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In vitro and in vivo antimalarial activity and chemical profiling of sugarcane leaves. (2022)
Journal Article
Okokon, J. E., Mobley, R., Edem, U. A., Bassey, A. I., Fadayomi, I., Drijfhout, F., …Li, W. (2022). In vitro and in vivo antimalarial activity and chemical profiling of sugarcane leaves. Scientific reports, 10250 - ?. https://doi.org/10.1038/s41598-022-14391-8

Saccharum officinarum Linn. (sugarcane, Family-Poaceae) is employed in Ibibio traditional medicine for the treatment of various infections and diseases such as malaria. We This study aims to assess the antiplasmodial effect of the leaf extract and fr... Read More about In vitro and in vivo antimalarial activity and chemical profiling of sugarcane leaves..

Biotransformation of artemisinin to a novel derivative via ring rearrangement by Aspergillus niger. (2022)
Journal Article
Luo, J., Mobley, R., Woodfine, S., Drijfhout, F., Horrocks, P., Ren, X., & Li, W. (2022). Biotransformation of artemisinin to a novel derivative via ring rearrangement by Aspergillus niger. Applied Microbiology and Biotechnology, 106, 2433-2444. https://doi.org/10.1007/s00253-022-11888-0

Artemisinin is a component part of current frontline medicines for the treatment of malaria. The aim of this study is to make analogues of artemisinin using microbial transformation and evaluate their in vitro antimalarial activity. A panel of microo... Read More about Biotransformation of artemisinin to a novel derivative via ring rearrangement by Aspergillus niger..

Alteration of the expression of sirtuins and var genes by heat shock in the malaria parasite Plasmodium falciparum (2022)
Journal Article
Anagu, L. O., Hulse, D. R., Horrocks, P. D., & Chakravorty, S. J. (2022). Alteration of the expression of sirtuins and var genes by heat shock in the malaria parasite Plasmodium falciparum. Molecular and Biochemical Parasitology, 111458 - 111458. https://doi.org/10.1016/j.molbiopara.2022.111458

Background In Plasmodium falciparum the monoallelic expression of var virulence genes is regulated through epigenetic mechanisms. A study in the Gambia showed that an increase in var gene expression is associated with fever, high blood lactate with... Read More about Alteration of the expression of sirtuins and var genes by heat shock in the malaria parasite Plasmodium falciparum.

N,N ''-Substituted thioureas and their metal complexes: syntheses, structures and electronic properties (2022)
Journal Article
Al-Riyahee, A. A. A., Horton, P. N., Coles, S. J., Berry, C., Horrocks, P. D., Pope, S. J. A., & Amoroso, A. J. (2022). N,N ''-Substituted thioureas and their metal complexes: syntheses, structures and electronic properties. Dalton Transactions, 51(9), 3531-3545. https://doi.org/10.1039/d1dt04091j

The synthesis of six N,N'-substituted thiourea ligands (L1a-L3b) was achieved in two steps. A corresponding extensive series of Cu(I), Cu(II), Ni(II) and Zn(II) complexes (1-24) with varying formulations were synthesised from these ligands by the rea... Read More about N,N ''-Substituted thioureas and their metal complexes: syntheses, structures and electronic properties.

Temperate zone plant natural products – a novel resource for activity against tropical parasitic diseases (2021)
Journal Article
Hameed, H., King, E., Doleckova, K., Bartholomew, B., Hollinshead, J., Mbye, H., …Price, H. (2021). Temperate zone plant natural products – a novel resource for activity against tropical parasitic diseases. Pharmaceuticals, 14(3), 1-17. https://doi.org/10.3390/ph14030227

The use of plant-derived natural products for the treatment of tropical parasitic diseases often has ethnopharmacological origins. As such, plants grown in temperate regions remain largely untested for novel anti-parasitic activities. We describe her... Read More about Temperate zone plant natural products – a novel resource for activity against tropical parasitic diseases.

In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues. (2020)
Journal Article
Ijeoma Uche, F., Guo, X., Okokon, J., Ullah, I., Horrocks, P., Boateng, J., …Li, W. (2020). In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues. Antimicrobial Agents and Chemotherapy, https://doi.org/10.1128/AAC.01995-20

Bisbenzylisoquinoline (BBIQ) alkaloids are a diverse group of natural products that demonstrate a range of biological activities. In this study, the in vitro antiplasmodial activity of three BBIQ alkaloids (cycleanine (1), isochondodendrine (2) and 2... Read More about In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues..

The relative rate of kill of the MMV Malaria Box compounds provide links to the mode of antimalarial action and highlight scaffolds of medicinal chemistry interest (2019)
Journal Article
Horrocks. (2019). The relative rate of kill of the MMV Malaria Box compounds provide links to the mode of antimalarial action and highlight scaffolds of medicinal chemistry interest. Journal of Antimicrobial Chemotherapy, 362-370. https://doi.org/10.1093/jac/dkz443

Objectives: Rapid rate-of-kill (RoK) is a key parameter in the target candidate profile 1 (TCP1) for the next-generation antimalarial drugs for uncomplicated malaria, termed Single Encounter Radical Cure and Prophylaxis (SERCaP). TCP1 aims to rapidly... Read More about The relative rate of kill of the MMV Malaria Box compounds provide links to the mode of antimalarial action and highlight scaffolds of medicinal chemistry interest.

Flavonoid versus artemisinin anti-malarial activity in Artemisia annua whole-leaf extracts (2019)
Journal Article
Horrocks. (2019). Flavonoid versus artemisinin anti-malarial activity in Artemisia annua whole-leaf extracts. Frontiers in Plant Science, https://doi.org/10.3389/fpls.2019.00984

Artemisinin, a sesquiterpene lactone produced by Artemisia annua glandular secretory trichomes, is the active ingredient in the most effective treatment for uncomplicated malaria caused by Plasmodium falciparum parasites. Other metabolites in A. annu... Read More about Flavonoid versus artemisinin anti-malarial activity in Artemisia annua whole-leaf extracts.

Discovery, synthesis and antibacterial evaluation of phenolic compounds from Cylicodiscus gabunensis (2019)
Journal Article
Aldulaimi, O., Drijfhout, F., Uche, F. I., Horrocks, P., & Li, W. (2019). Discovery, synthesis and antibacterial evaluation of phenolic compounds from Cylicodiscus gabunensis. BMC Complementary and Alternative Medicine, 183 -?. https://doi.org/10.1186/s12906-019-2589-2

BACKGROUND Cylicodiscus gabunensis Harms (Family Leguminosae) (CG) is an African medicinal plant used as a treatment of various ailments including malaria, liver diseases, and gastrointestinal disturbances. Its extracts showed potent in vitro antiba... Read More about Discovery, synthesis and antibacterial evaluation of phenolic compounds from Cylicodiscus gabunensis.

Development of NanoLuc-PEST expressing Leishmania mexicana as a new drug discovery tool for axenic- and intramacrophage-based assays. (2018)
Journal Article
Price, H., Berry, S., Hameed, H., Thomason, A., Maciej-Hulme, M., Saif Abou-Akkada, S., & Horrocks, P. (2018). Development of NanoLuc-PEST expressing Leishmania mexicana as a new drug discovery tool for axenic- and intramacrophage-based assays. PLoS Neglected Tropical Diseases, 12(7), Article e0006639 . https://doi.org/10.1371/journal.pntd.0006639

The protozoan parasite Leishmania causes leishmaniasis; a spectrum of diseases of which there are an estimated 1 million new cases each year. Current treatments are toxic, expensive, difficult to administer, and resistance to them is emerging. New th... Read More about Development of NanoLuc-PEST expressing Leishmania mexicana as a new drug discovery tool for axenic- and intramacrophage-based assays..

Investigation of the antibiofilm capacity of peptide-modified stainless steel (2018)
Journal Article
Cao, P., Li, W., Morris, A. R., Horrocks, P. D., Yuan, C., & Yang, Y. (2018). Investigation of the antibiofilm capacity of peptide-modified stainless steel. Royal Society Open Science, https://doi.org/10.1098/rsos.172165

Biofilm formation on surfaces is an important research topic in ship tribology and medical implants. In this study, dopamine and two types of synthetic peptides were designed and attached to 304 stainless steel surfaces, aiming to inhibit the formati... Read More about Investigation of the antibiofilm capacity of peptide-modified stainless steel.

G-quadruplex DNA motifs in the malaria parasite Plasmodium falciparum and their potential as novel antimalarial drug targets (2018)
Journal Article
Horrocks. (2018). G-quadruplex DNA motifs in the malaria parasite Plasmodium falciparum and their potential as novel antimalarial drug targets. Antimicrobial Agents and Chemotherapy, https://doi.org/10.1128/AAC.01828-17

G-quadruplexes are DNA or RNA secondary structures that can be formed from guanine-rich nucleic acids. These four-stranded structures, composed of stacked quartets of guanine bases, can be highly stable and have been demonstrated to occur in vivo in... Read More about G-quadruplex DNA motifs in the malaria parasite Plasmodium falciparum and their potential as novel antimalarial drug targets.

The synthesis and evaluation of thymoquinone analogues as anti-ovarian cancer and antimalarial agents (2018)
Journal Article
Mbye, H., Richardson, A., Li, W., Horrocks, P., Johnson-Ajinwo, O., & Ullah, I. (2018). The synthesis and evaluation of thymoquinone analogues as anti-ovarian cancer and antimalarial agents. Bioorganic and Medicinal Chemistry Letters, https://doi.org/10.1016/j.bmcl.2018.02.051

Thymoquinone (TQ), 2-isopropyl-5-methyl-1,4-benzoquinone, a natural product isolated from Nigella sativa L., has previously been demonstrated to exhibit antiproliferative activity in vitro against a range of cancers as well as the human malarial para... Read More about The synthesis and evaluation of thymoquinone analogues as anti-ovarian cancer and antimalarial agents.

Identification of heparin modifications and polysaccharide inhibitors of Plasmodium falciparum merozoite invasion that have potential for novel drug development. (2017)
Journal Article
Boyle, M. J., Skidmore, M., Dickerman, B., Cooper, L., Devlin, A., Yates, E., …Beeson, J. G. (2017). Identification of heparin modifications and polysaccharide inhibitors of Plasmodium falciparum merozoite invasion that have potential for novel drug development. Antimicrobial Agents and Chemotherapy, 61(11), https://doi.org/10.1128/AAC.00709-17

Despite recent successful control efforts, malaria remains a leading global health burden. Alarmingly, resistance to current antimalarials is increasing, and the development of new drug families is needed to maintain malaria control. Current antimala... Read More about Identification of heparin modifications and polysaccharide inhibitors of Plasmodium falciparum merozoite invasion that have potential for novel drug development..

A characterization of the antimalarial activity of the bark of Cylicodiscus gabunensis Harms (2017)
Journal Article
Aldulaimi, O., Uche a, F. I., Hameed, H., Mbye, H., Ullah, I., Drijfhout, F., …Li, W. (2017). A characterization of the antimalarial activity of the bark of Cylicodiscus gabunensis Harms. Journal of Ethnopharmacology, 198, 221-225. https://doi.org/10.1016/j.jep.2017.01.014

Ethnopharmacological relevance and aim A decoction of the bark of Cylicodiscus gabunensis Harms is used as a traditional medicine in the treatment of malaria in Nigeria. This study aims to validate the antimalarial potency of this decoction in vitro... Read More about A characterization of the antimalarial activity of the bark of Cylicodiscus gabunensis Harms.

A validated bioluminescence-based assay for the rapid determination of the initial rate of kill for discovery antimalarials (2016)
Journal Article
Horrocks. (2016). A validated bioluminescence-based assay for the rapid determination of the initial rate of kill for discovery antimalarials. Journal of Antimicrobial Chemotherapy, 717-726. https://doi.org/10.1093/jac/dkw449

Objectives: A future treatment for uncomplicated malaria will contain at least one component that exerts a rapid rate of kill. We describe here the validation and application of a simple, robust and rapid bioluminescence-based assay for the determina... Read More about A validated bioluminescence-based assay for the rapid determination of the initial rate of kill for discovery antimalarials.

Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond (2016)
Journal Article
Horrocks. (2016). Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond. PLOS pathogens a peer-reviewed open-access journal published by the Public Library of Science, https://doi.org/10.1371/journal.ppat.1005763

A major cause of the paucity of new starting points for drug discovery is the lack of interaction between academia and industry. Much of the global resource in biology is present in universities, whereas the focus of medicinal chemistry is still larg... Read More about Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond.

Bullying and undermining: a threat to both patient care and medical personnel wellbeing? A cross sectional survey of the Undergraduates, trainees and consultants in Obstetrics and Gynaecology in the West Midlands (2015)
Journal Article
Parry-Smith, W., Morse, L., Sutherland, A., Horrocks, P., & O’Mahony, F. (2015). Bullying and undermining: a threat to both patient care and medical personnel wellbeing? A cross sectional survey of the Undergraduates, trainees and consultants in Obstetrics and Gynaecology in the West Midlands. MedEdPublish,

Genome-wide and positional homopolymeric tract enrichment at promoter-exon boundaries and exclusion of nucleosomes in Plasmodium spp. and related parasites (2015)
Journal Article
Russell, K., Cheng, C., Bizzaro, J. W., Ponts, N., Emes, R., Marx, K. A., …Horrocks, P. (2015). Genome-wide and positional homopolymeric tract enrichment at promoter-exon boundaries and exclusion of nucleosomes in Plasmodium spp. and related parasites. Journal of Biomolecular Structure and Dynamics, 33, 13-13. https://doi.org/10.1080/07391102.2015.1032563