“In-silico Design and Development of Novel Hydroxyurea
Lipid Drug Conjugates for Breast Cancer Therapy Targeting
PI3K/AKT/mTOR Pathway”
Drug Res (Stuttg) 2024; 74: 32-41 DOI: 10.1055/a-2213-8457Hydroxyurea (HU) has shown promise in breast cancer treatment, but its
hydrophilic nature limits its efficacy. Therefore, conjugating HU with lipids
could increase its liphophilicity and improve its cellular uptake, leading to
increased efficacy and reduced toxicity. The PI3K/Akt/mTOR
pathway is an attractive therapeutic target in cancer not only because it is the
second most frequently altered pathway after p53, but also because it serves as
a convergence point for many stimuli. The aim of this study is to...
Source: Drug Research - January 11, 2024 Category: Drugs & Pharmacology Authors: Dharmaraj, Saranya Swaroop, Akey Krishna Esakkimuthukumar, Mariappan Negi, Preeya Jubie, Selvaraj Tags: Original Article Source Type: research
Quality by Design in Pharmaceuticals: A Review of its Impact on
Regulatory Compliance and Product Quality
In conclusion, by embracing the QbD approach, the pharmaceutical
industry can ensure the production of safe, effective and regulation-compliant
products while simultaneously improving process efficiency. This strategic shift
toward QbD represents a pivotal step in advancing pharmaceutical research and
manufacturing capabilities, ultimately benefiting both the industry and more
importantly, patients worldwide. [...] Georg Thieme Verlag Rüdigerstraße 14, 70469 Stuttgart,
GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Drug Research)
Source: Drug Research - December 22, 2023 Category: Drugs & Pharmacology Authors: Nunavath, Raja Shekhar Singh, Madhu Tanya Jain, Anubha Chakma, Marjita Arivuselvam, Rajaguru Azeeze, Mohamed Sheik Tharik Abdul Tags: Review Source Type: research
Structure-Based Drug Design for Targeting IRE1: An in Silico
Approach for Treatment of Cancer
Conclusion Our results revealed that designed compound 17 could inhibit
IRE1 activity. Therefore, this designed compound is a remarkable inhibitor of
IRE1 and introduces a promising therapeutic strategy for cancer treatment. [...] Georg Thieme Verlag Rüdigerstraße 14, 70469 Stuttgart,
GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Drug Research)
Source: Drug Research - December 22, 2023 Category: Drugs & Pharmacology Authors: Poustforoosh, Alireza Faramarz, Sanaz Nematollahi, Mohammad Hadi Mahmoodi, Mehdi Azadpour, Mahdiyeh Tags: Original Article Source Type: research
Dermaceutical Utilization of Nigella sativa Seeds:
Applications and Opportunities
Drug Res (Stuttg) DOI: 10.1055/a-2196-1815Skin diseases have recently become a major concern among people of all ages due
to their highly visible symptoms and persistent and difficult treatment, which
significantly impact their quality of life. Nigella sativa seeds, also
known as "black seeds" or "kalonji," are one of
the most commonly used herbal medicines due to their wide range of biological
and pharmacological activities. It contains a wide range of bioactive
constituents found in both fixed and essential oils. It has been used for
hundreds of years ...
Source: Drug Research - November 28, 2023 Category: Drugs & Pharmacology Authors: Khatoon, Mariyam Kushwaha, Poonam Usmani, Shazia Madan, Kumud Tags: Review Source Type: research
Parenteral Fosfomycin in Gastrointestinal Surgery: A Systematic
Review
Conclusion There were few postoperative infectious complications after
perioperative parenteral administration of one or more doses of 4 g fosfomycin
supplemented with metronidazole in various gastrointestinal procedures.
Fosfomycin was associated with few and mild harms. [...] Georg Thieme Verlag Rüdigerstraße 14, 70469 Stuttgart,
GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Drug Research)
Source: Drug Research - November 28, 2023 Category: Drugs & Pharmacology Authors: Fonnes, Siv Fonnes, Masja Klindt Holzknecht, Barbara Juliane Rosenberg, Jacob Tags: Review Source Type: research
Effects of Resveratrol Co-Administration on Celecoxib Disposition and
Pharmacokinetics in Healthy Volunteers
The objective of the current study was to investigate the effects of resveratrol
(RSV), a natural herbal remedy used as an adjacent anti-inflammatory supplement
on, the pharmacokinetics of celecoxib in healthy male volunteers. Twelve healthy
human participants were involved in two-period open-labeled trial. Celecoxib
(200 mg) was given as a single oral dose under fasting conditions as a
control phase. Afterward, RSV (500 mg) commenced as a single oral dose
for ten days as a treatment phase. Blood samples were collected during the
control and treatmen...
Source: Drug Research - November 7, 2023 Category: Drugs & Pharmacology Authors: Helal, Nagwa I. El-Khodary, Noha M. Omran, Gamal A. El-Masry, Soha M. Tags: Original Article Source Type: research
Diuretic, Natriuretic, And Ca2+-Sparing Effect Of
The Alkaloid Boldine In Rats
Conclusions This study reveals the diuretic, natriuretic,
Ca2+-sparing, and antiurolithiatic effects of boldine, an
action possibly related to muscarinic receptor activation and prostanoid
generation. [...] Georg Thieme Verlag Rüdigerstraße 14, 70469 Stuttgart,
GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Drug Research)
Source: Drug Research - November 7, 2023 Category: Drugs & Pharmacology Authors: Steimbach, Viviane Miranda Bispo da Silva, Ritade C ássia Vilhena Mariano, Lu ísa Nathália Bolda Zanovello, Mariana Macarini, Anelise Fel ício da Silva, Luisa Mota de Souza, Priscila Tags: Original Article Source Type: research
Inotodiol ameliorates the progression of osteoarthritis: An in
vitro and in vivo study
Drug Res (Stuttg) 2023; 73: 506-512 DOI: 10.1055/a-2176-4098Osteoarthritis is a common chronic degenerative disease, of which the essence is
the degenerative changes of bone and joint cartilage, involving damage in
multiple structures such as bone, synovium and joints. In the mechanism of
arthritis inflammation is closely related, and therefore the exploration to
inhibit inflammatory mediators is crucial for the clinical prevention and
treatment of osteoarthritis. Inotodiol is a lanostane triterpenoid isolated from
Inonotus obliquus, which had been extensively rep...
Source: Drug Research - November 7, 2023 Category: Drugs & Pharmacology Authors: Qian, Wanfeng Ji, Ruheng Ye, Qiujie Hu, Wenjun Zhou, Linying Pan, Hongwu Li, Xiaoming Tags: Original Article Source Type: research
A Review of PARP-1 Inhibitors: Assessing Emerging Prospects and
Tailoring Therapeutic Strategies
Drug Res (Stuttg) DOI: 10.1055/a-2181-0813Eukaryotic organisms contain an enzyme family called poly (ADP-ribose)
polymerases (PARPs), which is responsible for the poly (ADP-ribosylation) of
DNA-binding proteins. PARPs are members of the cell signaling enzyme class.
PARP-1, the most common isoform of the PARP family, is responsible for more than
90% of the tasks carried out by the PARP family as a whole. A
superfamily consisting of 18 PARPs has been found. In order to synthesize
polymers of ADP-ribose (PAR) and nicotinamide, the DNA damage nick monitor
PA...
Source: Drug Research - October 27, 2023 Category: Drugs & Pharmacology Authors: Ramesh, Soundarya Almeida, Shannon D Hammigi, Sameerana Radhakrishna, Govardan Katta Sireesha, Golla Panneerselvam, Theivendren Vellingiri, Shangavi Kunjiappan, Selvaraj Ammunje, Damodar Nayak Pavadai, Parasuraman Tags: Review Source Type: research
Evaluation and Comparison of Citalopram and Venlafaxine for
Management of Hot Flashes in Women with Breast Cancer
Conclusions Although citalopram was associated with more adverse effects,
including constipation, it was more effective in reducing the frequency of hot
flashes when compared to venlafaxine or placebo. [...] Georg Thieme Verlag Rüdigerstraße 14, 70469 Stuttgart,
GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Drug Research)
Source: Drug Research - August 30, 2023 Category: Drugs & Pharmacology Authors: Taleghani, Sasan Yaghoobi Etesam, Farnaz Esfandbod, Mohsen Tags: Original Article Source Type: research
Lupeol: A Triterpenoid Isolated from the Stem Bark of Hymenocardia
Acida (tul.) Exhibits a van der Waal Antagonism on the Alpha Subunit of Gastric
H+K+Atpase – A Promising Antiulcer
Principle
Conclusion The experimental studies justify the ethnomedicinal claim of
usage among locals. [...] Georg Thieme Verlag Rüdigerstraße 14, 70469 Stuttgart,
GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Drug Research)
Source: Drug Research - August 25, 2023 Category: Drugs & Pharmacology Authors: Oluwasegun, Adedokun Ogochukwu, Ume Ugochukwu, Ojukwu Mussaddiq, Ismail Bunyamin, Ayinde Tags: Original Article Source Type: research
Altered Gene Expression of Cytochrome P450 and ABC Transporter in
Human Hepatocellular Carcinoma HepG2 Cells Exposed to Bardoxolone
Methyl
In conclusion, this study demonstrated that the gene expression
of several CYPs and ABC transporters in HepG2 cells was altered when exposed to
BX, suggesting the need to pay careful attention to drug-drug interactions in
patients receiving BX for CKD treatment. [...] Georg Thieme Verlag Rüdigerstraße 14, 70469 Stuttgart,
GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Drug Research)
Source: Drug Research - August 17, 2023 Category: Drugs & Pharmacology Authors: Nagai, Katsuhito Fukuno, Shuhei Miura, Takeshi Yasuda-Imanishi, Eri Konishi, Hiroki Tags: Short Communication Source Type: research
GC-MS analysis and in silico docking of constituents of Cinnamomum
malabatrum against CYP450 17 α and CYP450 19 (Aromatase)- Key targets for
hyperandrogenism
In conclusion, this work throws a
new insight into the possibility of the active phytoconstituents on binding the
two active CYP45017 α and CYP45019 aromatase
enzymes which facilitates development of novel compounds for hyperandrogenism
associated with PCOS. [...] Georg Thieme Verlag Rüdigerstraße 14, 70469 Stuttgart,
GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Drug Research)
Source: Drug Research - August 17, 2023 Category: Drugs & Pharmacology Authors: Soumya, V. Deepa, S. Thachil, Knolin.K. Saravanan, J. Hariprasad, R. Tags: Original Article Source Type: research
Nitrosamine Impurities in Herbal Formulations: A Review of Risks and
Mitigation Strategies
In conclusion, the
presence of nitrosamines is not limited to pharmaceutical products and poses a
significant threat to the safety of herbal drugs as well. Adequate testing and
extensive research are crucial for producing and distributing herbal medicines
to the general population. [...] Georg Thieme Verlag Rüdigerstraße 14, 70469 Stuttgart,
GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Drug Research)
Source: Drug Research - July 24, 2023 Category: Drugs & Pharmacology Authors: Shekhar, Nunavath Raja Nagappan, Krishnaveni Singh, Madhu Tanya Dhanabal, S. P. Tags: Review Source Type: research
In silico docking and Molecular Dynamic (MD) simulations studies of
selected phytochemicals against Human Glycolate Oxidase (hGOX) and Oxalate
oxidase (OxO)
We present the
results of in silico docking and molecular dynamic (MD) simulation
studies on selected phytochemical including catechin, epicatechin, gallic acid,
gallocatechin, epigallocatechin, epigallocatechin 3-o-gallate,
4-methoxy-nor-securine, nor-securinine, and fisetin with human glycolate oxidase
(hGOX) and oxalate oxidase (OxO). Gallic acid, gallocatechin and fisetin showed
better docking scores than the rest. In MD simulation analysis, stable
interactions of the gallic acid with hGOX and OxO; gallocatechin and fisetin
with hGOX were o...
Source: Drug Research - July 24, 2023 Category: Drugs & Pharmacology Authors: Nageswari, Patnam Swathi, K Tags: Original Article Source Type: research
