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Plant Species from the Atlantic Forest Biome and Their Bioactive Constituents
Published in Luzia Valentina Modolo, Mary Ann Foglio, Brazilian Medicinal Plants, 2019
Rebeca Previate Medina, Carolina Rabal Biasetto, Lidiane Gaspareto Felippe, Lilian Cherubin Correia, Marília Valli, Afif Felix Monteiro, Alberto José Cavalheiro, Ângela Regina Araújo, Ian Castro-Gamboa, Maysa Furlan, Vanderlan da Silva Bolzani, Dulce Helena Siqueira Silva
Many examples can be cited, with some related to plant species of Peperomia and Piper genera from the Piperaceae family. Peperomia obtusifolia is a well-known ornamental plant distributed from Mexico to South America. Despite the plant's predominant ornamental usage, some communities in Central America use the leaves', stems' and fruits' extracts to treat insect and snake bites and as a skin cleanser (Batista et al., 2017). Previous phytochemical investigation on P. obtusifolia aerial parts showed the presence of prenylated chromans, lignans, amides, flavonoids and other phenolic derivatives (Batista et al., 2011; Mota et al., 2009; Tanaka et al., 1998). Crude extracts and fractions of P. obtusifolia leaves and stems showed potent trypanocidal activity and their chemical investigation afforded seven compounds (94–100), including chromanes, furofuran lignans and flavone C-diglycosides (Figure 9.19) (Mota et al., 2009). This study revealed that the most active compounds were the chromanes, peperobtusin A (94) and the carboxy derivative 3,4-dihydro-5-hydroxy-2,7-dimethyl-8-(2′′-methyl-2′′-butenyl)-2-(4′-methyl1′,3′-pentadienyl)-2H-1-benzopyran-6-carboxylic acid (95), with IC50 values of 3.1 µM (almost three times more active than the positive control benznidazole, IC50 10.4 µM) and 27.0 µM, respectively. The potent trypanocidal activity observed for these compounds seems to be related to a benzopyran nucleus substituted with isoprenyl moieties. The assay was performed measuring the proliferation of Y strain epimastigotes growing in axenic culture and the number of remaining viable protozoa was established by counting the parasites in a Neubauer chamber. Cytotoxicity assays using peritoneal murine macrophages indicated that the chromanes were not toxic at the level of the IC50 for trypanocidal activity (Mota et al., 2009), evidencing a selective index compatible with their use as prototypes for the development of therapeutic agents for Chagas disease.
Ubiquitin Proteasome System Activity is Suppressed by Curcumin following Exercise-Induced Muscle Damage in Human Skeletal Muscle
Published in Journal of the American College of Nutrition, 2021
Thomas D. Cardaci, Steven B. Machek, Dylan T. Wilburn, Paul S. Hwang, Darryn S. Willoughby
In a double-blind randomized manner, participants were assigned to orally ingest 2 g of cellulose placebo (Nutricology, Alameda, CA, USA) or 2 g of curcumin [(1E,6E)-1,7-bis (4-hydroxy- 3-methoxyphenyl)-1,6- heptadiene-3,5-dione)] standardized to 95% curcuminoids [certificate of analysis verified 99% purity and 95% curcuminoids (Bulk Supplements, Henderson, NV, USA)]. Additionally, previous pharmacokinetic data has demonstrated in healthy male participants piperine increases curcumin bioavailability by 2000% and significantly elevates curcumin serum concentrations with a Tmax of 0.69 h ± 0.07 (43). Therefore, both groups also supplemented with 20 mg of piperine [1-(5-[1,3-benzodioxol5-yl]-1-oxo-2,4-pentadienyl)] standardized to 95% 1-piperoylpiperidine (Natures Plus, Amityville, NY, USA). Participants ingested their respective supplement daily beginning 7 days prior to the muscle damaging exercise bout to ensure proper efficacy and saturation of the supplement continuing throughout the entire 11-day study. Compliance of the supplementation protocol was determined by a daily supplement compliance questionnaire and mean ± SD percent compliance for CUR and PLA was 99.10 ± 2.98% and 100 ± 0.00%, respectively.
Potential multifunctional agents with anti-hepatoma and anti-inflammation properties by inhibiting NF-кB activation
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Chang-Ming Su, Gui-Ge Hou, Chun-Hua Wang, Hong-Qin Zhang, Cheng Yang, Mei Liu, Yun Hou
Curcumin (Figure 1), a major active ingredient of turmeric, has been demonstrated showing anti-inflammatory and anti-cancer activities1. However, due to its poor solubility, unstability and low bioavailability, its clinical utility is limited2,3. Therefore, a lot of its analogues were developed. 3,5-bis(arylidene)-4-piperidone derivatives (BAPs) possess the 1,5-diaryl-3-oxo-1,4-pentadienyl pharmacophore leads a priorchemosensitivity to cancer cells rather than normal cells4,5. 3,5-Bis(2-flurobenzylidene)piperidin-4-one (EF24, Figure 1) inhibits cancer growth and metastasis through inhibiting NF-κB pathways6,7. CLEFMA induces cell apoptosis of lung cancer xenografts by inhibiting Bcl-2 expression and up-regulating Bax expression8. L49H37 (or MCAC 5B, Figure 1) exhibits better inhibitory effects on cell cycle of pancreatic stellate cells (PSCs), as well as anti-lung cancer activity, and chemosensitization based on ROS-mediated JNK pathway activation and NF-кB pathway inhibition9–11.
Hydroxyl-substituted double Schiff-base condensed 4-piperidone/cyclohexanones as potential anticancer agents with biological evaluation
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Lianshuang Zhang, Qin Chen, Guige Hou, Wei Zhao, Yun Hou
Curcumin (Figure 1), a major active component of the food flavor turmeric, has anti-inflammatory, antibacterial, anticancer and antioxidant activities1. Curcumin and its analogues containing the pharmacophore of 1,5-diaryl-3-oxo-1,4-pentadienyl, are thought to interact at the primary binding site, bio-thiols from susceptible neoplasms. Another pharmacophore of methoxyphenol groups at an auxiliary site also can influence their bio-activities. However, due to its low aqueous solubility, instability and low bioavailability, the clinical utility of curcumin is limited2,3. In recent years, researches have been focused on improving the bioavailability through the structure modification of curcumin4–6. Some 2,6-dibenzylidenecyclohexanone and 3,5-bis(arylidene)-4-piperidone derivatives (BAPs) were synthesized and evaluated bioactivity. These compounds generally possess the 1,5-diaryl-3-oxo-1,4-pentadienyl pharmacophore into their structures to form one or more α,β-unsaturated keto groups, which can react preferentially or exclusively with thiols in contrast to amino and hydroxy groups resulting in a greater chemosensitivity to tumors rather than with normal cells7,8. In addition, two of α,β-unsaturated keto groups enable sequential attacks of cellular thiols to display the better activities9. 3,5-Bis(2-flurobenzylidene)piperidin-4-one (EF24, Figure 1) is a novel curcumin analog, which can inhibit tumor growth and metastasis by inhibiting NF-κB pathways10,11. CLEFMA (Figure 1) can inhibit growth of lung cancer xenografts through inhibiting anti-apoptotic markers (cellular inhibitor of apoptosis protein-1 (cIAP1), Bcl-xL, Bcl-2, and survivin) expression, up-regulating the pro-apoptotic markers Bax and BID expression, and inducing apoptosis by cleavage of caspases 3/9 and PARP12. Curcumin analog (3E,5E)-3,5-bis(3,4,5-trimethoxybenzylidene)-1-methylpiperidin-4-one (L49H37, Figure 1) with fertile electron-donating substitutes exhibits more potent inhibitory effects than curcumin against pancreatic stellate cells (PSCs) cell cycle13. In addition, nitrogen-containing heterocyclic dienones, such as 4-piperidone, can display higher inhibitory properties toward human carcinoma cell lines compared with their homocyclic dienone analogs (such as cyclohexanone)14.