Category: Article

Medicinal plants are the important source of potentially useful chemotherapeutic agents which have made enormous contributions to human health and well-being. The bacteria, fungi, virus, etc have developed resistance against available drugs. The secondary metabolites of the variety of plants can serve as major source for the development of new drugs for the treatment of different diseases and infections. Depending upon the bioactive constituents present in the plant sample, these metabolites are extracted by different methods including most recent soxhlet, microwave, ultrasound, supercritical fluid, etc extractions. The different groups of secondary metabolites with their structural variations, chemical extraction methods and their potent biomedical applications have been discussed in this review.

Source:: http://www.pubs.iscience.in/journal/index.php/jbts/article/view/772

      

Murraya koenigii, commonly known as curry leaves, is a regular ingredient used in Indian cuisines. Not only it is beneficial for health but also it is speculated to have various medicinal properties. Although a large number of phytochemicals have been identified and tested for various properties but no compound have been extended for drug design purpose. Present work conducted on Murraya koenigii illustrates its anti-diabetic and anti-oxidant activities using various biochemical tests. From various evaluated leaf extracts of M.koenigii, DCM and Ethanol extracts were the one which showed best activity for anti-oxidant and anti-diabetic assays.

Source:: http://www.pubs.iscience.in/journal/index.php/jbts/article/view/765

      

Presentation abstracts of the Indo-Hungarian Symposium on Recent Advances in Chemistry and Biology held on 11 Dec 2017 at Miranda House, University of Delhi.

Convener: Dr. Amrita T Sheikh
Organizing Secretary: Dr. Poonam

Source:: http://www.pubs.iscience.in/journal/index.php/jbts/article/view/801

      

Herein we describe a simple method for the synthesis of Baylis-Hillman adducts and their acetates by utilizing inexpensively available cashew nut shell liquid (CNSL) natural resources. Furthermore, by using a molecular hybridization approach, a series of novel pyrimidine scaffolds (15a-15t) were synthesized via utilizing Baylis-Hillman acetates derived from cashew nut shell liquid (CNSL). All the newly synthesized compounds were screened for their in vitro antitumor activity. Baylis-Hillman compounds 5b and 5h showed promising anticancer activity against MCF-7. Among pyrimidine derivatives, compounds 15i, 15j and 15l showed promising activity against HEP-G2, whereas compounds 15j, 15k, 15l and 15m showed promising activity against MCF-7. In addition, compound 15m showed significant activity against K562 when compared with the standard. The structure-activity relationship (SAR) analysis suggests that the length of the carbon chain of phenyl ring played an important role in the potency of activity.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/753

      

Guest Editorial for special issue on Nuclear Medicine

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/767

      

Hyperparathyroidism (HPTH) is a condition in which the level of parathyroid hormone in blood is raised. Gold standard for the diagnosis of HPTH is a measurement of serum parathyroid hormone levels, accompanied by testing serum calcium levels, to differentiate between primary and secondary HPTH. The first line of treatment with primary HPTH is surgery to remove the adenoma or the tumor, whenever possible. It is in these cases that the imaging plays an important role for localization of tumor before surgery.Imaging can be anatomical that is ultrasound, CT and MRI or functional that is using nuclear medicine modalities (SPECT, SPECT/CT, PET/CT). This article reviews the nuclear medicine modalities, various radiopharmaceuticals and imaging techniques for parathyroid imaging.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/726

      

The current concepts of cancer therapy are moving towards personalized treatment regimen aiming to reduce toxicity and improve efficacy of therapeutic agents. With the development of molecular imaging and targeted therapies personalized care has received a shot in the arm. However, these developments are not without challenges. Drug delivery, metabolism, toxicity etc. challenge the effective utilization of such agents. Nanoparticles offer to overcome these hurdles with their unique physico-chemical properties which can be labeled with radionuclides and conjugated with ligands to achieve high specific activity in the intended areas. In this article, we discuss the present status of radiolabeled nanoparticles, the areas where they are being used and challenges that lie ahead. We intend to provide a basic outlook on the utilization of radiolabeled nanoparticles in cancer diagnosis and therapy.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/728

      

In this study, we have prepared a novel, dual-biomarker, targeting ligand having high affinity and specificity for PSMA/GRPr receptors that are expressed on most prostate cancers. [DUPA-6-Ahx-Lys(DOTA)-6-Ahx-RM2] was synthesized and the new conjugate was metallated macroscopically with GaCl₃, InCl₃, and LuCl₃ to form [DUPA-6-Ahx-Lys(M-DOTA)-6-Ahx-RM2] (where M = Ga, In, or Lu). These new agents, when radiolabeled with Ga-68, In-111, or Lu-177 hold theranostic potential for patients presenting with prostate cancer disease.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/718

      

In this paper we report the synthesis of 68Ga labeled NODAGA-Erlotinib for imaging of EGFR over-expressing tumors. NODAGA-Erlotinib conjugate was synthesized by reaction of the terminal alkyne of Erlotinib using Cu catalyzed click reaction. The conjugate was then radiolabeled with 68Ga in high radiochemical yields. The 68Ga NODAGA-Erlotinib conjugate also exhibited high in vitro stability. The log P value of 68Ga-NODAGA-Erlotinib was lower than that of 68Ga-NOTA-Erlotinib, a 68Ga based Erlotinib conjugate previously reported by our group. In the in vitro cell binding studies carried out in EGFR-positive A431 cells, 68Ga-NODAGA-erlotinib exhibited an uptake (7.8±1.3 %) lower than that of 68Ga-NOTA-Erlotinib (9.8±0.4%) showing that an increase in hydrophilicity possibly effected a decrease in cell permeability. The higher hydrophilicity of 68Ga-NODAGA-Erlotinib also led to significantly lower accumulation of 68Ga-NODAGA-Erlotinib in non-target organs in the biodistribution studies in Swiss mice. The overall properties of the 68Ga-NODAGA-Erlotinib conjugate are promising and reflect the role of hydrophilicity in reducing the non-specific uptake of the final radiotracer towards improving signal/noise ratio for further imaging studies.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/727

      

Coconut shell is an important byproduct of Cocos nucifera L. which is largely being wasted. The present study is focused on optimizing the extraction process of phenolic compounds and also to evaluate its physico-chemical and antioxidant properties. After studying the effect of different solvents and different extraction conditions, methanol was found to be the most effective solvent and extraction at 90^oC was suitable to give high phenolic yield (4045 mg GAE/100 g). For further precision of the ideal conditions, response surface methodology was carried out to optimize the solvent concentration, temperature and extraction time. The results revealed that methanol at 72%, extraction time 167 min and temperature 68^oC yielded maximal level of polyphenols from coconut shell. Both extraction temperature and solvent concentration were found to have significant effect on the phenolic yield. Suitable conditions could be applied to recover the antioxidant phenolic compounds from the coconut shell, an agricultural byproduct available at huge quantity in India. The physico-chemical and antioxidant properties of methanolic extract of coconut shell were noticed to be suitable for its application in food and pharmaceutical industries.

Source:: http://www.pubs.iscience.in/journal/index.php/jbts/article/view/681