Article
Biochemistry & Molecular Biology
Ya Wang, Xiao-Jing Shen, Fa-Wu Su, Yin-Rong Xie, Li-Xia Wang, Ning Zhang, Yi-Long Wu, Yun Niu, Dong-Ying Zhang, Cheng-Ting Zi, Xuan-Jun Wang, Jun Sheng
Summary: The study synthesized glucoside derivatives of EGCG and found that compounds 11 and 12 showed good growth inhibition in multiple cancer cell lines. The research also explored the relationship between the structure and activity of these derivatives, and it was discovered that perbutyrylated glucose residue enhanced cytotoxic activity.
Article
Biochemistry & Molecular Biology
Min Zou, Jiawen Li, Bo Jin, Mingsheng Wang, Huiping Chen, Zhuangli Zhang, Changzheng Zhang, Zhihong Zhao, Liyun Zheng
Summary: Dual targeting of EGFR/HER2 receptors is an attractive strategy for cancer therapy. Compound 6d, a 4-anilinoquinoline-3-carbonitrile derivative, showed significant antiproliferative activity against SK-BR-3 and A431 cell lines, with potency comparable to Lapatinib and higher than Neratinib. Molecular docking studies indicated the binding modes of compound 6d in EGFR and HER2 binding sites, suggesting it as a potential candidate for further investigation as a potent anticancer agent.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Samar S. Fatahala, Amira Sayed, Shahenda Mahgoub, Heba Taha, Mohamed-I Kotb El-Sayed, Mohamed F. El-Shehry, Samir M. Awad, Rania H. Abd El-Hameed
Summary: The designed and synthesized 2-thiouracil-5-sulfonamides derivatives showed promising anticancer activity and significant inhibition of CDK2A in various human cancer cell lines. The most active compound 6e induced cell growth arrest and apoptotic death in different phases of the cell cycle in cancer cells, ultimately leading to potent anticancer effects. Molecular docking of compound 6e confirmed its proper binding to CDK2A, explaining its strong anticancer activity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Habibullah Khalilullah, Deepak K. Agarwal, Mohamed J. Ahsan, Surender S. Jadav, Hamdoon A. Mohammed, Masood Alam Khan, Salman A. A. Mohammed, Riaz Khan
Summary: A newly designed series of indole-containing pyrazole analogs, pyrazolinylindoles, were synthesized and their anti-cancer activities were tested. Compounds HD02, HD05, and HD12 showed remarkable cytotoxic activities against various types of cancer cell lines, with HD05 exhibiting the highest inhibitory effect. Molecular docking simulation studies confirmed the activity of these compounds.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Carley Giffert L. Nongpiur, Akalesh Kumar Verma, Rohit Kumar Singh, Mayur Mohan Ghate, Krishna Mohan Poluri, Werner Kaminsky, Mohan Rao Kollipara
Summary: A series of new complexes of ruthenium(II), rhodium(III), and iridium(III) with pyrazoline-based ligands were synthesized and characterized. These compounds exhibited good antibacterial activity against Gram-positive bacteria and moderate antioxidant activity. They also showed moderate affinity for binding to Salmon Milt DNA and demonstrated higher cytotoxicity in Dalton's lymphoma cell lines.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Chemistry, Medicinal
Leyla Yurttas, Halide Edip Temel, Mehmet Onur Aksoy, Emre Fatih Bulbul, Gulsen Akalin Ciftci
Summary: The novel synthesized compounds showed high cytotoxicity against lung cancer and fibroblast cells, affecting apoptosis and cell cycle by inducing loss of mitochondrial potential and regulating protein expression.
DRUG DEVELOPMENT RESEARCH
(2022)
Article
Plant Sciences
Ahmed A. Zaki, Ahmed A. Al-Karmalawy, Ahmed E. Khodir, Yasser A. El-Amier, Ahmed Ashour
Summary: A germacranolide and four guaianolide sesquiterpenes were isolated from Reichardia tingitana, with compound 4 and compound 2 showing the highest cytotoxicity among the isolated compounds and promising antitumor activities.
SOUTH AFRICAN JOURNAL OF BOTANY
(2022)
Article
Biochemistry & Molecular Biology
Mateusz Kciuk, Martyna Malinowska, Adrianna Gielecinska, Rajamanikandan Sundaraj, Somdutt Mujwar, Anna Zawisza, Renata Kontek
Summary: This study explored the anticancer potential of novel aminobenzylnaphthols derived from the Betti reaction (MMZ compounds) through in vitro and in silico studies. The compounds exhibited cytotoxic and proapoptotic properties, and showed favorable ADMET profiles. In silico investigations indicated that the anticancer activity of MMZs could be attributed to the inhibition of ADORA1, CDK2, and TRIM24. MMZs constitute an interesting scaffold for the potential development of new anticancer agents.
Article
Chemistry, Medicinal
Lamya H. H. Al-Wahaibi, Anber F. F. Mohammed, Mostafa H. H. Abdelrahman, Laurent Trembleau, Bahaa G. M. Youssif
Summary: A small set of indole-based derivatives, Va-i, demonstrated promising antiproliferative activity against EGFR, BRAF(V600E), and VEGFR-2.
Article
Biochemistry & Molecular Biology
Halil I. Ciftci, Mohamed O. Radwan, Belgin Sever, Ahmed K. Hamdy, Safiye Emirdag, N. Gokce Ulusoy, Ece Sozer, Mustafa Can, Nurettin Yayli, Norie Araki, Hiroshi Tateishi, Masami Otsuka, Mikako Fujita, Mehlika Dilek Altintop
Summary: Compound 10 has been identified as the most potent anti-glioma agent against human glioblastoma cells, and it exerts selective antitumor action towards leukemic T-cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Sinthiya J. Gawandi, Vidya G. Desai, Shrinivas Joshi, Sunil Shingade, Raghuvir R. Pissurlenkar
Summary: In this study, a series of 1,5-benzodiazepine compounds were designed and synthesized, showing promising anticancer activity and strong synergistic effects with Methotrexate. The compounds exhibited superior IC50 values compared to standard drugs, and demonstrated potential as DNA intercalating agents.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Physical
Eman A. Fayed, Rogy R. Ezz Eldin, Ahmed B. M. Mehany, Ashraf H. Bayoumi, Yousry A. Ammar
Summary: Isatin derivatives exhibit significant anti-tumor activity against three human cancer cell lines by inducing apoptosis and cell cycle arrest. The compounds also show effective EGFR inhibitory activity and oral bioavailability without blood-brain barrier permeation. Molecular docking studies revealed a strong binding of the most potent derivative inside the active site of EGFR.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Medicinal
Anthi Petrou, Athina Geronikaki, Victor Kartsev, Antonios Kousaxidis, Aliki Papadimitriou-Tsantarliotou, Marina Kostic, Marija Ivanov, Marina Sokovic, Ioannis Nicolaou, Ioannis S. Vizirianakis
Summary: In this study, the antimicrobial activity of seventeen new derivatives was evaluated. The compounds exhibited strong antibacterial activity against both Gram-positive and Gram-negative bacteria, surpassing the activity of ampicillin and streptomycin by 10-50 fold. The most sensitive bacterium was En. Cloacae, while E. coli and M. flavus were the most resistant ones. Compound 8 was found to be the most potent, and exhibited excellent antifungal activity. Docking studies revealed that the antibacterial activity was likely due to the inhibition of E. coli MurB, while the antifungal mechanism involved inhibition of 14a-lanosterol demethylase of CYP51Ca. Drug-likeness and ADMET profile prediction were also performed, and cytotoxicity studies against normal MRC5 cells were conducted for the most active compounds.
Article
Biochemistry & Molecular Biology
Ali Oubella, Abdoullah Bimoussa, Said Byadi, Yassine Laamari, Mourad Fawzi, Abdellah N'ait Ousidi, Domen Oblack, Aziz Auhmani, Abdelkhalek Riahi, Hamid Morjani, My Youssef Ait Itto
Summary: This study investigated the cytotoxic and apoptotic effects of isoxazoline derivatives in various cancer cell lines. The results showed that these compounds inhibited cell growth and induced apoptosis in HT-1080 fibrosarcoma cells.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Mostafa M. Ghorab, Maged S. Abdel-Kader, Ali S. Alqahtani, Aiten M. Soliman
Summary: The quinazolinone derivatives synthesized from L-norephedrine showed cytotoxicity against various cancer cell lines and selective toxicity towards normal cells. Compounds 5 and 6 demonstrated radiosensitizing activity and induced apoptosis in tumor cells, with compound 5 also arresting the cell cycle at the G2-M phase.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
William M. R. Matshe, Lesego L. Tshweu, Sindisiwe Mvango, Zamani E. D. Cele, Avashnee S. Chetty, Lynne A. Pilcher, Ibukun M. Famuyide, Lyndy J. McGaw, Dale Taylor, Liezl Gibhard, Gregory S. Basarab, Mohammed O. Balogun
Summary: Currently, oral artemisinin-based combination therapy is effective for the treatment of uncomplicated malaria, but there is a lack of intravenous therapy for severe malaria. This is due to the absence of a water-soluble partner drug for artemisinin. A new approach using polymer therapeutics has been developed to create a water-soluble form of the antimalarial lumefantrine for intravenous administration. This polymer-lumefantrine conjugate shows promise for entering clinical use as a combination treatment for severe malaria.
MACROMOLECULAR BIOSCIENCE
(2023)
Article
Plant Sciences
Dorcas A. Gado, Muna Ali Abdalla, Marthie M. Ehlers, Lyndy J. McGaw
Summary: Loxostylis alata is a plant used in South African traditional medicine for pain relief and immune system boost. A compound named 5-demethyl sinensetin, found in the plant, showed antibacterial, antioxidant, and anti-inflammatory activities in vitro. It also exhibited potential cytotoxic effects on certain cell lines. Further research is needed to explore its anticancer properties.
SOUTH AFRICAN JOURNAL OF BOTANY
(2023)
Article
Plant Sciences
Dorcas A. Gado, Muna Ali Abdalla, Joseph O. Erhabor, Marthie M. Ehlers, Lyndy J. McGaw
Summary: Bacterial biofilms pose health challenges in clinical environments and the food industry. The resistance of pathogens to antibiotics is making conventional antibiotic use ineffective. Previous studies found that extracts from Loxostylis alata have antimicrobial potential against bacterial pathogens. In this study, the inhibitory effects of the extracts and a compound from L. alata on biofilm growth and development were investigated. The extracts and compound demonstrated the ability to reduce initial cell attachment and biofilm biomass, but were not able to inhibit the growth of preformed biofilms.
SOUTH AFRICAN JOURNAL OF BOTANY
(2023)
Article
Plant Sciences
Eucharia C. Ogbuadike, Sanah M. Nkadimeng, Chima C. Igwe, Jean P. Dzoyem, Daniel N. Qekwana, Inge-Marie Petzer, Lyndy J. McGaw
Summary: This study investigated the antimicrobial, anti-biofilm, and anti-quorum sensing activities of selected plants against Staphylococcus aureus isolates from clinical cases of bovine mastitis. Four plants, including Maytenus undata, Maurocenia frangula, Kalan-choe gunniae, and Bryophyllum pinnatum, showed promising activities. Kalanchoe gunniae extracts exhibited the best anti-quorum sensing activity.
SOUTH AFRICAN JOURNAL OF BOTANY
(2023)
Article
Plant Sciences
Jacobus Kori Madisha, Lyndy Joy McGaw
Summary: This study investigated the indigenous knowledge of plants used to treat respiratory and dermatological infections in livestock in the Sekhukhune district of South Africa. Ethnoveterinary data were collected from farmers and traditional healers, and 24 plant species were identified as commonly used for these ailments. The study highlights the extensive use of plant preparations in rural areas where access to orthodox veterinary healthcare is limited.
SOUTH AFRICAN JOURNAL OF BOTANY
(2023)
Article
Plant Sciences
T. E. Ramadwa, M. A. Selepe, M. S. Sonopo, L. J. McGaw, J. N. Eloff
Summary: The study aimed to develop a method for quantifying obliquumol in Ptaeroxylon obliquum leaves using UPLC-MS/MS and investigate the biological activity of ptaeroxylinol. Obliquumol was isolated from the leaves and converted to ptaeroxylinol. The method was able to quantify obliquumol in different P. obliquum extracts, and ptaeroxylinol showed good antimicrobial activity with low cytotoxicity. Rating: 8/10
SOUTH AFRICAN JOURNAL OF BOTANY
(2023)
Article
Chemistry, Multidisciplinary
Ayodele O. Akinboye, Ibukun M. Famuyide, Inge-Marie Petzer, Lyndy J. McGaw
Summary: Bovine mastitis in dairy livestock production is a serious economic problem caused by Staphylococcus aureus and non-aureus staphylococcus. Antimicrobial resistance hampers control of mastitis. Nine South African plants were tested for their antibacterial and cytotoxic activities against mastitis-causing staphylococci. The extracts showed promising antibacterial effects and low cytotoxicity, particularly the acetone extracts. Further investigation is recommended.
APPLIED SCIENCES-BASEL
(2023)
Article
Chemistry, Multidisciplinary
Emmanuel Mfotie Njoya, Hermine L. D. Maza, Shasank S. Swain, Chika. I. Chukwuma, Pierre Mkounga, Yves M. Nguekeu Mba, Samson S. Mashele, Tshepiso J. Makhafola, Lyndy J. McGaw
Summary: This study aims to investigate the anti-inflammatory and acetylcholinesterase (AChE) inhibitory potentials of three medicinal plants against brain-dysfunction diseases and inflammation. The crude extracts and isolated compounds were tested in vitro for their AChE inhibitory activity and anti-inflammatory activity. It was found that Tapinanthus bangwensis had the most active AChE inhibitory potential, and six natural compounds were identified as having anti-AChE potential. These compounds could be important candidates for further experimental studies on Alzheimer's disease and inflammation.
APPLIED SCIENCES-BASEL
(2023)
Article
Chemistry, Inorganic & Nuclear
Malose J. Mphahlele, Nontokozo M. Magwaza, Samantha Gildenhuys, Garland K. More, Sizwe J. Zamisa, Morole M. Maluleka
Summary: The secondary sulfonamido group is important in pharmacologically active organic molecules, and the incorporation of fluorine atom/s or fluorine-containing group/s on the aromatic ring can enhance their efficacy. In this study, ortho-arylsulfonamidoacetophenone derivatives substituted with fluorine atom/s or fluorine-containing group/s were synthesized, and the N-4(trifluoromethylbenzene)sulfonyl derivative showed the highest inhibitory activity against COX-1, COX-2, and VEGFR-2 tyrosine kinase compared to standard drugs.
JOURNAL OF FLUORINE CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Malose J. Mphahlele, Garland K. More, Marole M. Maluleka, Yee Siew Choong
Summary: A series of 2-nitrochalcones were synthesized and evaluated for their cytotoxicity against A549 and HEK293-T cell lines. Compound 3c and 3k induced early and late apoptosis of A549 cells. Furthermore, compounds 3c, 3h, 3j, and 3k exhibited significant inhibitory activity against VEGFR-2 tyrosine kinase.
MEDICINAL CHEMISTRY RESEARCH
(2023)
Review
Biochemistry & Molecular Biology
Chong Lee Ng, Theam Soon Lim, Yee Siew Choong
Summary: Since the development of hybridoma technology in 1975, continuous efforts have been made to engineer antibodies, including both the variable domains and the fragment crystallizable (Fc) region. Integrating computational techniques into antibody engineering designs allows for testable hypotheses and rational antibody design framework. This article discusses recent research on Fc-fused molecule design involving computational techniques and summarizes the usefulness of in silico techniques in therapeutic applications.
MOLECULAR BIOTECHNOLOGY
(2023)
Article
Plant Sciences
J. Van Wyngaard, I. M. Famuyide, L. Invernizzi, K. K. Ndivhuwo, A. S. W. Tordiffe, V. J. Maharaj, L. J. Mcgaw
Summary: Pelargonium sidoides is an important indigenous medicinal plant in South Africa, traditionally used to treat respiratory and gastrointestinal ailments. The study found that the 60% ethanol extracts from the roots exhibited superior antibacterial and antifungal activity, and polyphenol content may serve as a more reliable indicator of antimicrobial activity than umckalin levels.
SOUTH AFRICAN JOURNAL OF BOTANY
(2023)
Article
Plant Sciences
A. G. Omokhua-Uyi, B. Madikizela, A. O. Aro, M. A. Abdalla, J. Van Staden, L. J. McGaw
Summary: This study evaluated the antimycobacterial and hepatoprotective potentials of extracts and isolated flavonoid compounds from invasive Chromolaena odorata. The extracts and compounds showed promising antimycobacterial activity and minimal toxicity, suggesting their potential as leads for the development of safe and effective anti-tubercular drugs. Additionally, the flavonoid compounds exhibited hepatoprotective effects, improving cell viability in liver cells treated with a toxin.
SOUTH AFRICAN JOURNAL OF BOTANY
(2023)
Article
Plant Sciences
Mirela Uzelac, Barbara Sladonja, Ivana Sola, Slavica Dudas, Josipa Bilic, Ibukun M. Famuyide, Lyndy J. McGaw, Jacobus N. Eloff, Maja Mikulic-Petkovsek, Danijela Poljuha
Summary: Black locust, an invasive tree in Europe, has a rich composition of phenolic compounds with potential pharmaceutical use. The study conducted LC-MS screening of black locust from Croatia and found that the leaves had higher levels of total phenolics, flavonoids, and antioxidant capacity compared to the flowers. Ethanol extracts showed higher levels of total phenolics and non-flavonoids. A total of 64 compounds were identified, with flavonols and hydroxycinnamic acid derivatives being the most commonly represented. The extracts exhibited promising quorum sensing, biofilm prevention, and eradicating capacity.
Article
Chemistry, Physical
Malose J. Mphahlele, Tarek M. El-Gogary, Sizwe J. Zamisa
Summary: The structures of 2-hydroxy-3-iodo-6-methoxyacetophenone and 2-hydroxy-3-iodo-6-methoxybenzaldehyde were elucidated using spectroscopic techniques and X-ray diffraction analysis. The study also investigated the hydrogen bonding and halogen bonding affinity of these compounds.
JOURNAL OF MOLECULAR STRUCTURE
(2023)