The modification of natural products for medical use

Guo, Zengjun

doi:10.1016/j.apsb.2016.06.003

Cited by 272 publications

(195 citation statements)

References 41 publications

Supporting

Mentioning

192

Contrasting

Unclassified

Order By: Relevance

“…[150] Many other examples of NP derivatization in relationt od rug discoveryh ave been described in the literature;t he subject was reviewed recently. [151,152] Despite all success stories and advantages, NP-based drug discoveryh as af ew important drawbacks compared with synthetic drugs. In fact, many NP-based drug-discoveryp rograms were curtailed by pharmaceutical companies when HTS of combinatorial chemistry libraries emerged.…”

Section: Role Of Nps In Drug Discoverymentioning

confidence: 99%

The Symbiotic Relationship Between Drug Discovery and Organic Chemistry

Grygorenko

Volochnyuk

Ryabukhin

et al. 2019

Chemistry A European J

135

123

View full text Add to dashboard Cite

All pharmaceutical products contain organic molecules; the source may be a natural product or a fully synthetic molecule, or a combination of both. Thus, it follows that organic chemistry underpins both existing and upcoming pharmaceutical products. The reverse relationship has also affected organic synthesis, changing its landscape towards increasingly complex targets. This Review article sets out to give a concise appraisal of this symbiotic relationship between organic chemistry and drug discovery, along with a discussion of the design concepts and highlighting key milestones along the journey. In particular, criteria for a high‐quality compound library design enabling efficient virtual navigation of chemical space, as well as rise and fall of concepts for its synthetic exploration (such as combinatorial chemistry; diversity‐, biology‐, lead‐, or fragment‐oriented syntheses; and DNA‐encoded libraries) are critically surveyed.

show abstract

Section: Role Of Nps In Drug Discoverymentioning

confidence: 99%

The Symbiotic Relationship Between Drug Discovery and Organic Chemistry

Grygorenko

Volochnyuk

Ryabukhin

et al. 2019

Chemistry A European J

135

123

View full text Add to dashboard Cite

show abstract

“…Additionally, the molecule is susceptible to metabolic conjugation at is phenolic residue. Structural modification by alteration of the phenolic group and conversion of the O ‐glycoside link into a C ‐glycoside enhanced its metabolic stability …”

Section: Effect Of Chemical Structure On Physicochemical Properties Amentioning

confidence: 99%

Chemical structure modifications and nano‐technology applications for improving ADME‐Tox properties, a review

Farouk

Shamma

2019

Archiv der Pharmazie

View full text Add to dashboard Cite

The chemical structure of a drug molecule affects its physicochemical properties and subsequent biological activities. Many pharmacologically active molecules fail to reach the market or have an inconvenient route of administration due to their chemical structure. This is especially important with the recent tendency to develop drug candidates beyond the drug-likeness space for addressing difficult targets such as protein-protein interfaces. The objective of this review is to discuss chemical and pharmaceutical approaches for circumventing structure-related problems and achieving acceptable ADME-Tox properties. The chemical structure-associated limitations are critically discussed. Chemical modifications and pharmaceutical technology applications for improving drug-likeness are illustrated. Attention is paid to modern therapeutic candidates and targets. In conclusion, chemical modifications as well as nanotechnology applications can be used effectively to enhance absorption, permeability, and selective distribution to a body compartment, to improve drug specificity, to limit off-target toxicity as well as to enhance stability and to protect against metabolism. The nano-technology-based solutions are relatively easier to develop over a new molecular entity, but adopting the chemical approach is more established in terms of safety, quality control, and regulatory assessment methods. K E Y W O R D Sblood-brain barrier, cancer tissue delivery, drug delivery, drug targeting, protein-protein interaction

show abstract

“…A new vaccine for primary prevention against H. pylori is currently under development [30].Due to the decrease in the efficacy of first-line treatments, increase of side-effects, and worldwide reports of H. pylori's resistance to antibiotics, new approaches are needed to manage this problematic infection; thus, efforts are being directed towards the development and delivery of new anti-H. pylori drugs [31]. Natural products, especially compounds derived from medicinal plants, have been sought as a source of new medicine, due to the great variety of chemical structures and structural modifications [32][33][34][35][36]. The essential oils produced by several medicinal plants are rich in monoterpenes, which are compounds with a great diversity of biological activities and potential therapeutic applications [37].…”

mentioning

confidence: 99%

Systematic Analysis of Monoterpenes: Advances and Challenges in the Treatment of Peptic Ulcer Diseases

et al. 2020

View full text Add to dashboard Cite

Peptic ulcer disease (PUD) is a multifactorial and complex disease caused by an imbalance of protective and aggressive factors (endogenous and exogenous). Despite advances in recent years, it is still responsible for substantial mortality and triggering clinical problems. Over the last decades, the understanding of PUD has changed a lot with the discovery of Helicobacter pylori infection. However, this disease continues to be a challenge due to side-effects, incidence of relapse from use of various anti-ulcer medicines, and the rapid appearance of antimicrobial resistance with current H. pylori therapies. Consequently, there is the need to identify more effective and safe anti-ulcer agents. The search for new therapies with natural products is a viable alternative and has been encouraged. The literature reports the importance of monoterpenes based on the extensive pharmacological action of this class, including wound healing and anti-ulcerogenic agents. In the present study, 20 monoterpenes with anti-ulcerogenic properties were evaluated by assessing recent in vitro and in vivo studies. Here, we review the anti-ulcer effects of monoterpenes against ulcerogenic factors such as ethanol, nonsteroidal anti-inflammatory drugs (NSAIDs), and Helicobacter pylori, highlighting challenges in the field.Biomolecules 2020, 10, 265 2 of 18 PUD results from an imbalance in mucosal defensive factors, such as mucus secretion, bicarbonate efflux, endogenous antioxidant, cell regeneration, continuous synthesis and release of prostaglandin E 2 (PGE 2 ), nitric oxide (NO), and sulfhydryl compounds (SH); and aggressive agents such as smoking, alcohol consumption, dietary factors, stress, prolonged and excessive intake of nonsteroidal anti-inflammatory drugs (NSAIDs), and Helicobacter pylori (H. pylori) infection, among others [6][7][8][9]. For a long time, it was believed that the main factor implicated in the development and progression of peptic ulceration was an hypersecretory acidic environment and together with dietary factors and/or stress was thought to cause most of PUD. But the discovery of H. pylori infection and the widespread use of NSAIDs in the second half of the 20 th century changed this perception. In recent years, peptic ulcer has been found to have multiple causes-H. pylori infection, NSAIDs, smoking, alcohol consumption, stress, lifestyle, and genetic predispositions are determined as major risk factors for the development of PUD [2]. PathophysiologyUnder normal conditions, gastric and duodenal mucosa integrity is maintained by the mucus-bicarbonate barrier, the neutral pH, and continuous epithelial cell renewal [10,11]. PGE 2 stimulates cell proliferation, mucus, and bicarbonate production, promoting a crucial function in mucosa preservation. Another vital factor in gastric homeostasis is adequate blood flow. The NO and PGs are responsible for the maintenance of proper perfusion to the gastric mucosa, assuring the delivery of oxygen and nutrients, as well as removing toxic metabolites, preventing damages to the ti...

show abstract

The modification of natural products for medical use

Cited by 272 publications

References 41 publications

The Symbiotic Relationship Between Drug Discovery and Organic Chemistry

The Symbiotic Relationship Between Drug Discovery and Organic Chemistry

Chemical structure modifications and nano‐technology applications for improving ADME‐Tox properties, a review

Systematic Analysis of Monoterpenes: Advances and Challenges in the Treatment of Peptic Ulcer Diseases

Contact Info

Product

Resources

About