Structure-Activity Relationship (SAR) Studies to Maximize the Activity of Compounds Isolated from Octocorals

Duque, Carmenza; Castellanos, Leonardo; Tello, Edisson

doi:10.5772/intechopen.74686

Cited by 3 publications

(6 citation statements)

References 55 publications

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“…It has become increasingly essential as a tool for organizing, mining, and interpreting data, to guide further investigation for drug discovery [ 154 ]. It is also a strategy to increase the value of the activity initially detected [ 155 ]. Natural products contain steric and electronic features in their bioactive sites (pharmacophores), which are responsible for the optimal supramolecular interactions with specific biologic targets and to trigger (or block) their biologic responses.…”

Section: Structure–activity Relationships Of Some Promising Natural P...mentioning

confidence: 99%

Plant-Derived Natural Products as Lead Agents against Common Respiratory Diseases

Oriola

Oyedeji

2022

Molecules

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Never has the world been more challenged by respiratory diseases (RDs) than it has witnessed in the last few decades. This is evident in the plethora of acute and chronic respiratory conditions, ranging from asthma and chronic obstructive pulmonary disease (COPD) to multidrug-resistant tuberculosis, pneumonia, influenza, and more recently, the novel coronavirus (COVID-19) disease. Unfortunately, the emergence of drug-resistant strains of pathogens, drug toxicity and side effects are drawbacks to effective chemotherapeutic management of RDs; hence, our focus on natural sources because of their unique chemical diversities and novel therapeutic applications. This review provides a summary on some common RDs, their management strategies, and the prospect of plant-derived natural products in the search for new drugs against common respiratory diseases.

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Section: Structure–activity Relationships Of Some Promising Natural P...mentioning

confidence: 99%

Plant-Derived Natural Products as Lead Agents against Common Respiratory Diseases

Oriola

Oyedeji

2022

Molecules

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“…However, due to the structural differences between Pseudopterosin compounds (glycosylation position, aglycone stereochemistry, and carbon skeleton) as well as differences in disease pathology and pathophysiology, no conclusive comparison of relative potency can be made. [24][25][26][27][28]38 Furthermore, it has been demonstrated that PsG, PsP, PsQ, PsS, PsT, PsU, 3-O-acetyl-PsU, seco-PsJ and seco-PsK are not selectively cytotoxic to malignant cell lines as they exhibited similar cytotoxic effects in the non-malignant cell line. 25 In regard to PsH, additional studies will need to be conducted on non-malignant cell lines to determine if PsH is selectively cytotoxic to PC-3 cells.…”

Section: Pseudopterosin H Reduces Pc-3 Cell Viability By Inducing Apo...mentioning

confidence: 99%

“…[23][24][25] Pseudopterosins are isolated from gorgonian soft corals and each derivative possess a tricyclic diterpene core with a fucose or xylose moiety and differ in the degree of acetylation of the glycoside group as well as stereochemistry (C1 position can be alpha or beta). 23,26 These compounds are of interest for therapeutic use in various human diseases due to their diverse range of biological activities that include anti-inflammatory, analgesic, anti-microbial, anti-proliferative, wound healing, neuroprotective, and anti-cancer effects. 25,[27][28][29][30] The known anti-inflammatory properties of Pseudopterosin compounds (hypothesized to occur via blocking the inflammatory pathway nuclear factor κB (NF-κB) through novel mechanisms of action), have resulted in their use in cosmetic skin care.…”

Section: Introductionmentioning

confidence: 99%

“…[27][28][29] The anti-cancer effects of many of these compounds has remains vastly unexplored despite a handful of studies on Pseudopterosins (Ps) A-D, PsP, PsQ, PsS, PsT, PsU, 3-O-acetyl-PsU, seco-PsJ, and seco-PsU having demonstrated cytotoxic and anti-proliferative activity in various malignant cell lines (HeLa, cervical cancer; PC-3, prostate cancer; HCT116, colorectal cancer; MCF-7, breast cancer; BJ, fibroblasts; MDA-MB-231, breast cancer). 25,26,28,29 Additionally, to our knowledge, no studies have been published on the possible anti-cancer effects of Pseudopterosin H (PsH) on the PC-3 PC cell line.…”

Section: Introductionmentioning

confidence: 99%

“…Previous studies investigating the anti-cancer potential of structurally related Pseudopterosin compounds on a triple negative breast cancer cell line have concluded that these compounds possess cytotoxic and anti-cancer activity. 25,26,28,29 Therefore, due to the analogous nature of breast and prostate cancer, as well as the known anti-inflammatory effects of the Pseudopterosins, we hypothesize that treatment with Pseudopterosin H will reduce PC-3 cell viability by inducing apoptosis and altering the concentration of intracellular reactive oxygen species (ROS).…”

Section: Introductionmentioning

confidence: 99%

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Therapeutic potential of Pseudopterosin H on a prostate cancer cell line

Bowers¹,

Caraballo²,

Bentley³

et al. 2021

JCPCR

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Metastatic castration resistant prostate cancer has remained predominantly incurable despite various advancements in cancer therapeutics. The lack of readily available and effective treatment options have driven research into alternative therapies, such as the use of marine natural products. Marine natural products are secondary metabolites produced by and isolated from marine organisms. A family of diterpene glycosides isolated from gorgonian soft corals, known as the Pseudopterosins, are of interest in cancer research. Previous studies performed on the Pseudopterosins have indicated that these compounds possess cytotoxic, anti-inflammatory, and anti-cancer activity in various malignant cell lines. We hypothesized that Pseudopterosin H will demonstrate anti-neoplastic activity in the PC-3 prostate cancer cell line by reducing cell viability and altering intracellular reactive oxygen species concentration through cytotoxic and apoptotic effects. Pseudopterosin H was isolated from the marine coral Pseudopterogorgia elisabethae. We assessed the therapeutic efficacy of Pseudopterosin H on the PC-3 cell line, at various treatment concentrations, through in-vitro assay screening using the MTT, NBT, and LDH assays, as well as AO/ EB fluorescence. Results from our study have shown that treatment with Pseudopterosin H reduces PC-3 cell viability by inducing apoptosis and downregulating the production of intracellular reactive oxygen species. The chemosensitivity of PC-3 cells to treatment with Pseudopterosin H suggests the potential for prophylactic and therapeutic advantage in the treatment of metastatic castration resistant prostate cancer.

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Isolation and elucidation of antibacterial compounds from roots and stems of Synadenium glaucescens Pax

Rwegoshora,

Msengwa,

Mabiki

et al. 2023

EAJSTI

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Extracts of Synadenium glaucescens Pax are reported to contain biologically active compounds against bacterial and viral infections. This study aimed at isolating pure compounds from its bioactive extracts as well as evaluating their antibacterial efficacy. A phytochemical investigation of the root and stem barks involved total maceration in methanol (MeOH). The root barks extract was then partitioned by Vacuum Liquid Chromatography (VLC) in a solvent gradient system to afford three fractions of Hexane (Hex), Ethyl acetate (EtOAc) and finally MeOH for the least, moderate, and most polar compounds respectively. The MeOH extract of stem barks was also partitioned in the same way by using two solvents: dichloromethane (DCM) and MeOH. All fractions were finally dried on a rotary evaporator at < 60 OC of the water bath. Isolation of pure compound from the EtOAc and DCM led to isolation of four compounds namely, hexacosane (G1), β-sitosterol (G2), octacosyl ferulate (G3) and hexacosanoic acid (G4). Their structures were analyzed and confirmed through NMR, GC-MS and in comparison, with literature. Antibacterial assay for G1, G3 and G4 against P. aeruginosa, E. coli, S. aureus, and E. faecalis was achieved by broth serial microdilution. Compounds, G3 demonstrated strong activity against S. aureus (MIC = 0.125 mg/mL) and weak activity against the rest strains (MIC = 2 mg/ mL). Also, the test results indicated G1 had weak activity against all tested strains (MIC = 2 mg/mL or above). While G4 demonstrated a moderate activity (1.0 mg/mL) against E. coli, S. aureus, E. faecalis and weak against P. aeruginosa (MIC > 2 mg/mL). These findings support traditional use and promise for antibacterial drug agents from S. glaucescens Pax.

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Structure-Activity Relationship (SAR) Studies to Maximize the Activity of Compounds Isolated from Octocorals

Cited by 3 publications

References 55 publications

Plant-Derived Natural Products as Lead Agents against Common Respiratory Diseases

Plant-Derived Natural Products as Lead Agents against Common Respiratory Diseases

Therapeutic potential of Pseudopterosin H on a prostate cancer cell line

Isolation and elucidation of antibacterial compounds from roots and stems of Synadenium glaucescens Pax

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