Design, Synthesis, Docking Studies and Molecular Dynamics Simulation of New 1,3,5-Triazine Derivatives as Anticancer Agents Selectively Targeting Pancreatic Adenocarcinoma (Capan-1)
Chem Biodivers. 2024 Apr 12:e202400112. doi: 10.1002/cbdv.202400112. Online ahead of print.ABSTRACTOn the basis of remarkable anticancer profile of s-triazine nucleus, a new series of 2-methoxy-4-(3-morpholino-5-(arylamino)phenoxy)benzaldehyde derivatives 11 a-u was prepared and evaluated for in vitro antiproliferative activity against eight diverse human cancer cell lines (Capan-1, HCT-116, LN229, NCI-H460, DND-41, HL-60, K562 and Z138). Compounds 11 o, 11 r and 11 s were the most potent anticancer agents on pancreatic adenocarcinoma (Capan-1) cell line with IC50 value of 1.4, 5.1 and 5.3 μM, respectively, while compound...
Source: Chemistry and Biodiversity - April 12, 2024 Category: Biochemistry Authors: Shazia Asghar Shahid Hameed Najim A Al-Masoudi Bahjat Saeed Amneh Shtaiwi Source Type: research
Active Constituents with Tyrosinase Inhibitory Activities from Waste Tobacco leaves
Chem Biodivers. 2024 Apr 12:e202400463. doi: 10.1002/cbdv.202400463. Online ahead of print.ABSTRACTOne novel compound, (R)-3, 6-diethoxy-4-hydroxycyclohex-3-en-1-one (1) and thirteen known compounds was isolated from the waste leaves of Nicotiana tabacum. The structures of three compounds (1-3) were confirmed and attributed firstly by the extensive spectroscopic data, including 1D/2D NMR, IR, HR-ESI-MS, CD, and ECD spectra. Notably, seven compounds (2, 3, 9, 10, 11, 12, and 13) exhibited better tyrosinase inhibitory activity than the positive control, kojic acid. The binding modes of these compounds revealed that their str...
Source: Chemistry and Biodiversity - April 12, 2024 Category: Biochemistry Authors: Shu Zhen Mu Mei Zhang Jia-Yu Sun Hong-Mao Qiu Peng Zhang Lu-Lu Deng Jiang Li Xiao-Jiang Hao Xian-Kun Su Source Type: research
CYTOTOXICITY AND BIOLOGICAL ACTIVITIES OF GEOPOPOLIS EXTRACT FROM THE STINGLESS BEE (Melipona scutellaris) IN CLINICAL ISOLATES OF Staphylococcus aureus
Chem Biodivers. 2024 Apr 12:e202301982. doi: 10.1002/cbdv.202301982. Online ahead of print.ABSTRACTThis work aims to evaluate the biological activities of the EEGP, in order to contribute with a natural therapeutic alternative, to face infections. The EEGP MIC tests showed antibacterial activity against two strains of S. aureus (LPM 63 and LPM 86), both at concentrations of 550 µg/mL. The MBC performed with the inhibition values showed that the EEGP has bacteriostatic activity in both strains. Biofilm inhibition rates exhibited an average value greater than 65% at the highest concentration. The EEGP antioxidant potential ...
Source: Chemistry and Biodiversity - April 12, 2024 Category: Biochemistry Authors: Maria Gabriella Borges Luanna Lima Ana Caroline Veras Rafael Ferreira Danielle Alves Isac Medeiros Marciane Magnani Marianna Sobral Ricardo Castro Saulo Tintino Cicera Oliveira-Tintino Henrique Coutinho Felipe Guerra Daniela Barros Maria Bet ânia Oliveir Source Type: research
Investigations of Limeum indicum Plant for Diabetes Mellitus and Alzheimer's disease Dual Therapy: Phytochemical, GC-MS Chemical Profiling, Enzyme Inhibition, Molecular Docking and In-vivo Studies
Chem Biodivers. 2024 Apr 12:e202301858. doi: 10.1002/cbdv.202301858. Online ahead of print.ABSTRACTLimeum indicum has been widely utilized in traditional medicine but no experimental work has been done on this herb. The primary objective of this study was to conduct a phytochemical analysis and assess the multifunctional capabilities of aforementioned plant in dual therapy for Alzheimer's disease (AD) and Type 2 diabetes (T2D). The phytochemical screening of ethanol, methanol extract, and their derived fractions of Limeum indicum was conducted using GC-MS, HPLC, UV-analysis and FTIR. The antioxidant capacity was evaluated ...
Source: Chemistry and Biodiversity - April 12, 2024 Category: Biochemistry Authors: Tahira Shamim Hafiz Muhammad Asif Syeda Abida Ejaz Zahid Hussain Tanveer A Wani Laila Sumreen Muhammad Abdullah Zubair Ahmed Jamshed Iqbal Song Ja Kim Muhammad Kamal Shah Source Type: research
Retrobisabolane A, a Novel Bisabolane-Derived Sesquiterpenoid Isolated from Deep-Sea-Derived Fungus Retroconis fusiformis MCCC 3A00792
Chem Biodivers. 2024 Apr 12:e202400805. doi: 10.1002/cbdv.202400805. Online ahead of print.ABSTRACTOne novel bisabolane-derived sesquiterpenoid retrobisabolane A (1), featuring a methyl group location at the C-4 position instead of C-3 in the bisabolanes, and a known ester-substituted eremophilane-type sesquiterpenoid cryptosphaerolide (2), along with three known indole alkaloids (3‒5) were discovered from the fermented cultures of a deep-sea-derived fungus Retroconis fusiformis MCCC 3A00792. The planar structure of new compound 1 was determined by extensive analysis of the NMR and HRESIMS spectra. The relative and absol...
Source: Chemistry and Biodiversity - April 12, 2024 Category: Biochemistry Authors: Xin Liu Yinghui Lv Jianlin He Bihong Hong Zongze Shao Miao Yu Siwen Niu Source Type: research
Sulfated Polysaccharides with Anticoagulant Potential: A Review Focusing on Structure-Activity Relationship and Action Mechanism
Chem Biodivers. 2024 Apr 10:e202400152. doi: 10.1002/cbdv.202400152. Online ahead of print.ABSTRACTThromboembolism is the culprit of cardiovascular diseases, leading to the highest global mortality rate. Anticoagulation emerges as the primary approach for managing thrombotic conditions. Notably, sulfated polysaccharides exhibit favorable anticoagulant efficacy with reduced side effects. This review focuses on the structure-anticoagulant activity relationship of sulfated polysaccharides and the underlying action mechanisms. It is concluded that chlorosulfonicacid-pyridine method serves as the preferred technique to synthesi...
Source: Chemistry and Biodiversity - April 11, 2024 Category: Biochemistry Authors: Qianfeng Chen Mengjiao Zhang Yue Liu Wei Liu Cheng Peng Lixue Zheng Source Type: research
Diaporchalasins A-E, New Cytochalasins from the Endophytic Fungus Diaporthe sp. BMX12 Isolated from Aquilaria sinensis
Chem Biodivers. 2024 Apr 11:e202400567. doi: 10.1002/cbdv.202400567. Online ahead of print.ABSTRACTFive new cytochalasins, diaporchalasins A-E (1-5), together with 14 known congeners (6-19) were isolated from the endophytic fungus Diaporthe sp. BMX12, which was isolated from the branches of Aquilaria sinensis. The structures of the new compounds were elucidated by extensive spectroscopic analyses including high-resolution electron spray ionization mass spectrometry (HRESIMS) and nuclear magnetic resonance (NMR). Their absolute configurations were assigned by theoretical electronic circular dichroism (ECD) calculations. Com...
Source: Chemistry and Biodiversity - April 11, 2024 Category: Biochemistry Authors: Li Yang Qi Wang Qing-Yun Ma Qing-Yi Xie Cui-Juan Gai You-Gen Wu Hao-Fu Dai Zhao Youxing Source Type: research
Design, Synthesis, and Biological Evaluation of Novel Quinazoline Derivatives Possessing a Trifluoromethyl Moiety as Potential Antitumor Agents
Chem Biodivers. 2024 Apr 11:e202301776. doi: 10.1002/cbdv.202301776. Online ahead of print.ABSTRACTA novel series of trifluoromethyl-containing quinazoline derivatives with a variety of functional groups was designed, synthesized, and tested for their antitumor activity by following a pharmacophore hybridization strategy. Most of the 20 compounds displayed moderate to excellent antiproliferative activity against five different cell lines (PC3, LNCaP, K562, HeLa, and A549). After three rounds of screening and structural optimization, compound 10 b was identified as the most potent one, with IC50 values of 3.02, 3.45, and 3....
Source: Chemistry and Biodiversity - April 11, 2024 Category: Biochemistry Authors: Mingxiu Chen Sha Cheng Xing Dai Jia Yu HuiDi Wang BiXue Xu Heng Luo Guangcan Xu Source Type: research
Industrial Distillation Fractions of Garlic Essential Oil, Design, Synthesis, and Antifungal Activity Evaluation of Aliphatic Substituted Trisulfide Derivatives
In this study, enzymatic treatment of garlic resulted in an increase of approximately 50 % in the yield of essential oil, a feasible GC-MS analytical program for garlic oil was provided. Vacuum fractionation of the volatile oil and determination of its inhibitory activity against 10 fungi demonstrated that garlic oil has good antifungal activity. The antifungal activity levels were ranked as diallyl trisulfide (S-3)>diallyl disulfide (S-2)>diallyl monosulfide (S-1), with an EC50 value of S-3 against Botrytis cinerea reached 8.16 mg/L. Following the structural modification of compound S-3, a series of derivatives, inc...
Source: Chemistry and Biodiversity - April 11, 2024 Category: Biochemistry Authors: Yao Chen Hui Wang Haiyang Wang Jie Gao Yamin Huang Yu Zhang Xianhai Lv Source Type: research
Sulfated Polysaccharides with Anticoagulant Potential: A Review Focusing on Structure-Activity Relationship and Action Mechanism
Chem Biodivers. 2024 Apr 10:e202400152. doi: 10.1002/cbdv.202400152. Online ahead of print.ABSTRACTThromboembolism is the culprit of cardiovascular diseases, leading to the highest global mortality rate. Anticoagulation emerges as the primary approach for managing thrombotic conditions. Notably, sulfated polysaccharides exhibit favorable anticoagulant efficacy with reduced side effects. This review focuses on the structure-anticoagulant activity relationship of sulfated polysaccharides and the underlying action mechanisms. It is concluded that chlorosulfonicacid-pyridine method serves as the preferred technique to synthesi...
Source: Chemistry and Biodiversity - April 11, 2024 Category: Biochemistry Authors: Qianfeng Chen Mengjiao Zhang Yue Liu Wei Liu Cheng Peng Lixue Zheng Source Type: research
Diaporchalasins A-E, New Cytochalasins from the Endophytic Fungus Diaporthe sp. BMX12 Isolated from Aquilaria sinensis
Chem Biodivers. 2024 Apr 11:e202400567. doi: 10.1002/cbdv.202400567. Online ahead of print.ABSTRACTFive new cytochalasins, diaporchalasins A-E (1-5), together with 14 known congeners (6-19) were isolated from the endophytic fungus Diaporthe sp. BMX12, which was isolated from the branches of Aquilaria sinensis. The structures of the new compounds were elucidated by extensive spectroscopic analyses including high-resolution electron spray ionization mass spectrometry (HRESIMS) and nuclear magnetic resonance (NMR). Their absolute configurations were assigned by theoretical electronic circular dichroism (ECD) calculations. Com...
Source: Chemistry and Biodiversity - April 11, 2024 Category: Biochemistry Authors: Li Yang Qi Wang Qing-Yun Ma Qing-Yi Xie Cui-Juan Gai You-Gen Wu Hao-Fu Dai Zhao Youxing Source Type: research
Design, Synthesis, and Biological Evaluation of Novel Quinazoline Derivatives Possessing a Trifluoromethyl Moiety as Potential Antitumor Agents
Chem Biodivers. 2024 Apr 11:e202301776. doi: 10.1002/cbdv.202301776. Online ahead of print.ABSTRACTA novel series of trifluoromethyl-containing quinazoline derivatives with a variety of functional groups was designed, synthesized, and tested for their antitumor activity by following a pharmacophore hybridization strategy. Most of the 20 compounds displayed moderate to excellent antiproliferative activity against five different cell lines (PC3, LNCaP, K562, HeLa, and A549). After three rounds of screening and structural optimization, compound 10 b was identified as the most potent one, with IC50 values of 3.02, 3.45, and 3....
Source: Chemistry and Biodiversity - April 11, 2024 Category: Biochemistry Authors: Mingxiu Chen Sha Cheng Xing Dai Jia Yu HuiDi Wang BiXue Xu Heng Luo Guangcan Xu Source Type: research
Industrial Distillation Fractions of Garlic Essential Oil, Design, Synthesis, and Antifungal Activity Evaluation of Aliphatic Substituted Trisulfide Derivatives
In this study, enzymatic treatment of garlic resulted in an increase of approximately 50 % in the yield of essential oil, a feasible GC-MS analytical program for garlic oil was provided. Vacuum fractionation of the volatile oil and determination of its inhibitory activity against 10 fungi demonstrated that garlic oil has good antifungal activity. The antifungal activity levels were ranked as diallyl trisulfide (S-3)>diallyl disulfide (S-2)>diallyl monosulfide (S-1), with an EC50 value of S-3 against Botrytis cinerea reached 8.16 mg/L. Following the structural modification of compound S-3, a series of derivatives, inc...
Source: Chemistry and Biodiversity - April 11, 2024 Category: Biochemistry Authors: Yao Chen Hui Wang Haiyang Wang Jie Gao Yamin Huang Yu Zhang Xianhai Lv Source Type: research
Revealing the 1H NMR Profiling of Six Edible Mushrooms Consumed in the Northeastern Highlands of Puebla, Mexico
Chem Biodivers. 2024 Apr 10:e202301851. doi: 10.1002/cbdv.202301851. Online ahead of print.ABSTRACTThe 1H NMR metabolomics profiling of six edible mushrooms consumed in the northeastern highlands of Puebla, Mexico is presented. These fungi were morpho- and molecularly identified as Infundibulicybe squamulosa, Amanita jacksonii, Lepista nuda, Russula delica, Russula brevipes, and Lactarius indigo. The chemical profiling confirmed the presence of eight essential amino acids and their derivatives, six organic acids, six nucleosides, low amounts of reducing sugars, and valuable nutraceuticals such as betaine, carnitine, glycer...
Source: Chemistry and Biodiversity - April 10, 2024 Category: Biochemistry Authors: Yesenia Pacheco-Hern ández Nemesio Villa-Ruano Edmundo Lozoya-Gloria Estafania de Jesus Ter án-Sánchez Elvia Becerra-Mart ínez Source Type: research
Transforming Pharmaceutical Synthesis with Sein-E-B Nanocomposite Photocatalyst through 1,4-NAD(P)H Cofactor Regeneration and C-N Bond Activation
Chem Biodivers. 2024 Apr 8:e202400329. doi: 10.1002/cbdv.202400329. Online ahead of print.ABSTRACTThe need for sunlight chemical renewal and contemporary organic transformation has fostered the advancement of environmentally friendly photocatalytic techniques. For the first time, we report on the novel crafting of a bright future with selenium-infused Eosin-B (Sein-E-B) nanocomposite photocatalysts in this work. The Sein-E-B nanocomposite materials were created using a hydrothermal process for solar chemical regeneration and organic transformation under visible light. The synthesized samples were subjected to UV-DRS-visibl...
Source: Chemistry and Biodiversity - April 9, 2024 Category: Biochemistry Authors: Ravindra Shukla Rajesh Yadav Vitthal Gole Rajat Singhal Rehana Shahin Shaifali Mishra Satyam Singh Kanchan Sharma Jin-Ook Baeg Gamal El-Hiti Krishna Yadav Navneet Kumar Gupta Source Type: research
