NobleBlocks

International Center for Chemical and Biological Sciences

facilityKarachi, Pakistan

Research output, citation impact, and the most-cited recent papers from International Center for Chemical and Biological Sciences (Pakistan). Aggregated across the NobleBlocks index of 300M+ scholarly works.

Total works
10.7K
Citations
351.0K
h-index
154
i10-index
9.1K
Also known as
HEJ Research Institute of ChemistryHussain Ebrahim Jamal Research Institute of ChemistryInternational Center for Chemical and Biological Sciencesکیمیائی اور حیاتیاتی سائنس کے لئے بین الاقوامی مرکز

Top-cited papers from International Center for Chemical and Biological Sciences

Glioblastoma Multiforme: A Review of its Epidemiology and Pathogenesis through Clinical Presentation and Treatment
Farina Hanif, Kanza Muzaffar, Kahkashan Perveen, Saima Mehmood Malhi +1 more
2017· Europe PMC (PubMed Central)1.2Kdoi:10.22034/apjcp.2017.18.1.3

Glioblastoma multiforme (GBM) is one of the most malignant types of central nervous system tumors. Despite advances in treatment modalities it remains largely incurable. The objective of our review is to provide a holistic picture of GBM epidemiology, etiology, pathogenesis, clinical findings and treatment. A literature search was conducted for GBM at PubMed and Google Scholar, with relevant key words like glioblastoma multiforme, pathogenesis, signs and symptoms, treatment etc., and papers published until 2015 were reviewed. It was found that radiation and certain genetic syndromes are the only risk factors identified to date for GBM. Depending on the tumor site patients may present to the clinic with varying symptoms. To confirm the presence and the extent of tumor, various invasive and non-invasive imaging techniques require employment. The literature survey revealed the pathogenesis to involve aberrations of multiple signaling pathways through multiple genetic mutations and altered gene expression. Although several treatment options are available, including surgery, along with adjuvant chemo- and radio-therapy, the disease has a poor prognosis and patients generally succumb within 14 months of diagnosis.

Antidiabetic Potential of Medicinal Plants and Their Active Components
Bahare Salehi, Athar Ata, N. V. Anil Kumar, Farukh Sharopov +4 more
2019· Biomolecules718doi:10.3390/biom9100551

Diabetes mellitus is one of the major health problems in the world, the incidence and associated mortality are increasing. Inadequate regulation of the blood sugar imposes serious consequences for health. Conventional antidiabetic drugs are effective, however, also with unavoidable side effects. On the other hand, medicinal plants may act as an alternative source of antidiabetic agents. Examples of medicinal plants with antidiabetic potential are described, with focuses on preclinical and clinical studies. The beneficial potential of each plant matrix is given by the combined and concerted action of their profile of biologically active compounds.

Anticancer potential of quercetin: A comprehensive review
Abdur Rauf, Muhammad Imran, Imtiaz Khan, Mujeeb ur Rehman +3 more
2018· Phytotherapy Research639doi:10.1002/ptr.6155

Diet plays a key role to maintaining healthy life. Many natural products present in our diet, such as flavonoids, can prevent the progression of cancer. Quercetin, a distinctive bioactive flavonoid, is a dietary component that has attracted the attention of dietitians and medicinal chemists due to its numerous health-promoting effects. It is an outstanding antioxidant that has a well-documented role in reducing different human cancers. Quercetin exhibits direct proapoptotic effects on tumor cells and thus can inhibit the progress of numerous human cancers. The anticancer effect of quercetin has been documented in numerous in vitro and in vivo studies that involved several cell lines and animal models. On the other hand, the high toxic effect of quercetin against cancer cells is accompanied with little or no side effects or harm to normal cells. Accordingly, this review presents an overview of recent developments on the use of quercetin against different types of cancer along with mechanisms of action. In addition, the present review summarizes the literature pertaining to quercetin as an anticancer agent and provides an assessment of the potential utilization of this natural compound as a complimentary or alternative medicine for preventing and treating cancer.

Overview of Bee Pollination and Its Economic Value for Crop Production
Shaden A. M. Khalifa, Esraa H. Elshafiey, Aya A. Shetaia, Aida A. Abd El‐Wahed +4 more
2021· Insects607doi:10.3390/insects12080688

Pollination plays a significant role in the agriculture sector and serves as a basic pillar for crop production. Plants depend on vectors to move pollen, which can include water, wind, and animal pollinators like bats, moths, hoverflies, birds, bees, butterflies, wasps, thrips, and beetles. Cultivated plants are typically pollinated by animals. Animal-based pollination contributes to 30% of global food production, and bee-pollinated crops contribute to approximately one-third of the total human dietary supply. Bees are considered significant pollinators due to their effectiveness and wide availability. Bee pollination provides excellent value to crop quality and quantity, improving global economic and dietary outcomes. This review highlights the role played by bee pollination, which influences the economy, and enlists the different types of bees and other insects associated with pollination.

Marine Natural Products: A Source of Novel Anticancer Drugs
Shaden A. M. Khalifa, Nizar Elias, Mohamed A. Farag, Lei Chen +4 more
2019· Marine Drugs550doi:10.3390/md17090491

Cancer remains one of the most lethal diseases worldwide. There is an urgent need for new drugs with novel modes of action and thus considerable research has been conducted for new anticancer drugs from natural sources, especially plants, microbes and marine organisms. Marine populations represent reservoirs of novel bioactive metabolites with diverse groups of chemical structures. This review highlights the impact of marine organisms, with particular emphasis on marine plants, algae, bacteria, actinomycetes, fungi, sponges and soft corals. Anti-cancer effects of marine natural products in in vitro and in vivo studies were first introduced; their activity in the prevention of tumor formation and the related compound-induced apoptosis and cytotoxicities were tackled. The possible molecular mechanisms behind the biological effects are also presented. The review highlights the diversity of marine organisms, novel chemical structures, and chemical property space. Finally, therapeutic strategies and the present use of marine-derived components, its future direction and limitations are discussed.

Dietary Sources of Lutein and Zeaxanthin Carotenoids and Their Role in Eye Health
El‐Sayed M. Abdel‐Aal, Humayoun Akhtar, Khalid Zaheer, Rashida Ali
2013· Nutrients543doi:10.3390/nu5041169

The eye is a major sensory organ that requires special care for a healthy and productive lifestyle. Numerous studies have identified lutein and zeaxanthin to be essential components for eye health. Lutein and zeaxanthin are carotenoid pigments that impart yellow or orange color to various common foods such as cantaloupe, pasta, corn, carrots, orange/yellow peppers, fish, salmon and eggs. Their role in human health, in particular the health of the eye, is well established from epidemiological, clinical and interventional studies. They constitute the main pigments found in the yellow spot of the human retina which protect the macula from damage by blue light, improve visual acuity and scavenge harmful reactive oxygen species. They have also been linked with reduced risk of age-related macular degeneration (AMD) and cataracts. Research over the past decade has focused on the development of carotenoid-rich foods to boost their intake especially in the elderly population. The aim of this article is to review recent scientific evidences supporting the benefits of lutein and zexanthin in preventing the onset of two major age-related eye diseases with diets rich in these carotenoids. The review also lists major dietary sources of lutein and zeaxanthin and refers to newly developed foods, daily intake, bioavailability and physiological effects in relation to eye health. Examples of the newly developed high-lutein functional foods are also underlined.

Antimicrobial natural products: an update on future antibioticdrug candidates
Muhammad Saleem, Mamona Nazir, Muhammad Shaiq Ali, Hidayat Hussain +3 more
2009· Natural Product Reports534doi:10.1039/b916096e

Over the last decade, it has become clear that antimicrobial drugs are losing their effectiveness due to the evolution of pathogen resistance. There is therefore a continuing need to search for new antibiotics, especially as new drugs only rarely reach the market. Natural products are both fundamental sources of new chemical diversity and integral components of today's pharmaceutical compendium, and the aim of this review is to explore and highlight the diverse natural products that have potential to lead to more effective and less toxic antimicrobial drugs. Although more than 300 natural metabolites with antimicrobial activity have been reported in the period 2000-2008, this review will describe only those with potentially useful antimicrobial activity, viz. with MICs in the range 0.02-10 microg mL(-1). A total of 145 compounds from 13 structural classes are discussed, and over 100 references are cited.

An update on bioactive plant lignans
Muhammad Saleem, Hyoung Ja Kim, Muhammad Shaiq Ali, Yong Sup Lee
2005· Natural Product Reports492doi:10.1039/b514045p

Lignans are a class of secondary plant metabolites produced by oxidative dimerization of two phenylpropanoid units. Although their molecular backbone consists only of two phenylpropane (C6-C3) units, lignans show an enormous structural diversity. There is a growing interest in lignans and their synthetic derivatives due to applications in cancer chemotherapy and various other pharmacological effects. This review deals with lignans possessing anticancer, antioxidant, antimicrobial, anti-inflammatory and immunosuppressive activities, and comprises the data reported in more than 100 peer-reviewed articles, so as to highlight the recently reported bioactive lignans that could be a first step towards the development of potential new therapeutic agents.

Metal nanoparticles fabricated by green chemistry using natural extracts: biosynthesis, mechanisms, and applications
Hesham R. El‐Seedi, Rehan M. El-Shabasy, Shaden A. M. Khalifa, Aamer Saeed +4 more
2019· RSC Advances437doi:10.1039/c9ra02225b

Nanoparticles (NPs) are new inspiring clinical targets that have emerged from persistent efforts with unique properties and diverse applications. However, the main methods currently utilized in their production are not environmentally friendly. With the aim of promoting a green approach for the synthesis of NPs, this review describes eco-friendly methods for the preparation of biogenic NPs and the known mechanisms for their biosynthesis. Natural plant extracts contain many different secondary metabolites and biomolecules, including flavonoids, alkaloids, terpenoids, phenolic compounds and enzymes. Secondary metabolites can enable the reduction of metal ions to NPs in eco-friendly one-step synthetic processes. Moreover, the green synthesis of NPs using plant extracts often obviates the need for stabilizing and capping agents and yields biologically active shape- and size-dependent products. Herein, we review the formation of metallic NPs induced by natural extracts and list the plant extracts used in the synthesis of NPs. In addition, the use of bacterial and fungal extracts in the synthesis of NPs is highlighted, and the parameters that influence the rate of particle production, size, and morphology are discussed. Finally, the importance and uniqueness of NP-based products are illustrated, and their commercial applications in various fields are briefly featured.

Chemistry and Mechanism of Urease Inhibition
Zareen Amtul, Atta‐ur Rahman, Rafat A. Siddiqui, M. Iqbal Choudhary
2002· Current Medicinal Chemistry392doi:10.2174/0929867023369853

Studies on enzyme inhibition remain an important area of pharmaceutical research since these studies have led to the discoveries of drugs useful in a variety of physiological conditions. The enzyme inhibitors can interact with enzymes and block their activity towards natural substrates. Urease inhibitors have recently attracted much attention as potential new anti-ulcer drugs. Ironically, urease was the first enzyme crystallized but its mechanism of action is still largely misunderstood. This chapter therefore reviews comprehensive developments in the field of urease inhibitors. Inhibitors of urease can be broadly classified into two categories: (1) active site directed (substrate-like), (2) mechanism-based directed. We present here the examples of selected inhibitors along with their mechanisms of action to characterize their mode of urease inhibition. The observations that urease due to its high substrate (urea) specificity can only bind to a few inhibitors with a similar binding mode as urea is also discussed. Several non-covalent interactions including hydrogen bonds and hydrophobic contacts stabilize the enzyme-inhibitor complex. Regardless of the class of compound, it is reported that only a few functional groups with electronegative atoms such as oxygen, nitrogen and sulfur act either as bidentate (mostly), tridentate (rarely), or as ligand-chelator to form octahedral complexes with two slightly distorted octahedral Ni ions of the enzyme. Bulky groups attached to the pharmacophore were found to decrease the activity of inhibitors, since the lack of a bulky attachment makes it easier for urease inhibitors to enter the substrate-binding pocket as well as avoid unfavorable steric interactions with amino acid residues in its vicinity. This review is intended to provide highlights of the inhibition of urease by hydroxamic acids (HXAs), phosphorodiamidates (PPDs), imidazoles, phosphazene and related compounds. These compounds are compared to previously reported urease inhibitors for the catalytic models proposed for urease activity. The differences in inhibition of urease activities from plants and of bacterial origin by various inhibitors and physiological implications of urease inhibition are discussed.

Schiff bases in medicinal chemistry: a patent review (2010-2015)
Abdul Hameed, Mariya al‐Rashida, Maliha Uroos, Syed Abid Ali +1 more
2016· Expert Opinion on Therapeutic Patents382doi:10.1080/13543776.2017.1252752

INTRODUCTION: Schiff bases are synthetically accessible and structurally diverse compounds, typically obtained by facile condensation between an aldehyde, or a ketone with primary amines. Schiff bases contain an azomethine (-C = N-) linkage that stitches together two or more biologically active aromatic/heterocyclic scaffolds to form various molecular hybrids with interesting biological properties. Schiff bases are versatile metal complexing agents and have been known to coordinate all metals to form stable metal complexes with vast therapeutic applications. Areas covered: This review aims to provide a comprehensive overview of the various patented therapeutic applications of Schiff bases and their metal complexes from 2010 to 2015. Expert opinion: Schiff bases are a popular class of compounds with interesting biological properties. Schiff bases are also versatile metal complexing ligands and have been used to coordinate almost all d-block metals as well as lanthanides. Therapeutically, Schiff bases and their metal complexes have been reported to exhibit a wide range of biological activities such as antibacterial including antimycobacterial, antifungal, antiviral, antimalarial, antiinflammatory, antioxidant, pesticidal, cytotoxic, enzyme inhibitory, and anticancer including DNA damage.

The Expanding Role of Pyridine and Dihydropyridine Scaffolds in Drug Design
Yong Ling, Zhi‐You Hao, Dong Liang, Chun‐Lei Zhang +2 more
2021· Drug Design Development and Therapy377doi:10.2147/dddt.s329547

Pyridine-based ring systems are one of the most extensively used heterocycles in the field of drug design, primarily due to their profound effect on pharmacological activity, which has led to the discovery of numerous broad-spectrum therapeutic agents. In the US FDA database, there are 95 approved pharmaceuticals that stem from pyridine or dihydropyridine, including isoniazid and ethionamide (tuberculosis), delavirdine (HIV/AIDS), abiraterone acetate (prostate cancer), tacrine (Alzheimer's), ciclopirox (ringworm and athlete's foot), crizotinib (cancer), nifedipine (Raynaud's syndrome and premature birth), piroxicam (NSAID for arthritis), nilvadipine (hypertension), roflumilast (COPD), pyridostigmine (myasthenia gravis), and many more. Their remarkable therapeutic applications have encouraged researchers to prepare a larger number of biologically active compounds decorated with pyridine or dihydropyridine, expandeing the scope of finding a cure for other ailments. It is thus anticipated that myriad new pharmaceuticals containing the two heterocycles will be available in the forthcoming decade. This review examines the prospects of highly potent bioactive molecules to emphasize the advantages of using pyridine and dihydropyridine in drug design. We cover the most recent developments from 2010 to date, highlighting the ever-expanding role of both scaffolds in the field of medicinal chemistry and drug development.

Identification of chymotrypsin-like protease inhibitors of SARS-CoV-2 <i>via</i> integrated computational approach
Salman Ali Khan, Komal Zia, Sajda Ashraf, Reaz Uddin +1 more
2020· Journal of Biomolecular Structure and Dynamics345doi:10.1080/07391102.2020.1751298

) of Coronavirus. Considering the severity of the spread of coronavirus, the current study is in-line with the concept of finding the new inhibitors against the vital pathway of the corona virus to expedite the process of drug discovery.Communicated by Ramaswamy H. Sarma.

Application of nanotechnology in agriculture, postharvest loss reduction and food processing: food security implication and challenges
Kumera Neme, Ayman Nafady, Siraj Uddin, Yetenayet B. Tola
2021· Heliyon344doi:10.1016/j.heliyon.2021.e08539

Ensuring food security in developing countries is highly challenging due to low productivity of the agriculture sector, degradation of natural resources, high post farming losses, less or no value addition, and high population growth. Researchers are striving to adopt newer technologies to enhance supply to narrow the food demand gap. Nanotechnology is one of the promising technologies that could improve agricultural productivity via nano fertilizers, use of efficient herbicides and pesticides, soil feature regulation, wastewater management, and pathogen detection. It is equally beneficial for industrial food processing with enhanced food production with excellent market value, elevated nutritional and sensing property, improved safety, and better antimicrobial protection. Nanotechnology can also reduce post-farming losses by increasing the shelf life with the aid of nanoparticles. However, further investigation is required to solve the safety and health risks associated with the technology.

Burden of 375 diseases and injuries, risk-attributable burden of 88 risk factors, and healthy life expectancy in 204 countries and territories, including 660 subnational locations, 1990–2023: a systematic analysis for the Global Burden of Disease Study 2023
Simon I Hay, Kanyin Liane Ong, Damian Santomauro, A Bhoomadevi +4 more
2025· The Lancet326doi:10.1016/s0140-6736(25)01637-x

BACKGROUND: For more than three decades, the Global Burden of Diseases, Injuries, and Risk Factors Study (GBD) has provided a framework to quantify health loss due to diseases, injuries, and associated risk factors. This paper presents GBD 2023 findings on disease and injury burden and risk-attributable health loss, offering a global audit of the state of world health to inform public health priorities. This work captures the evolving landscape of health metrics across age groups, sexes, and locations, while reflecting on the remaining post-COVID-19 challenges to achieving our collective global health ambitions. METHODS: The GBD 2023 combined analysis estimated years lived with disability (YLDs), years of life lost (YLLs), and disability-adjusted life-years (DALYs) for 375 diseases and injuries, and risk-attributable burden associated with 88 modifiable risk factors. Of the more than 310 000 total data sources used for all GBD 2023 (about 30% of which were new to this estimation round), more than 120 000 sources were used for estimation of disease and injury burden and 59 000 for risk factor estimation, and included vital registration systems, surveys, disease registries, and published scientific literature. Data were analysed using previously established modelling approaches, such as disease modelling meta-regression version 2.1 (DisMod-MR 2.1) and comparative risk assessment methods. Diseases and injuries were categorised into four levels on the basis of the established GBD cause hierarchy, as were risk factors using the GBD risk hierarchy. Estimates stratified by age, sex, location, and year from 1990 to 2023 were focused on disease-specific time trends over the 2010-23 period and presented as counts (to three significant figures) and age-standardised rates per 100 000 person-years (to one decimal place). For each measure, 95% uncertainty intervals [UIs] were calculated with the 2·5th and 97·5th percentile ordered values from a 250-draw distribution. FINDINGS: Total numbers of global DALYs grew 6·1% (95% UI 4·0-8·1), from 2·64 billion (2·46-2·86) in 2010 to 2·80 billion (2·57-3·08) in 2023, but age-standardised DALY rates, which account for population growth and ageing, decreased by 12·6% (11·0-14·1), revealing large long-term health improvements. Non-communicable diseases (NCDs) contributed 1·45 billion (1·31-1·61) global DALYs in 2010, increasing to 1·80 billion (1·63-2·03) in 2023, alongside a concurrent 4·1% (1·9-6·3) reduction in age-standardised rates. Based on DALY counts, the leading level 3 NCDs in 2023 were ischaemic heart disease (193 million [176-209] DALYs), stroke (157 million [141-172]), and diabetes (90·2 million [75·2-107]), with the largest increases in age-standardised rates since 2010 occurring for anxiety disorders (62·8% [34·0-107·5]), depressive disorders (26·3% [11·6-42·9]), and diabetes (14·9% [7·5-25·6]). Remarkable health gains were made for communicable, maternal, neonatal, and nutritional (CMNN) diseases, with DALYs falling from 874 million (837-917) in 2010 to 681 million (642-736) in 2023, and a 25·8% (22·6-28·7) reduction in age-standardised DALY rates. During the COVID-19 pandemic, DALYs due to CMNN diseases rose but returned to pre-pandemic levels by 2023. From 2010 to 2023, decreases in age-standardised rates for CMNN diseases were led by rate decreases of 49·1% (32·7-61·0) for diarrhoeal diseases, 42·9% (38·0-48·0) for HIV/AIDS, and 42·2% (23·6-56·6) for tuberculosis. Neonatal disorders and lower respiratory infections remained the leading level 3 CMNN causes globally in 2023, although both showed notable rate decreases from 2010, declining by 16·5% (10·6-22·0) and 24·8% (7·4-36·7), respectively. Injury-related age-standardised DALY rates decreased by 15·6% (10·7-19·8) over the same period. Differences in burden due to NCDs, CMNN diseases, and injuries persisted across age, sex, time, and location. Based on our risk analysis, nearly 50% (1·27 billion [1·18-1·38]) of the roughly 2·80 billion total global DALYs in 2023 were attributable to the 88 risk factors analysed in GBD. Globally, the five level 3 risk factors contributing the highest proportion of risk-attributable DALYs were high systolic blood pressure (SBP), particulate matter pollution, high fasting plasma glucose (FPG), smoking, and low birthweight and short gestation-with high SBP accounting for 8·4% (6·9-10·0) of total DALYs. Of the three overarching level 1 GBD risk factor categories-behavioural, metabolic, and environmental and occupational-risk-attributable DALYs rose between 2010 and 2023 only for metabolic risks, increasing by 30·7% (24·8-37·3); however, age-standardised DALY rates attributable to metabolic risks decreased by 6·7% (2·0-11·0) over the same period. For all but three of the 25 leading level 3 risk factors, age-standardised rates dropped between 2010 and 2023-eg, declining by 54·4% (38·7-65·3) for unsafe sanitation, 50·5% (33·3-63·1) for unsafe water source, and 45·2% (25·6-72·0) for no access to handwashing facility, and by 44·9% (37·3-53·5) for child growth failure. The three leading level 3 risk factors for which age-standardised attributable DALY rates rose were high BMI (10·5% [0·1 to 20·9]), drug use (8·4% [2·6 to 15·3]), and high FPG (6·2% [-2·7 to 15·6]; non-significant). INTERPRETATION: Our findings underscore the complex and dynamic nature of global health challenges. Since 2010, there have been large decreases in burden due to CMNN diseases and many environmental and behavioural risk factors, juxtaposed with sizeable increases in DALYs attributable to metabolic risk factors and NCDs in growing and ageing populations. This long-observed consequence of the global epidemiological transition was only temporarily interrupted by the COVID-19 pandemic. The substantially decreasing CMNN disease burden, despite the 2008 global financial crisis and pandemic-related disruptions, is one of the greatest collective public health successes known. However, these achievements are at risk of being reversed due to major cuts to development assistance for health globally, the effects of which will hit low-income countries with high burden the hardest. Without sustained investment in evidence-based interventions and policies, progress could stall or reverse, leading to widespread human costs and geopolitical instability. Moreover, the rising NCD burden necessitates intensified efforts to mitigate exposure to leading risk factors-eg, air pollution, smoking, and metabolic risks, such as high SBP, BMI, and FPG-including policies that promote food security, healthier diets, physical activity, and equitable and expanded access to potential treatments, such as GLP-1 receptor agonists. Decisive, coordinated action is needed to address long-standing yet growing health challenges, including depressive and anxiety disorders. Yet this can be only part of the solution. Our response to the NCD syndemic-the complex interaction of multiple health risks, social determinants, and systemic challenges-will define the future landscape of global health. To ensure human wellbeing, economic stability, and social equity, global action to sustain and advance health gains must prioritise reducing disparities by addressing socioeconomic and demographic determinants, ensuring equitable health-care access, tackling malnutrition, strengthening health systems, and improving vaccination coverage. We live in times of great opportunity. FUNDING: Gates Foundation and Bloomberg Philanthropies.

Marine natural products of fungal origin
Muhammad Saleem, Muhammad Shaiq Ali, Shafqat Hussain, Abdul Jabbar +2 more
2007· Natural Product Reports321doi:10.1039/b607254m

In the search for novel and bioactive molecules for drug discovery, marine-derived natural resources are becoming an important research area. Over 15 marine-derived secondary metabolites are currently in human clinical trials. Terrestrial fungi have produced many therapeutically significant molecules. However, the potential of marine fungi has only been investigated to a limited extent. This review article contains 103 marine-derived fungal metabolites and 77 references.

Analgesic and Antioxidant Activity of Mangiferin and Its Derivatives: the Structure Activity Relationship
Ahsana Dar, Shaheen Faizi, Sabira Naqvi, Talat Roome +4 more
2005· Biological and Pharmaceutical Bulletin289doi:10.1248/bpb.28.596

Mangiferin, 2-beta-D-glucopyranosyl-1,3,6,7-tetrahydroxy-9H-xanthen-9-one, obtained directly from methanolic extracts of Bombax ceiba leaves in substantial amounts demonstrated strong antioxidant activity (EC(50) 5.8+/-0.96 mug/ml or 13.74 muM) using DPPH assay comparable to rutin, commonly used as antioxidant for medical purposes. The acetyl and cinnamoyl derivatives were found to be less active than mangiferin whereas, methyl and 3,6,7-trimethylether tetraacetate derivatives were inactive implying that for antioxidant activity, free hydroxyl groups and catechol moiety are essential. Moreover, mangiferin showed hepatoprotective activity against carbon tetrachloride induced liver injury further supporting the free radical scavenging property in the in vivo system. Additionally, plant extracts and mangiferin failed to exhibit acute anti-inflammatory activity whereas, it displayed significant analgesic effect in acetic acid-induced writhing and hot plate tests in mice. Using naloxone, it was revealed that plant extracts induced analgesia was independent of opioid receptor, whereas, mangiferin demonstrated significant interaction with it at peripheral site with a slight contribution at the neuronal level.

Scientific challenges in disaster risk reduction for the Sichuan–Tibet Railway
Peng Cui, Yonggang Ge, Shaojun Li, Zhenhong Li +4 more
2022· Engineering Geology279doi:10.1016/j.enggeo.2022.106837

Traversing the Qinghai–Tibetan Plateau, the Sichuan–Tibet Railway is by far the most difficult railway project in the world. The Qinghai–Tibetan Plateau features the most active crustal dynamics on earth, the strongest coupling effects of endogenic and exogenic dynamics, and the environment most sensitive to global climate change. The project area is characterized by extremely cold climate, high elevation and relief, high seismic intensity, high geothermal activity, and high tectonic stress. Consequently, the threat of various disaster risks is ever-present at different stages of the entire life cycle of the Sichuan–Tibet Railway. There is urgent need to systematically study these problems at various levels from the fundamental science to the development of key technologies. This article investigates the different disaster risks recognized during the various stages of construction of the Sichuan–Tibet Railway project, and summarizes the scientific challenges and technical problems faced in relation to disaster risk prevention and control. This work also introduces the scientific deployment and relevant research progress of the Sichuan–Tibet Fund special project initiated by the National Natural Science Foundation of China. Here, we also aim to solve the major fundamental scientific challenges in terms of long-term risk prevention and control during the construction of the Sichuan–Tibet Railway, and lay a theoretical foundation to promote breakthroughs in the bottleneck of key technologies. The scientific challenges addressed in the study of disaster risk associated with the Sichuan–Tibet Railway include the following: The quantitative assessment of the activity of deep-large faults and strong earthquake prediction, the evolution of physical fields in areas of strong tectonic activity, the development mechanisms of tunnel hazards, the slope evolution processes under coupled endogenic and exogenic dynamics in alpine gorges, the impact of climate change on the formation and evolution of surface hazards, and the evolution of extreme wind fields in deep-cut canyons. The technical problems faced in disaster risk prevention and mitigation in relation to the Sichuan–Tibet Railway are as follows: Advanced identification, monitoring, and early warning of geological disasters in mountainous areas with steep and complex terrain; risk analysis, prevention, and control of railway engineering disasters based on their dynamic processes; tunnel engineering hazard monitoring, early warning, risk analysis, prevention, and control technologies; key technologies for emergency response; and the green and resilient railway system and lifecycle risk management. The Sichuan–Tibet Fund special project will include five key research topics: (1) the interior geological structure and dynamic evolution of the eastern plateau; (2) the hazard-inducing mechanisms of coupled internal and external forces in canyons and gullies within plateaus; (3) the cataclysm mechanics of deeply buried long-distance tunnel engineering; (4) risk identification and projection of major disasters affecting the railway; and (5) the integrated management of scientific innovations and super large-scale railway construction. Systematic research is expected to reveal the evolution of earth surface movements and coupled engineering-disturbance related disasters. It will also enable the formation of a comprehensive risk analysis method for major engineering disasters, and promote the development of green, safe, efficient, and resilient engineering disaster risk reduction technologies that will support the disaster risk management during the entire lifecycle of the Sichuan–Tibet Railway.

Paclitaxel: Application in Modern Oncology and Nanomedicine‐Based Cancer Therapy
Javad Sharifi‐Rad, Cristina Quispe, Jayanta Kumar Patra, Yengkhom Disco Singh +4 more
2021· Oxidative Medicine and Cellular Longevity271doi:10.1155/2021/3687700

Nutt. It is a representative of a class of diterpene taxanes, which are nowadays used as the most common chemotherapeutic agent against many forms of cancer. It possesses scientifically proven anticancer activity against, e.g., ovarian, lung, and breast cancers. The application of this compound is difficult because of limited solubility, recrystalization upon dilution, and cosolvent-induced toxicity. In these cases, nanotechnology and nanoparticles provide certain advantages such as increased drug half-life, lowered toxicity, and specific and selective delivery over free drugs. Nanodrugs possess the capability to buildup in the tissue which might be linked to enhanced permeability and retention as well as enhanced antitumour influence possessing minimal toxicity in normal tissues. This article presents information about paclitaxel, its chemical structure, formulations, mechanism of action, and toxicity. Attention is drawn on nanotechnology, the usefulness of nanoparticles containing paclitaxel, its opportunities, and also future perspective. This review article is aimed at summarizing the current state of continuous pharmaceutical development and employment of nanotechnology in the enhancement of the pharmacokinetic and pharmacodynamic features of paclitaxel as a chemotherapeutic agent.

Isatin-derived Antibacterial and Antifungal Compounds and their Transition Metal Complexes
Zahid H. Chohan, Humayun Pervez, Abdur Rauf, Khalid Khan +1 more
2004· Journal of Enzyme Inhibition and Medicinal Chemistry261doi:10.1080/14756360410001710383

A series of isatins incorporating thiazole, thiadiazole, benzothiazole and p-toluene sulfonyl hydrazide moieties, along with their cobalt(II), copper(II), nickel(II) and zinc(II) metal complexes have been synthesized and characterized by elemental analyses, molar conductances, magnetic moments, IR, NMR and electronic spectral data. These compounds have been screened for antibacterial activity against Escherichia coli, Bacillus subtillis, Shigella flexneri, Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella typhi, and for antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani and Candida glaberata using the agar-well diffusion method. All the synthesized compounds have shown good affinity as antibacterial and/or antifungal agents which increased in most of the cases on complexation with the metal ions.