Natural products to drugs: natural product derived compounds in clinical trials

Butler, Mark S.

doi:10.1039/b402985m

Cited by 505 publications

(286 citation statements)

References 622 publications

(251 reference statements)

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“…Most thiazolylpeptides show potent activity against Gram-positive pathogens, yet their poor solubility has limited clinical progress, and only a derivative of GE2270 has entered clinical trials for the topical treatment of acne. 46 Novel members of this class have been described (Figure 2b): thiomuracins 47 belong to the subgroup targeting EF-Tu, with an antibacterial profile similar to GE2270; thiazomycin 48 and philipimycin, 49 which target the 50S subunit, show high activity against Gram-positive strains, and a similar profile to thiostrepton.…”

Section: Improved Variants From Microbial Sourcesmentioning

confidence: 99%

Antibiotic discovery in the twenty-first century: current trends and future perspectives

Donadio¹,

Maffioli²,

Monciardini³

et al. 2010

J Antibiot

223

126

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New antibiotics are necessary to treat microbial pathogens that are becoming increasingly resistant to available treatment. Despite the medical need, the number of newly approved drugs continues to decline. We offer an overview of the pipeline for new antibiotics at different stages, from compounds in clinical development to newly discovered chemical classes. Consistent with historical data, the majority of antibiotics under clinical development are natural products or derivatives thereof. However, many of them also represent improved variants of marketed compounds, with the consequent risk of being only partially effective against the prevailing resistance mechanisms. In the discovery arena, instead, compounds with promising activities have been obtained from microbial sources and from chemical modification of antibiotic classes other than those in clinical use. Furthermore, new natural product scaffolds have also been discovered by ingenious screening programs. After providing selected examples, we offer our view on the future of antibiotic discovery.

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Section: Improved Variants From Microbial Sourcesmentioning

confidence: 99%

Antibiotic discovery in the twenty-first century: current trends and future perspectives

Donadio¹,

Maffioli²,

Monciardini³

et al. 2010

J Antibiot

223

126

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“…In many cases, this quest has already resulted in leads and scaffolds for drugs [1][2][3] and many reports highlight the use of plant-derived compounds as anticancer drugs 4,5 that contribute to new leads in clinical trials. 6 Anisomelic acid (AA) (Fig. S1 †) is a diterpenoid compound isolated from the medicinal plant Anisomeles malabarica 7 , which we have previously shown to be cytotoxic to oral and cervical cancer cells.…”

Section: Introductionmentioning

confidence: 99%

Targeted delivery of a novel anticancer compound anisomelic acid using chitosan-coated porous silica nanorods for enhancing the apoptotic effect

et al. 2015

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Targeted delivery of a novel anticancer compound anisomelic acid using chitosan-coated porous silica nanorods for enhancing the apoptotic effect, 2015, BIOMATERIALS SCIENCE, (3) Targeted cancer therapies are currently a strong focus in biomedical research. The most common approach is to use nanocarrier-based targeting to specifically deliver conventional anticancer drugs to enhance their therapeutic efficacy, increase bioavailabil ity, and decrease the side-effects on normal cells. A step further towards higher specificity and efficacy would be to employ specific novel drugs along with specific nanocarrier -based targeting. Our recent studies have demonstrated that a plant-derived diterpenoid compound, anisomelic acid (AA), induces apoptosis in cervical cancer cells. In this work, we describe the development of a folic acid (FA)-targeted AA delivery system using chitosan-coated rod-shaped mesoporous silica particles (Chitosan-NR-MSP). The cellular internalization and and uptake enhancement of the FA-Chitosan-NR-MSP towards cancerous folate receptor (FR) -positive (SiHa and HeLa) and/or normal FR-negative (HEK 293) cells were assessed, which indicated that the intracellular uptake of FA-conjugated Chitosan-NR-MSP was more target-specific. Furthermore, the induction of apoptosis by AA-loaded chitosan-coated rod-shaped particles on SiHa cells was studied. By employing caspase activation and PARP cleavage as measure of apoptosis, the FA-particle mediated AA treatment was clearly more effective, significantly enhancing apoptosis in comparison to non-targeted Chitosan-NR-MSP or free AA in SiHa cells, suggesting that the FA-Chitosan-NR-MSPs can be potentially utilized as a drug delivery system for cervical cancer treatment.

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“…With developments in modern science and technology, isolation of bioactive components from natural sources and identification of their molecular mechanism of action in the living system became an important pharmacological research [8][9][10]. Several promising natural products and natural product-inspired compounds are currently in clinical and pre-clinical developmental stages for cancer treatment [7,[11][12][13]. Limited supply of active compounds from natural sources, difficulties in complete profiling of their cellular targets and characterization of their molecular mechanisms of Phytochemicals and their synthetic derivatives are making a significant contribution in modern drug discovery programs by targeting several human diseases, including cancer.…”

Section: Introductionmentioning

confidence: 99%

Key cell signaling pathways modulated by zerumbone: Role in the prevention and treatment of cancer

Prasannan

Kalesh

Shanmugam

et al. 2012

Biochemical Pharmacology

126

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Natural products to drugs: natural product derived compounds in clinical trials

Cited by 505 publications

References 622 publications

Antibiotic discovery in the twenty-first century: current trends and future perspectives

Antibiotic discovery in the twenty-first century: current trends and future perspectives

Targeted delivery of a novel anticancer compound anisomelic acid using chitosan-coated porous silica nanorods for enhancing the apoptotic effect

Key cell signaling pathways modulated by zerumbone: Role in the prevention and treatment of cancer

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