Determination of activities of human carbonic anhydrase II inhibitors from curcumin analogs

Aditama, Reza; Eryanti, Yum; Mujahidin, Didin; Syah, Yana Maolana; Hertadi, Rukman

doi:10.4314/tjpr.v16i4.14

Cited by 7 publications

(6 citation statements)

References 15 publications

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“…These compounds have gained increasing interest over the last few decades due to a wide variety of biological activities, including antioxidant [ 19 ], anti-inflammatory [ 20 ], antitumor [ 21 ], antidiabetic [ 22 ], antibacterial [ 23 ], antiparasitic [ 24 ], and antihyperuricemic [ 25 ]. In addition, diarylpentanoids have also been described for their ability to interfere with several proteins, namely enzymes [ 26 , 27 , 28 , 29 , 30 , 31 , 32 ] (oxidoreductases, glycosidases, phosphatases, cholinesterases, and carbonic anhydrase II), and channel proteins (P-gp, BCRP, MRP1, MRP5, TRPA1, TRPM8, and TRPV1). The antitumor potential of diarylpentanoids has been widely studied, having identified several compounds as potent in vitro growth inhibitors of human tumor cell lines, with GI 50 values of nanomolar range [ 21 ].…”

Section: Introductionmentioning

confidence: 99%

BP-M345, a New Diarylpentanoid with Promising Antimitotic Activity

et al. 2021

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Previously, we reported the in vitro growth inhibitory effect of diarylpentanoid BP-M345 on human cancer cells. Nevertheless, at that time, the cellular mechanism through which BP-M345 exerts its growth inhibitory effect remained to be explored. In the present work, we report its mechanism of action on cancer cells. The compound exhibits a potent tumor growth inhibitory activity with high selectivity index. Mechanistically, it induces perturbation of the spindles through microtubule instability. As a consequence, treated cells exhibit irreversible defects in chromosome congression during mitosis, which induce a prolonged spindle assembly checkpoint-dependent mitotic arrest, followed by massive apoptosis, as revealed by live cell imaging. Collectively, the results indicate that the diarylpentanoid BP-M345 exerts its antiproliferative activity by inhibiting mitosis through microtubule perturbation and causing cancer cell death, thereby highlighting its potential as antitumor agent.

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Section: Introductionmentioning

confidence: 99%

BP-M345, a New Diarylpentanoid with Promising Antimitotic Activity

et al. 2021

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“…Rukman and co-workers studied the biological screening of novel curcumin derivatives as carbonic anhydrase II (CA-II) inhibitors for glaucoma treatment. [85] These curcumin hybrids have shown potential inhibitory against CA-II with IC 50 values ranging from 7.92 to 72.31 μmol. Compound 114 (Figure 23) showed the best biological activity.…”

Section: Miscellaneous Agentsmentioning

confidence: 99%

The Multi‐Biological Targeted Role of Dehydrozingerone and its Analogues

et al. 2022

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Curcumin (Cur) has shown its potential in the treatment of a wide variety of ailments. As a result, several investigations on curcumin have been conducted in vitro, in vivo, and in clinical trials. Regrettably, researchers have largely lost interest in this excellent scaffold due to its chemical instability, poor solubility, and rapid metabolism, which directly affect its pharmacological properties. Alternatively, the researchers are working on it to improve the solubility and biological half-life, it is one of the most researched natural phytochemical to date. Among these, Dehydrozingerone (DZG), a curcumin half structure has garnered considerable research interest due to a wide spectrum of its biological activities. Thus, this study offers insight into the pharmacological activity of modified DZG conjugates (incorporate multiple effective modifications to the various positions), which have been developed since 2016. Additionally, the structure-activity relationship (SAR) of DZG hybrids was illustrated for their specific pharmacological properties. This review presents an update for the scientific community, which could assist in addressing the gaps, challenges and pharmacological aspects of DZG.

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“…Additionally, the substitutions on the 4-piperidone core seemed to interfere with inhibitory activity, since compounds 713 and 726 with the N -methyl-4-piperidone and N -propyl-4-piperidone moiety, respectively, exhibited contrasting results to 702 , which possesses an unsubstituted 4-piperidone core ( Figure 19 ). Lastly, molecular docking analysis revealed that compound 702 formed hydrogen interactions with Thr199, Thr200, and Gln92 at the active site of CA-II [ 75 ].…”

Section: Biological Activity Of Diarylpentanoidsmentioning

confidence: 99%

Bioactive Diarylpentanoids: Insights into the Biological Effects beyond Antitumor Activity and Structure–Activity Relationships

2022

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Diarylpentanoids, a class of natural products and their synthetic analogs which are structurally related to chalcones, have gained increasing attention due to their wide array of biological activities, including antitumor, anti-infective, antioxidant, anti-inflammatory, antidiabetic, anti-hyperuricemic, and neuroprotective properties. Previously, we reviewed diarylpentanoids with promising antitumor activity. However, in view of the wide range of biological activities described for this class of compounds, the purpose of this review is to provide a more detailed overview of the synthetic bioactive diarylpentanoids that have been described over the last two decades, beyond simply their antitumor effects. A total of 745 compounds were found, highlighting the main synthetic methodologies used in their synthesis as well as the structure–activity relationship studies and structural features for all activities reported. Collectively, this review highlights the diarylpentanoid scaffold as a promising starting point for the development of new therapeutic agents.

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Determination of activities of human carbonic anhydrase II inhibitors from curcumin analogs

Cited by 7 publications

References 15 publications

BP-M345, a New Diarylpentanoid with Promising Antimitotic Activity

BP-M345, a New Diarylpentanoid with Promising Antimitotic Activity

The Multi‐Biological Targeted Role of Dehydrozingerone and its Analogues

Bioactive Diarylpentanoids: Insights into the Biological Effects beyond Antitumor Activity and Structure–Activity Relationships

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