New molecular entities and structure–activity relationships of drugs designed by the natural product derivatization method from 2010 to 2018

Cui, Qingxin; Bian, Ruibin; Xu, Fangfang; Liu, Qingshan; Wang, Wenhu; Bian, Qiang

doi:10.1016/b978-0-12-819487-4.00016-1

Cited by 12 publications

(5 citation statements)

References 139 publications

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“…Further, the positive control (VAN) used at (100 mg/mL) showed lower antiadhesion activity (8.9%) compared to TSB as a negative control. The hydrophilic and polycationic characteristics of VAN towards the MRSA (ATCC-43300) surface may relate to this weak detachment activity [ 71 ]. On this account, the TP/Ag NCs proved to be efficient antifouling surfaces against multidrug-resistant Gram-positive bacteria such as MRSA (ATCC-43300).…”

Section: Resultsmentioning

confidence: 99%

Synthesis, Characterization, and Docking Study of Novel Thioureidophosphonate-Incorporated Silver Nanocomposites as Potent Antibacterial Agents

et al. 2023

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Newly synthesized mono- and bis-thioureidophosphonate (MTP and BTP) analogues in eco-friendly conditions were employed as reducing/capping cores for 100, 500, and 1000 mg L−1 of silver nitrate. The physicochemical properties of silver nanocomposites (MTP(BTP)/Ag NCs) were fully elucidated using spectroscopic and microscopic tools. The antibacterial activity of the nanocomposites was screened against six multidrug-resistant pathogenic strains, comparable to ampicillin and ciprofloxacin commercial drugs. The antibacterial performance of BTP was more substantial than MTP, notably with the best minimum inhibitory concentration (MIC) of 0.0781 mg/mL towards Bacillus subtilis, Salmonella typhi, and Pseudomonas aeruginosa. Among all, BTP provided the clearest zone of inhibition (ZOI) of 35 ± 1.00 mm against Salmonella typhi. After the dispersion of silver nanoparticles (AgNPs), MTP/Ag NCs offered dose-dependently distinct advantages over the same nanoparticle with BTP; a more noteworthy decline by 4098 × MIC to 0.1525 × 10−3 mg/mL was recorded for MTP/Ag-1000 against Pseudomonas aeruginosa over BTP/Ag-1000. Towards methicillin-resistant Staphylococcus aureus (MRSA), the as-prepared MTP(BTP)/Ag-1000 displayed superior bactericidal ability in 8 h. Because of the anionic surface of MTP(BTP)/Ag-1000, they could effectively resist MRSA (ATCC-43300) attachment, achieving higher antifouling rates of 42.2 and 34.4% at most optimum dose (5 mg/mL), respectively. The tunable surface work function between MTP and AgNPs promoted the antibiofilm activity of MTP/Ag-1000 by 1.7 fold over BTP/Ag-1000. Lastly, the molecular docking studies affirmed the eminent binding affinity of BTP over MTP—besides the improved binding energy of MTP/Ag NC by 37.8%—towards B. subtilis-2FQT protein. Overall, this study indicates the immense potential of TP/Ag NCs as promising nanoscale antibacterial candidates.

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Section: Resultsmentioning

confidence: 99%

Synthesis, Characterization, and Docking Study of Novel Thioureidophosphonate-Incorporated Silver Nanocomposites as Potent Antibacterial Agents

et al. 2023

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“…Phytocannabinoids are an interesting group of naturally occurring compounds that can produce several effects in humans by their attachment to specific human receptors (endocannabinoid system) ( 65 ). These compounds can be found in plants of the genus Cannabis , and these are classified into eight subgroups, including cannabigerol, cannabichromene, cannabidiol, tetrahydrocannabinol and cannabinol, cannabielsoin, isotetrahydrocannabinol, cannabicyclol, and cannabicitran ( 66 ). These phytocannabinoids are one of the most significant hemp bioactive components, because of the potential health benefits that they exert, including antineoplastic (i.e., cannabigerol, cannabidiol), antidepressant (i.e., cannabichromen), analgesic, anti-inflammatory, anxiolytic (i.e., cannabidiol), anti-epileptic (i.e., Δ9-tetrahydrocannabivarin), sleep improving and appetite-stimulating (Δ9-tetrahydrocannabinol), anti-glaucoma (Δ8-tetrahydrocannabinol), among others ( 67 ).…”

Section: Bioactive Compounds From Hemp Seeds and Their Potential Uses...mentioning

confidence: 99%

Hemp seeds: Nutritional value, associated bioactivities and the potential food applications in the Colombian context

et al. 2023

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For many years, Colombia was one of the countries with the largest illegal cultivation of cannabis around the world. Currently, it is going through a period of transition with a new government law that recently allows the cultivation, transformation, and commercialization of such plant species. In this sense, the identification of strategies for the valorization of products or by-products from Cannabis sativa represent a great opportunity to improve the value chain of this crop. One of these products is hemp seeds, which are exceptionally nutritious and rich in healthy lipids (with high content of three polyunsaturated fatty acids: linoleic acid, alpha-linolenic acid, and gamma-linolenic acid), good quality protein, and several minerals. In addition, hemp seeds contain THC (tetrahydrocannabinol) or CBD (cannabidiol) in traces, molecules that are responsible for the psychoactive and therapeutic properties of cannabis. These low terpenophenolic contents make it more attractive for food applications. This fact, together with the constant search for proteins of vegetable origin and natural food ingredients, have aroused an important interest in the study of this biomass. Some bioactivities of phytochemical compounds (polyphenols and terpenoids, mainly) present in hemp seeds have provided antioxidant, antimicrobial, and anti-inflammatory properties. This review summarizes and discusses the context of hemp use in Latin-American and the new opportunities for hemp seeds culture in Colombia considering the valuable nutritional value, main functional bioactivities, and recent advances in food market applications of hemp seeds.

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“…Natural statins initially isolated from fungus Penicillium citrinum in 1971 and the compound was named as mevastatin 35 (Figure 10). [109] Then, in 1978, Merck Laboratories isolated another statin molecule from fungus Aspergillus terreus and named it as lovastatin 36 (Figure 10) that became first commercial statin. It was approved by USFDA and indicated for treatment of coronary artery diseases and hypercholesterolemia.…”

Section: Statinsmentioning

confidence: 99%

A Concise Review on Natural Products and Their Derivatives for Breast Cancer Treatment

Gupta

Kumar

Gupta

et al. 2023

Chemistry & Biodiversity

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Cancer is a leading cause of death worldwide. Among other cancers, breast cancer has been found to produce maximum number of cases in 2020. Different factors including geographical, genetic, hormonal, oral contraceptives and modern lifestyle could be responsible for the development of breast cancer and different pathways can be targeted for breast cancer treatment. The various conventional approaches used for the treatment of breast cancer including radiotherapy, chemotherapy, hormone and immunotherapy. But due to the side effects associated with these conventional treatments such as non‐selectivity, multidrug resistance and bioavailability, there is a need for the development of better therapeutic agents for breast cancer treatment. Several natural products have been explored for breast cancer treatment. However, many of these natural products suffered from the limitations of poor water solubility and possess toxic side effects. To overcome these limitations, several structural analogs of natural products have been synthesized and possess potent anti‐breast cancer effects with less side effects over their precursor molecules. In the present manuscript, we describe the pathogenesis of breast cancer, some potent natural products used in the treatment of breast cancer and their selected structural analogs possessing potent anti‐breast cancer effects. Database such as Science direct, Pubmed and Google scholar were searched using keywords ‘risk factors’, ‘screening methods’,'receptors’, and ‘natural products and derivatives’, Registered clinical trials on selected natural products were also analyzed. Present study concludes that eight selected natural products and their derivatives possess wide potential to exhibit anti‐breast cancer effects and could be explored further to develop better chemotherapeutic agents against breast cancer.

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New molecular entities and structure–activity relationships of drugs designed by the natural product derivatization method from 2010 to 2018

Cited by 12 publications

References 139 publications

Synthesis, Characterization, and Docking Study of Novel Thioureidophosphonate-Incorporated Silver Nanocomposites as Potent Antibacterial Agents

Synthesis, Characterization, and Docking Study of Novel Thioureidophosphonate-Incorporated Silver Nanocomposites as Potent Antibacterial Agents

Hemp seeds: Nutritional value, associated bioactivities and the potential food applications in the Colombian context

A Concise Review on Natural Products and Their Derivatives for Breast Cancer Treatment

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