metabolites has been seriously considered. The source of bioactive metabolites are not only the most numerous but also represent the richest source. A unique source is from the oceans or marine species which demonstrated intriguing chemical and biological diversity which represents an astonishing reserve for discovering novel anticancer drugs. Notably, marine sponges produce the largest amount of diverse bioactive peptides, alkaloids, terpenoids, polyketides along with many secondary metabolites whose potential is mostly therapeutic. In this review, our main focus is on the marine derived secondary metabolites which demonstrated cytotoxic effects towards numerous breast cancer cells and have been isolated from the marine sources such as marine sponges, cyanobacteria, fungi, algae, tunicates, actinomycetes, ascidians, and other sources of marine organisms.
Publikation

Hussain, H.; Mamadalieva, N. Z.; Hussain, A.; Hassan, U.; Rabnawaz, A.; Ahmed, I.; Green, I. R.; Fruit peels: Food waste as a valuable source of bioactive natural products for drug discovery Current Issues in Molecular Biology 44, 1960-1994, (2022) DOI: 10.3390/cimb44050134

Fruits along with vegetables are crucial for a balanced diet. These not only have delicious flavors but are also reported to decrease the risk of contracting various chronic diseases. Fruit by-products are produced in huge quantity during industrial processing and constitute a serious issue because they may pose a harmful risk to the environment. The proposal of employing fruit by-products, particularly fruit peels, has gradually attained popularity because scientists found that in many instances peels displayed better biological and pharmacological applications than other sections of the fruit. The aim of this review is to highlight the importance of fruit peel extracts and natural products obtained in food industries along with their other potential biological applications.
Publikation

Hussain, H.; Rashan, L.; Hassan, U.; Abbas, M.; Hakkim, F. L.; Green, I. R.; Frankincense diterpenes as a bio-source for drug discovery Expert Opinion on Drug Discovery 17, 513-529, (2022) DOI: 10.1080/17460441.2022.2044782

Introduction Frankincense (Boswellia sp.) gum resins have been employed as an incense in cultural and religious ceremonies for many years. Frankincense resin has over the years been employed to treat depression, inflammation, and cancer in traditional medicines. Areas coveredThis inclusive review focuses on the significance of frankincense diterpenoids, and in particular, incensole derivatives for establishment future treatments of depression, neurological disorders, and cancer. The authors survey the available literature and furnish an overview of future perspectives of these intriguing molecules. Expert opinion Numerous diterpenoids including cembrane, prenylaromadendrane, and the verticillane-type have been isolated from various Boswellia resins. Cembrane-type diterpenoids occupy a crucial position in pharmaceutical chemistry and related industries because of their intriguing biological and encouraging pharmacological potentials. Several cembranes have been reported to possess anti-Alzheimer, anti-inflammatory, hepatoprotective, and antimalarial effects along with a good possibility to treat anxiety and depression. Although some slight drawbacks of these compounds have been noted, including the selectivity of these diterpenoids, there is a great need to address these in future research endeavors. Moreover, it is vitally important for medicinal chemists to prepare libraries of incensole-heterocyclic analogs as well as hybrid compounds between incensole or its acetate and anti-depressant or anti-inflammatory drugs.
Bücher und Buchkapitel

Hussain, H.; Elizbit, .; Ali, I.; Mamadalieva, N. Z.; Abbas, G.; Ali, M.; Zaman, G.; Khan, A.; Hassan, U.; Green, I. R.; Fruitful decade of Phoma secondary metabolites from 2011 to 2020: Chemistry, chemical diversity, and biological activities (Rai, M., Zimowska, B., Kövics, G.J.). Phoma: Diversity, Taxonomy, Bioactivities, and Nanotechnology 183–203, (2022) ISBN: 978-3-030-81217-1 DOI: 10.1007/978-3-030-81218-8_10

Fungi have been an extraordinary area of scientific research, and many secondary metabolites with intriguing chemical diversity along with interesting biological activities have been identified. Fungi like Phoma sp. have been investigated as a source of structurally unique metabolites over the past 10 years (2011–2020). A diverse range of natural products, viz., α-pyrone derivatives, isocoumarins, anthraquinones, xanthones, thiodiketopiperazines, cytochalasin derivatives, diphenyl ether derivatives, furopyrans, xyloketals, chromones, meroterpenoids, diterpenoids, polyketides, and alkaloids, have been reported from various Phoma spp. These metabolites illustrated phytotoxic, cytotoxic, antibacterial, antifungal, herbicidal, immunosuppressive, antiviral, antidiabetic (PTP1B inhibition), anti-Alzheimer (acetylcholinesterase inhibition), and antioxidant activities.
Publikation

Shamraiz, U.; Elizbit, .; Badshah, A.; Alfantazi, A.; Hussain, H.; Raza, B.; Ullah, S.; Green, I. R.; Solvent mediated fabrication of ditched hollow indium sulfide (In2S3) spheres for overall electrocatalytic water splitting Journal of The Electrochemical Society 168, 066510, (2021) DOI: 10.1149/1945-7111/ac0605

The controlled synthesis of nanomaterials is of prime importance in modern-day science. We report the shape-controlled synthesis of In2S3 spheres via a one-step solvent-mediated method. The process is very economical as it only requires the switching of solvent during synthesis (pure ethylene glycol, ethylene glycol/water, and ethylene glycol/ethanol mixtures) to fabricate porous and hollow In2S3 spheres. We have deliberately chosen a high boiling solvent and a combination of high and low boiling solvents to control the morphology. The synthesized In2S3 hollow spheres proved to be electrocatalytically active for an overall electrocatalytic water splitting and drive the oxygen evolution reactions at 230 mV and the hydrogen evolution reactions at 239 mV to produce a current density of 10 mA cm-2, respectively.
Publikation

Nazir, M.; Saleem, M.; Tousif, M. I.; Anwar, M. A.; Surup, F.; Ali, I.; Wang, D.; Mamadalieva, N. Z.; Alshammari, E.; Ashour, M. L.; Ashour, A. M.; Ahmed, I.; Elizbit, .; Green, I. R.; Hussain, H.; Meroterpenoids: A comprehensive update insight on structural diversity and biology Biomolecules 11, 957, (2021) DOI: 10.3390/biom11070957

Meroterpenoids are secondary metabolites formed due to mixed biosynthetic pathways which are produced in part from a terpenoid co-substrate. These mixed biosynthetically hybrid compounds are widely produced by bacteria, algae, plants, and animals. Notably amazing chemical diversity is generated among meroterpenoids via a combination of terpenoid scaffolds with polyketides, alkaloids, phenols, and amino acids. This review deals with the isolation, chemical diversity, and biological effects of 452 new meroterpenoids reported from natural sources from January 2016 to December 2020. Most of the meroterpenoids possess antimicrobial, cytotoxic, antioxidant, anti-inflammatory, antiviral, enzyme inhibitory, and immunosupressive effects.
Publikation

Nazir, M.; Saleem, M.; Ali, I.; Abbas, G.; Rehman, N. U.; Green, I. R.; Hussain, W.; Khan, S.; Hussain, H.; Fungal metabolites as anti-diabetic agents: emphasison PTP1B inhibitors Phytochemistry 20, 119-143, (2021) DOI: 10.1007/s11101-020-09701-9

In the last decade the prevalence of diabetes has escalated globally and it is estimated that the number of diabetic people will increase to 642 million by 2040. Although numerous classes of pharmaceutical drugs are available to treat Type ll diabetes, they manifest certain side effects. PTP1B has attracted significant interest as an important therapeutic agent and has been validated to target diabetes and obesity. Fungi, in general, produce secondary metabolites with some amazing chemical and structural diversity and are recognized to be a valuable source for therapeutic molecules. In this review, the focus is on describing the PTP1B effects and their potential as anti-diabetic agents for the various metabolites isolated from fungi.
Publikation

Hussain, H.; Ali, I.; Wang, D.; Hakkim, F. L.; Westermann, B.; Ahmed, I.; Ashour, A. M.; Khan, A.; Hussain, A.; Green, I. R.; Shah, S. T. A.; Glycyrrhetinic acid: a promising scaffold for the discovery of anticancer agents Expert Opinion on Drug Discovery 16, 1497-1516, (2021) DOI: 10.1080/17460441.2021.1956901

Introduction: Oleanane-type pentacyclic triterpenes named glycyrrhetinic acids (GAs) featuring a C-30 carboxylic acid group, are extracted from the licorice (Glycyrrhiza uralensis). Numerous biological properties of GA have been reported and have attracted researchers from all over the world in recent years due to the peculiar GA scaffold-based semisynthetic cytotoxic effects.Areas covered: This review represents the applications of semisynthetic derivatives of GA for the development of future cancer treatments. Included in the review are important structural features of the semisynthetic GAs crucial for cytotoxic effects.Expert opinion: Numerous semisynthetic GA derivatives illustrated excellent cytotoxic effects toward various cancer cells. Notably the C-3(OH) at ring A along with C30-CO2H at ring E as vital structural features, make GA very appealing as a lead scaffold for medicinal chemistry, since these two groups permit the creation of further chemical diversity geared toward improved cytotoxic effects. Furthermore, numerous GA derivatives have been synthesized and indicate that compounds featuring cyanoenone moieties in ring A, or compounds having the amino group or nitrogen comprising heterocycles and hybrids thereof, illustrate more potent cytotoxicity. Furthermore, GA has a great capability to be conjugated with other anticancer molecules to synergistically enhance their combined cytotoxicity.
Publikation

Hussain, H.; Mamadalieva, N. Z.; Ali, I.; Elizbit, .; Green, I. R.; Wang, D.; Zou, L.; Simal-Gandara, J.; Cao, H.; Xiao, J.; Fungal glycosides: Structure and biological function Trends in Food Science & Technology 110, 611-651, (2021) DOI: 10.1016/j.tifs.2021.02.029

Background: Natural products acquire vast and intriguing structural diversity and have been recognized as a tremendously diverse source of new lead compounds. Numerous bioactive secondary metabolites are present in the form of glycosylated molecules in which the sugar parts are normally associated with the interaction along with molecular recognition of the cellular target.Scope and approach: The presence of sugar entities are crucial as well as in some cases necessary, for therapeutic effects. Establishing novel and potent glycosylated secondary metabolites has formed a main goal in the natural product field from fungi and bacteria. These compounds possess a diverse range of sugar units.Key findings and conclusions: Fungi is considered one of the important sources for approved drugs with a diverse range of mode of action. The sugar part in numerous pharmacologically active natural products enhances bioavailability, biological potential, reduce toxicity, and improve stability. The vast majority of glyocosides showed antimicrobial effects, cytotoxic, antiviral and antiinflammatory effects. Notably, numerous fungal glycosides presented in this review illustrate significant antimicrobial effects towards various microorganisms especially against plant pathogens. The antimicrobial effects of these fungal glycosides indicate that these metabolites could be employed as natural preservatives in food in order to abolish or control the growth of pathogenic and spoilage microorganisms.
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