In cell development, the cell cycle is crucial, and the cycle progression’s main controllers are endogenous CDK inhibitors, cyclin-dependent kinases (CDKs), and cyclins. In response to the mitogenic signal, cyclin D is produced and retinoblastoma protein (Rb) is phosphorylated due to activated CDK4/CDK6. This causes various proteins required in the cell cycle progression to be generated. In addition, complexes of CDK1-cyclin A/B, CDK2-cyclin E/A, and CDK4/CDK6-cyclin D are required in each phase of this progression. Cell cycle dysregulation has the ability to lead to cancer. Based on its role in the cell cycle, CDK has become a natural target of anticancer therapy. Therefore, understanding the CDK structures and the complex formed with the drug, helps to foster the development of CDK inhibitors. This development starts from non-selective CDK inhibitors to selective CDK4/CDK6 inhibitors, and these have been applied in clinical cancer treatment. However, these inhibitors currently require further development for various hematologic malignancies and solid tumors, based on the results demonstrated. In drug development, the main strategy is primarily to prevent and asphyxiate drug resistance, thus a determination of specific biomarkers is required to increase the therapy’s effectiveness as well as patient selection suitability in order to avoid therapy failure. This review is expected to serve as a reference for early and advanced-stage researchers in designing new molecules or repurposing existing molecules as CDK4/CDK6 inhibitors to treat breast cancer.
Objective: The aim of this study was to observe the antidyslipidemic and antioxidant activity of andrographolide (AND) compound from Sambiloto (Andrographis paniculata) herb. The antidyslipidemic activity could be described by lowering TC (total cholesterol), TG (triglyceride), and LDL (low-density lipoprotein) level in the blood and by increasing HDL (high-density lipoprotein) level in the blood. The antioxidant activity could be described by inhibiting the ox-LDL (oxidized low-density lipoprotein) formation.Methods: AND was separated from the sambiloto ethanolic extract. Atherosclerosis in rats was induced by rich fat food (5% yolk, 10% lard), 1% calcium and 20.000 IU vitamin D3 for 90 d. The rats were treated with AND compound on the 61st day for 30 d. On the 90th day, the blood of rats had been collected, and its blood vessel was also extracted. Antidyslipidemic activity was measured by estimating the level of TC, TG, LDL and HDL in the blood. Antioxidant activity was measured by calculating the ox-LDL concentration in blood and histopathology parameter.Results: 18 mg/kg BW AND could reduce the level TC, TG, and LDL in blood, and could increase HDL blood level significantly (p<0.05). This compound can also significantly inhibit LDL oxidation (p<0.05), and the histopathology result showed that this compound could protect the vessel from adhesive lipid plaques.Conclusion: AND compound from sambiloto herb showed the antidyslipidemic and antioxidant effect in atherogenic rats.
Propionibacterium acnes merupakan bakteri utama penyebab jerawat, dimana dilaporkan dalam suatu penelitian bahwa persentase ditemukannya bakteri P. acnes pada lesi jerawat sebesar 78,8%. Daun sirih hijau telah banyak dilaporkan memiliki aktivitas sebagai antibakteri. Kemampuan antibakteri daun sirih hijau disebabkan karena adanya senyawa golongan fenol yang terdiri dari kavikol, hydroxychavicol, chavibetol, estragol, eugenol, carvacrol dan golongan senyawa seskuiterpen. Penelitian ini bertujuan untuk mengetahui metode optimum yang menghasilkan aktivitas antibakteri terhadap bakteri P. acnes dari enam fraksi yang diperoleh. Metode purifikasi yang digunakan untuk mendapatkan ke-6 fraksi tersebut adalah LLE dengan penggunaan pelarut polar etanol-air yang tidak bercampur dengan pelarut heksan, kloroform dan dietileter. Ke-6 fraksi uji tersebut selanjutnya diuji aktivitas antibakterinya dengan metode difusi disk dan dilanjutkan dengan metode tambahan yaitu KLT bioautografi kontak. Analisis data yang dilakukan secara deskriptif terhadap nilai diameter zona hambat dengan mengkategorikannya berdasarkan CLSI dan terhadap hasil skrining fitokimia. Dari hasil penelitian ini diperoleh hanya dua fraksi yaitu fraksi n-heksan dan fraksi dietileter yang mampu menghambat pertumbuhan bakteri P. acnes dengan nilai diameter zona hambat sebesar 8 mm dan 9 mm. Metode purifikasi ekstrak daun sirih hijau yang merupakan gabungan metode maserasi dan LLE yang dilakukan belum optimal karena dilihat dari 6 fraksi yaitu fraksi etanol-air (FEA I), etanol-air (FEA II), etanol-air (FEA III), kloroform, dietil eter dan fraksi n- belum mampu menghambat pertumbuhan bakteri P. acnes dimana ke-6 fraksi tersebut termasuk dalam kategori resistant.
ABSTRAKReactive Oxygen Species (ROS) merupakan suatu produk alami yang terbentuk dari metabolisme aerobik normal dalam tubuh yang secara potensial dapat menyebabkan kerusakan. Penelitian bertujuan untuk mengetahui potensi antioksidan yang paling kuat dari ekstrak buah mengkudu (Morinda citrifolia L), ekstrak daun kelor (Moringa oleifera) dan ekstrak daun kedondong hutan (Spondias pinnata (l.f) kurz). Pengujian aktivitas antioksidan dari ketiga tanaman ini yaitu dilakukan dengan metode DPPH yang kemudian diamati dengan Spektro UV-Vis pada panjang gelombang maksimum 315 nm. Analisis data dilakukan dengan menghitung persen inhibisi (% inhibisi) yang kemudian dibuat persamaan regresi linear. Hasil yang diperoleh bahwa nilai IC 50 ekstrak buah mengkudu yaitu 22,95 µg/mL, nilai IC 50 dari ekstrak daun kelor yaitu 42,19 µg/mL sedangkan nilai IC 50 dari ekstrak daun kedondong hutan yaitu 49,97 µg/mL
Atherosclerosis is a chronic inflammatory disease that begins with endothelial dysfunction, it caused fat accumulation and plaque growth in the inner arteries walls. Endothelial dysfunction will activate the Mitogen Activated Protein Kinase (MAPK) pathway involving ERK1, ERK2, JNK1, JNK2, and p38MAPK proteins, as well as the Nuclear Factor Kappa B (NF-kB) pathway involving IKK proteins. Terpinen-4-ol is constituent found in the bangle rhizome. The purpose of this study were to determine the affinity and mechanisms of terpinen-4-ol against ERK1, ERK2, JNK1, JNK2, and p38MAPK proteins as anti-inflammatory in atherosclerosis performed using molecular docking method. The study was conducted exploratively with several steps such as preparation and optimization of terpinen-4-ol structure, preparation of 3D ERK1, ERK2, JNK1, JNK2, and p38MAPK proteins, validation method of molecular docking, and docking terpinen-4-ol in these proteins. The docking result are assessed from the binding energy and hydrogen bonds formed between terpinen-4-ol and proteins. The smaller value of binding energy terpinen-4-ol with target proteins showed the complex that form more stable. The result showed that terpinen-4-ol and has activity in inhibiting the inflammatory process because it is able to disturb ERK1, ERK2, JNK1, JNK2, and p38MAPK proteins with respective bond energy values -5,12; -5,24; -5,08; -5,88; and -4,99 Kcal/mol. The molecular mechanism in inhibiting the activity of ERK1, ERK2, JNK1, JNK2, and p38MAPK proteins is through the formation of hydrogen bonds in these proteins. These results show that terpinen-4-ol have the potential to inhibit inflammatory process and the formation of atherosclerotic plaque can be obstructed. Keywords : atherosclerosis, terpinen-4-ol, molecular docking, in silico
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