Most Cited Article – Formulation Strategies and Therapeutic Applications of Shikonin and Related Derivatives

Author(s):Kirandeep KaurAtamjit SinghHamayal SharmaSanha Punj and Neena Bedi*

Volume 16, Issue 1, 2022

Published on: 01 April, 2022

Page: [55 – 67]

Pages: 13

DOI: 10.2174/2667387816666220302112201


Shikonin and its derivatives are excellent representatives of biologically active naphthoquinones. A wide range of investigations carried out in the last few decades validated their pharmacological efficacy. Besides having magnificent therapeutic potential, shikonin and its derivatives suffer from various pharmacokinetic, toxicity, and stability issues like poor bioavailability, nephrotoxicity, photodegradation, etc. Recently, various research groups have developed an extensive range of formulations to tackle these issues to ease their path to clinical practice. The latest formulation approaches have been focused on exploiting the unique features of novel functional excipients, which in turn escalate the therapeutic effect of shikonin. Moreover, the codelivery approach in various drug delivery systems has been taken into consideration in a recent while to reduce toxicity associated with shikonin and its derivatives. This review sheds light on the essential reports and patents published related to the array of formulations containing shikonin and its derivatives. Read more:

Podcast | Cancer Nanotechnology: A New Revolution for Cancer Diagnosis and Therapy


Journal Name: Current Drug Metabolism

Author(s): Vivek K Chaturvedi, Anshuman Singh, Vinay K. Singh, Mohan P. Singh*.


Background: Nanotechnology is gaining significant attention worldwide for cancer treatment. Nanobiotechnology encourages the combination of diagnostics with therapeutics, which is a vital component of a customized way to deal with the malignancy. Nanoparticles are being used as Nanomedicine which participates in diagnosis and treatment of various diseases including cancer. The unique characteristic of Nanomedicine i.e. their high surface to volume ratio enables them to tie, absorb, and convey small biomolecule like DNA, RNA, drugs, proteins, and other molecules to targeted site and thus enhances the efficacy of therapeutic agents.

Objective: The objective of the present article is to provide an insight of several aspect of nanotechnology in cancer therapeutics such as various nanomaterials as drug vehicle, drug release strategies and role of nanotechnology in cancer therapy.

Methods: We performed an extensive search on bibliographic database for research article on nanotechnology and cancer therapeutics and further compiled the necessary information from various articles into the present article.

Results: Cancer nanotechnology confers a unique technology against cancer through early diagnosis, prevention, personalized therapy by utilizing nanoparticles and quantum dots.Nano-biotechnology plays an important role in the discovery of cancer biomarkers. Quantum dots, gold nanoparticles, magnetic nanoparticles, carbon nanotubes, gold nanowires etc. have been developed as a carrier of biomolecules that can detect cancer biomarkers. Nanoparticle assisted cancer detection and monitoring involves biomolecules like proteins, antibody fragments, DNA fragments, and RNA fragments as the base of cancer biomarkers.

Conclusion: This review highlights various approaches of cancer nanotechnology in the advancement of cancer therapy. For article details, please visit:


To subscribe our YouTube Channel, please click here:

Editors Choice Article | Genus Moquiniastrum (Asteraceae): Overview of Chemical and Bioactivity Studies


Journal Name: Current Bioactive Compounds

Author(s): Victoria de Moraes Goncalves, Angelita Da Silveira Moreira*, Patricia Diaz de Oliveira.



The genus Moquiniastrum belongs to the Asteraceae family and is widely and exclusively dispersed throughout South America. Its species adapt easily to different cultivation conditions, and present a varied chemical composition with a great performance in pharmacological and pharmacognosy studies, mainly for sesquiterpene lactones. Moquiniastrum polymorphum is a species distinguished in the genus, presenting socioeconomic potential in several sectors, besides great application in folk medicine to treat respiratory diseases. The bioactive properties highlighted in the research are antioxidant, allelopathic, anti-inflammatory, insecticidal, antiviral and antimicrobial activity, and toxicity against different cancer lines, among others. To date, from 21 species belonging to the genus Moquiniastrum 11 species have been studied for their chemical composition, and only five species have been studied for their biological or toxicological activity. Different parts of the plants have been analysed, such as flowers, leaves and bark of the trunk and roots, and extracts obtained by different extraction methods and solvents. The genus has in its chemical composition classes of molecules such as sesquiterpene lactones, sesquiterpenes, diterpenes, triterpenes, flavonoids, coumarins, caffeic acid derivatives, acetylene and non-protein amino acids. Isolation studies of the chemical constituents of the species are promising considering that they are safe to use since they do not cause changes in DNA and can be used even during the gestational period. To read out more, please visit:

Most Accessed Articles | Synthesis and Biological Evaluation of PF-543 Derivative


Journal Name: Letters in Organic Chemistry

Author(s): Seon Woong Kim, Taeho Lee, Joo-Youn Lee, Sanghee Kim, Hee-Sook Jun, Eun-Young Park*, Dong Jae Baek*.



PF-543 has been known as a substance that strongly inhibits SK1. However, it also exhibits antineoplastic activity that is lower than other inhibitors of SK1. In this study, we compared PF-543 and synthesized a newly designed derivative of PF-543 (compound 2) in which two aromatic structures were connected in para-form. The synthesized derivative showed inhibitory effect on SK1, similar to that of PF-543. However, it was more cytotoxic to HT29, AGS, and PC3 cells than PF-543. We also carried out a docking study for SK1 and demonstrated that the synthesized derivative showed interaction with SK1 similar to PF-543. Results obtained from this study suggest that the structure of compound 2 may be well substituted for the structure of PF-543 in terms of biological activity, providing us important structural information for the design of new derivatives of PF-543. Read out full article here:


ARTICLE BY DISEASE – Discovery of Hedgehog Antagonists for Cancer Therapy





Background: The evolutionarily conserved Hedgehog (Hh) signaling cascade is one of the key mediators of embryonic development of many metazoans. This pathway has been extensively targeted by small molecule inhibitors as its misregulation leads to various malignancies and developmental disorders. Thus, blocking this pathway can be a novel therapeutic avenue for the treatment of Hedgehog-dependent cancers. This review covers the mechanism of hedgehog signaling in vertebrate cells, provides an overview of reported small molecule Hh pathway inhibitors, with the synthetic routes and SAR studies of some of them discussed briefly.

Methods: A comprehensive survey of literature related to synthetic and naturally occurring Hh signaling antagonists reported till date is presented.

Results: Given the selectivity of small molecules targeting, this pathway for cancer treatment compared to kinase, tubulin or HDAC inhibitors, several such antagonists have been discovered, of which some are in preclinical development and clinical studies. Most of the reported small molecules primarily antagonize the Smoothened receptor although agents targeting Gli1 transcription factor and Shh ligand have also been discovered. Till date, nine Smo antagonists have been evaluated in clinical trials.GDC- 0449/Vismodegib and NVP-LDE225/Erismodegib, were granted approval by the U.S. Food and Drug Administration (U.S. FDA) for the treatment of basal cell carcinoma.

Conclusion: The challenge is to identify agents that target the pathway downstream of Smo and develop strategies to overcome acquired drug resistance to the current Smo inhibitors with deeper understanding of the resistance mechanisms.



For more details, please visit:

EDITOR’S CHOICE – Extraction, Identification and Biological Activities of Saponins in Sea Cucumber Pearsonothuria graeffei – Combinatorial Chemistry & High Throughput Screening

Journal: Combinatorial Chemistry & High Throughput Screening

Author(s): Rafat Afifi Khattab, Mohamed Elbandy, Andrew Lawrence, Tim Paget, Jung Rae-Rho, Yaser S. Binnaser, Imran Ali*


Aims and Objectives: Secondary metabolism in marine organisms produces a diversity of biologically important natural compounds that are not present in terrestrial species. Sea cucumbers belong to the invertebrate Echinodermata and are famous for their nutraceutical, medical and food values. They are known for possession triterpenoid glycosides (saponins) with various ecological roles. The current work aimed to separate, identify and test various biological activities (antibacterial, antifungal, antileishmanial and anticancer properties) of saponins produced by the holothurian Pearsonothuria graeffei from the Red Sea, Egypt.

Materials and Methods: The structures were identified by 1D and 2D NMR (1H, 13C, TOCSY, COSY, HSQC, HMBC, and ROESY) experiments and acid hydrolysis. The crude and purified fractions was analyzed using matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS)/MS to identify saponins and characterize their molecular structures. Partially purified fraction, mainly containing compounds 1 and 2, was screened for its antifungal activity against three clinical isolates of Candida albicans (Candida 580 (1), Candida 581(2) and Candida MEO47228. Antileishmanial activity against Leishmania major and toxicity on colon cell-line were also evaluated.

Results: Two lanostane type sulfated triterpene monoglycosides were isolated from the Holothurian Pearsonothuria graeffei from the Red Sea, Egypt. Holothurin A (1) and echinoside A (2) triterpene saponins were separated by reversed phase semi-preparative HPLC. LC50 values (µg/mL); calculated for the fraction containing saponins 1 and 2 as major constituents; against Candida albicans, Leishmania major and colon cell-line were 10, 20 and 0.50, respectively.

Conclusion: Consequently, this study demonstrated the potential use of sea cucumber Pearsonothuria graeffei not only as appreciated functional food or nutraceuticals but also as the source of functional ingredients for pharmaceutical products with antifungal, antileishmanial and anticancer properties.

Read more here:


EDITOR’S CHOICE – Cytotoxicity of Silver Nanoparticles Against Bacteria and Tumor Cells – Current Protein & Peptide Science

Journal: Current Protein & Peptide Science

Author(s): Tianyuan Shi, Xuesong Sun*, Qing-Yu He


With the rapid increase of multiple drug-resistant bacteria, silver nanoparticles (AgNPs) with broad-spectrum antibacterial activities have been widely applied in the treatment of bacterial infection. Meanwhile, AgNPs also have anticancer activities against different cell lines. The toxic effects of AgNPs depend on concentration, size, shape, coated materials and surrounding environments. In order to better understand the antibacterial and antitumor effects of AgNPs, various investigations have been carried out to uncover the molecular mechanism of action. This review summarizes the recent studies on the action mechanisms of AgNPs related to their antibacterial activities including collapsing cell walls, inducing reactive oxygen species, inhibiting aerobic respiration and damaging DNA and their antitumor effects including impairing mitochondria, blocking cell cycle, and activating apoptosis. In these investigations, the systematic approaches have not been extensively applied. Increasingly matured omics techniques including genomics, transcriptomic, translatomics and proteomics should be more widely explored to provide the comprehensive views of the cytotoxic effects of AgNPs to bacteria and tumor cells and thus globally illustrate the molecular mechanisms of the cytotoxicity, promoting the better medical application of AgNPs in the future.

Read more here:



Qicai Xiao

Contributed Article: “Discovery and Development of Natural Products and their Derivatives as Photosensitizers for Photodynamic Therapy

Highlighted Article – Update on Nitazoxanide – Current Drug Discovery Technologies

CDDT-Articles_14-4-Anshul Shakya

To access this article, please visit:

Essential Journals on Patent Information

Click on the journal to access the complete list of articles:

Recent Patents on Anti-Cancer Drug Discovery
Recent Patents on Nanotechnology

Browse journals by subject here:


%d bloggers like this: