19 research outputs found
Pengembangan Senyawa-senyawa Heterosiklik Nitrogen sebagai Antituberkulosis dan Antikanker
No full textTuberkulosis merupakan penyakit menular yang disebabkan oleh bakteri Mycobacterium tuberculosis. Pirazinamida merupakan senyawa heterosiklik nitrogen yang termasuk salah satu obat tuberkulosis lini pertama. Kasus resistensi terhadap obat tuberkulosis dan belum ditemukannya obat baru menjadikan tuberkulosis sebagai ancaman global. Senyawa-senyawa analog pirazinamida menunjukkan potensi sebagai lead compounds dalam pengembangan senyawa-senyawa antituberkulosis baru. Sintesis analog pirazinamida pada umumnya melibatkan pereaksi tionil klorida yang termasuk dalam daftar bahan kimia untuk produksi senjata kimia dan melepaskan gas beracun sulfur dioksida sebagai hasil samping, sehingga perlu dikembangkan metoda sintesis baru. Penelitian yang dilakukan berhasil mengembangkan metoda sintesis baru tanpa melibatkan pereaksi tionil klorida, yang diterapkan pada sintesis dua puluh senyawa analog pirazinamida dengan struktur yang bervariatif. Uji bioaktivitas dua puluh senyawa tersebut terhadap M. tuberculosis H37Rv mendapatkan bahwa N-(2-etil-heksil)pirazina-2-karboksamida dan N-(4-florobenzil)pirazina-2-karboksamida mempunyai aktivitas antituberculosis dengan konsentrasi hambat minimum (MIC) <6,25 μg/mL; yang lebih baik dari pada pirazinamida dengan MIC 100 μg/mL.
Kanker merupakan penyakit yang menyebabkan kematian nomor dua di seluruh dunia setelah jantung. Kanker paru-paru dan kanker prostat merupakan jenis kanker yang sering diderita dengan masing-masing presentase kejadian sebesar 11,4% dan 7,3% dan presentase kematian sebesar 18% dan 3,8%. Kemoterapi merupakan metode pengobatan untuk menghambat dan mematikan sel kanker yang telah menjalar ke berbagai organ tubuh yang lain. Pengobatan tersebut tidak hanya berdampak pada sel-sel kanker, tetapi juga pada sel-sel normal. Senyawa-senyawa 3,3-di(indolil)indolin-2-on (trisindolina) merupakan senyawa heterosiklik nitrogen bahan alam yang diketahui mempunyai bioaktivitas sebagai antikanker. Selain menghambat proliferasi sel kanker, sebagian trisindolina dilaporkan tidak toksik terhadap sel normal paru-paru manusia. Senyawa-senyawa ini juga mempunyai bioaktivitas antikanker, antituberkulosis, antibakteri, spermisidal dan inhibitor enzim α-glukosidase. Penelitian yang dilakukan berhasil mendapatkan enam senyawa trisindolina dengan struktur yang bervariatif. Uji bioaktivitas enam senyawa tersebut terhadap sel kanker paru-paru A549 dan sel kanker prostat DU-145 mendapatkan bahwa tiga trisindolina dengan gugus ester memiliki aktivitas antiproliferasi lebih baik daripada trisindolina dengan gugus hidroksi. 5-Kloro-3,3-di((metil indol-5-karboksilat)-3-il)-2-indolon menunjukkan aktivitas terhadap terhadap sel kanker A549 dan sel kanker DU-145 masing-masing dengan IC50 11,02 dan 9,2 μg/mL yang lebih baik daripada cisplatin dengan IC50 491,25 dan 25,05 μg/mL.
====================================================================================================
Tuberculosis is an infectious disease caused by the Mycobacterium tuberculosis. Pyrazinamide is a nitrogen heterocyclic compound which is one of the first-line tuberculosis drugs. Cases of resistance to tuberculosis drugs and the discovery of new drugs have made tuberculosis a global threat. Pyrazinamide analogue compounds show potential as lead compounds in the development of new antituberculosis compounds. Synthesis of pyrazinamide analogues generally involves the reagent of thionyl chloride which is included in the list of chemicals for the productions of chemical weapons. Additionally, it can release toxic gas sulfur dioxide as a byproduct, so it is necessary to develop new synthesis methods. The research carried out succeeded in developing a new synthesis method without involving thionyl chloride reagent, which was applied to the synthesis of seventeen pyrazinamide analogues with varied structures. The bioactivity assay of these seventeen synthesized compounds against M. tuberculosis H37Rv found that N-(2-ethylhexyl)pyrazine-2-carboxamide and N-(4-florobenzyl)pyrazine-2-carboxymide have antituberculosis activity with minimum inhibitory concentration (MIC) of <6.25 µg/mL which is better than pyrazinamide with a MIC of 100 µg/mL.
Cancer is the second leading cause of death worldwide after heart disease. Lung cancer and prostate cancer are the most common types of cancer with incidence rates of 11.4% and 7.3%, respectively, and mortality rates of 18% and 3.8%. Chemotherapy is a method of treatment to inhibit and kill cancer cells that have spread to various other organs of the body. The treatment not only affects cancer cells, but also normal cells. 3,3-di(indolyl)indoline-2-ones, known as trisindolines, are nitrogen heterocyclic natural products which are known to have bioactivity as anticancer. In addition to inhibiting the proliferation of cancer cells, some trisindolines are reported to be non-toxic to normal human lung cells. These compounds also have anticancer, antitubercular, antibacterial, spermicidal, and α-glucosidase enzyme bioactivity. The research carried out succeeded in obtaining six trisindolines with varied structures. The bioactivity test of these six compounds against lung cancer cells A549 and prostate cancer cells DU-145 found that three trisindolines with ester groups have better antiproliferative activity than trisindolines with hydroxy groups. 5-Chloro-3,3-di((methyl indole-5-carboxylate)-3-yl)-2-indolone showed activity against cancer cells A549 and cancer cells DU-145 with IC50 of 11.02 and 9.2 µg/mL in repectively, which is better than cisplatin with IC50 491.25 dan 25.05 µg/mL
Sintesis N-(3-bromofenil)pirazina-2-karboksamida dan N-(4-bromofenil)pirazina-2-karboksamida dengan Metoda Yamaguchi
No full textPirazina-2-karboksamida merupakan salah satu obat anti tuberkulosis lini pertama. Beberapa senyawa analog pirazina-2-karboksamida memiliki kemampuan yang lebih baik dalam menghambat perkembangan Mycobacterium tuberculosis, salah satunya adalah N-fenilpirazina-2-karboksamida. MDR-TB (Multi-drag Resistant Tuberculosis) atau resistensi ganda terhadap obat anti tuberkulosis merupakan salah satu masalah yang mengakibatkan penderita kebal terhadap obat anti tuberkulosis lini pertama. Sintesis N-fenilpirazina-2-karboksamida umumnya dilakukan melalui dua tahap, yakni pembentukan asil klorida dan karboksamida. Pereaksi Yamaguchi umumnya digunakan untuk sintesis ester dan tioester. Penelitian yang dilakukan berhasil mensintesis dua turunan N-fenilpirazina-2-karboksamida yakni N-(3-bromofenil)pirazina-2-karboksamida dan N-(4-bromofenil)pirazina-2-karboksamida dengan metoda Yamaguchi yang memiliki satu tahap reaksi. Senyawa hasil reaksi diduga memiliki aktivitas antimikobakteria dengan rendemen masing-masing 64% dan 93%
STUDI IN SILICO SENYAWA HIBRID GABUNGAN PIRAZINAMIDA DENGAN ASAM 4-(2-AMINOTIAZOL-4-IL)BENZOAT
No full textSaat ini, kasus TB terus menjadi tantangan global dengan lebih dari 10 juta kasus baru setiap tahun, dan lebih dari 500.000 di antaranya resisten terhadap obat TB. Indonesia menyumbang sekitar 10% dari total kasus TB global dan menempati peringkat kedua sebagai negara dengan jumlah kasus TB tertinggi di dunia. Peningkatan kasus TB kambuh dipicu oleh resistensi terhadap obat TB sehingga memerlukan pengembangan obat baru yang efektif, singkat dalam pengobatan, dan tidak rentan terhadap Mycobacterium tuberculosis. Pirazinamida merupakan salah satu obat komersial untuk menangani tuberkulosis. Cincin pirazin memiliki peran penting dalam aktivitas bakterisidal. Senyawa yang mengalami N-substitusi dengan 4-feniltiazol-2-amin dan perpanjangan fenil dengan subtitusi gugus asam karboksilat telah terbukti memiliki aktivitas yang efektif. Dalam penelitian ini, dilakukan analisis in silico terhadap senyawa hibrid yang mengombinasikan pirazinamida dengan Asam 4-(2-aminotiazol-4-il)benzoat. Studi in silico melibatkan penelitian studi penambatan, sifat fisikokimia, dan sifat farmakokinetik. Hasil analisis menunjukkan bahwa senyawa hibrid (5) dan (6) memiliki potensi sebagai penghambat protein InhA dan dapat dianggap sebagai kandidat obat oral
STRATEGI KEPALA SEKOLAH DALAM MENINGKATKAN KINERJA GURU DI SD NEGERI SLEMAN 1
No full textThis research is motivated by the principal's strategy in improving teacher performance both through programmed and non-programmed supervision. The principal makes the plans and programs needed to improve the quality of teachers, including: procurement of workshops, increasing teacher motivation, participating in the KKG (teacher working group) program, participating in webinars, visits to places where they can learn such as PPGP (Teacher Driving Education Program) and others.
The method in this study is a qualitative descriptive research. The researcher used data collection techniques in the form of interviews, observations and documentation. The technique of selecting responses in interviews, observations, and documentation is determined by the 3M criteria, namely understanding, experiencing, and knowing related to the research topic. The subjects of this study include: Principal, Vice President for Student Affairs, Vice President for Curriculum, Teachers and TU. Data analysis uses trancscipt, coding, grouping, comparing and contrasting techniques. Furthermore, in the data validity technique, the researcher uses the source triangulation technique and the triangulation technique.
The results of the research at SD Negeri Sleman 1 can be concluded that: First, the principal's strategy in improving teacher performance has 5 stages, namely (1) teacher performance development by including teachers in training activities held by the government and various agencies, (2) supervision of teacher performance in mastery and classroom management by supervising teachers in teaching and learning in the classroom, (3) coaching discipline of education personnel by monitoring the attendance of teachers every day, (4) providing motivation, (5) giving awards for dedication and achievements. Second, supporting factors are a good work environment, completeness of school facilities, level of education or teacher experience, teaching supervision and education and training. Meanwhile, the inhibiting factors are the lack of awareness and motivation of teachers about the importance of good teacher performance for educational success, difficulties in adjusting the curriculum and syllabus in learning and lack of understanding of the abilities of each student.
Keywords: Strategy, Principal, Teacher, Teacher Performanc
A STUDI IN SILICO: POTENSI SENYAWA KATEKIN DAN TURUNANNYA DARI TEH HIJAU SEBAGAI INHIBITOR HGF SERTA PROFIL TOKSISITASNYA
No full textGreen tea is a plant with a high content of catechins. Catechins are a secondary metabolites that possess many benefits and potencies, one of which is as an antitumor. This study aims to describe the potential of catechin and its derivatives as antitumor inhibitor of HGF and their toxicity profiles through in silico analysis. The ligands used in this study were catechin, gallocatechin, epicatechin, and epigallocatechin. The results showed that epicatechin has better potency (-6.6 kcal/mol) than other catechin derivatives. The toxicity characteristics of the four catechins indicate that they do not exhibit hepatotoxicity, mutagenicity, or carcinogenicity, and possess a safe LD50 value. Further studies, such as in vitro and in vivo, must reveal its potential as an antitumor HGF inhibitor.Teh hijau merupakan salah satu tumbuhan dengan kandungan katekin yang tinggi. Katekin merupakan salah satu metabolit sekunder yang memiliki banyak manfaat dan potensi. Salah satunya sebagai antitumor. Penelitian ini bertujuan untuk mendeskripsikan potensi katekin dan turunan sebagai antitumor inhibitor HGF serta profil toksisitasnya melalui analisis in silico. Ligan yang digunakan dalam penelitian ini adalah katekin, galokatekin, epikatekin, dan epigalokatekin. Hasil penelitian menunjukkan bahwa epikatekin memiliki potensi lebih baik (-6,6 kkal/mol) dibandingkan turunan katekin lainnya. Profil toksisitas keempat katekin tersebut menunjukkan bahwa keempatnya tidak hepatotoksik, tidak mutagentik, tidak karsinogenik, dan memiliki nilai LD50 yang aman. Penelitian lebih lanjut seperti in vitro dan in vivo diperlukan untuk menguak potensinya sebagai antitumor inhibitor HGF
POTENSI SENYAWA EUGENOL DARI CENGKEH (Syzygium aromaticum) SEBAGAI INHIBITOR PROTEASE HIV-1 (PR)
No full textSyzygium aromaticum is a medicinal plant that is well known for its uses in the medical world. This plant contains essential oil that has a lot of bioactivitis, namely eugenol. This study aims to determine the potency of the compound eugenol and its derivatives as an inhibitor of HIV-1 protease (PR), an HIV-1 antiviral candidate. The ligands used in this study were eugenol, methyl eugenol, acetyl eugenol, and isoeugenol. The results showed that the compound acetyl eugenol has the potential to act as an HIV-1 protease inhibitor better than other eugenol derivatives because it has a lower binding affinity value (-6.2 kcal/mol) of the other compounds. Further studies such as in vitro and in vivo tests are needed to prove its activity as an HIV-1 protease.Syzygium aromaticum merupakan tanaman obat yang terkenal akan kegunaannya di dunia medis. Tanaman ini mengandung minyak esensial yang memiliki banyak bioaktivitas yakni eugenol. Penelitian ini bertujuan untuk mengetahui potensi senyawa eugenol dan turunannya sebagai inhibitor HIV-1 Protease (PR) kandidat antivirus HIV-1. Ligan yang digunakan dalam penelitian ini adalah eugenol, metil eugenol, asetil eugenol, dan isoeugenol. Hasil penelitian menunjukkan bahwa senyawa asetil eugenol memiliki potensi sebagai inhibitor HIV-1 Protease lebih baik dibandingkan turunan eugenol yang lainnya karena memiliki nilai binding affinity (-6,2 kkal/mol) lebih rendah senyawa lain. Penelitian lebih lanjut seperti uji in vitro dan in vivo diperlukan untuk membuktikan aktivitasnya sebagai HIV-1 Protease
The Effect of Prenatal Yoga on Emesis Gravidarum in the First Trimester Pregnant Women
No full textBackground: Increased levels of progesterone, estrogen, and HCG (chorionic gonadotropin hormone) during the first trimester of pregnancy can produce morning sickness, also known as emesis gravidarum (nausea and vomiting). To lessen the release of hormones that induce anxiety, severe nausea, and vomiting, prenatal yoga practitioners can block the stimulation of sympathetic nerves by practicing muscle relaxation. This study aims to ascertain how prenatal yoga affects first-trimester emesis gravidarum. Method: This study used a pre-experimental design with a pretest-posttest design in one group, involving 16 mothers who had emesis gravidarum at PMB Fatimah Bandung Rejosari, Sukun, Malang. Data collection was done using the questionnaire. Results: The result was that two prenatal yoga sessions over two weeks demonstrated significant benefits. Prenatal yoga affects emesis gravidarum in the first trimester of pregnancy, as indicated by the independent t-test technique (2-tailed) of 0.000 <0.005. Discussion: Steroid hormones can slow down stomach emptying, which causes emesis gravidarum. Excessive or low cortisol levels can be brought back to normal with yoga. Yoga offers numerous mental and physical health advantages. Conclusion We can conclude that the course of treatment impacts the severity of emesis gravidarum, or nausea and vomiting, during the first trimester of pregnancy
Probing maximal zero textures with broken cyclic symmetry in inverse seesaw
No full textAbstractWithin the framework of inverse seesaw mechanism we investigate neutrino mass matrices invariant under cyclic symmetry (Z3) with maximal zero texture (6 zero textures). We explore two different approaches to obtain the cyclic symmetry invariant form of the constituent matrices. In the first one we consider explicit cyclic symmetry in the neutrino sector of the Lagrangian which dictates the emerged effective neutrino mass matrix (mν) to be symmetry invariant and hence leads to a degeneracy in masses. We then consider explicit breaking of the symmetry through a dimensionless parameter ϵ′ to remove the degeneracy. It is seen that the method doesn't support the current neutrino oscillation global fit data even after considering the correction from cyclic symmetry invariant charged lepton mass matrix (ml) unless the breaking parameter is too large. In the second method, we assume the same forms of the neutrino mass matrices, however, symmetry is broken in the charged lepton sector. All the structures of the mass matrices are now dictated by an effective residual symmetry of some larger symmetry group in the Lagrangian. For illustration, we exemplify a toy model based on softly broken A4 symmetry group which leads to one of the combinations of ml, mD, MRS and μ to generate effective mν. All the emerged mass matrices predict a constraint range of the CP violating phases and atmospheric mixing angle along with an inverted hierarchical structure of the neutrino masses. Further, significant predictions on ββ0ν decay parameter |m11| and the sum of the three light neutrino masses (Σimi) are also obtained
Effect of Trisindolina-5 Compound on Cancer Stem Cell (CSC) Proliferation in-Vitro
No full textCancer stem cells (CSCs) are a subset of cancer cells that have the abilities of normal stem cells. CSCs are cancer cell pioneers with self-renewal abilities that can cause CSCs to differentiate into several cancer cells. Because CSCs are resistant to conventional therapies, killing CSCs necessitates the use of a compound with powerful anticancer properties. Trisindoline has been shown to have powerful anticancer properties. Trisindoline has been synthesized into several modifications, the most recent of which is Trisindoline-5. The goal of this study is to find out what the IC50 value of Trisindoline-5 is. The cytotoxicity assay using Microculture Tetrazolium Technique Assay (MTT Assay) is used to determine IC50. The IC50 value of the Trisindoline-5 compound is 24.683 μM at 24 hours incubation, which classifies it as a medium cytotoxic compound, 17.067 μM at 48 hours incubation, which classifies it as a highly toxic compound, and 6497 μM at 72 hours incubation, which classifies it as a compound with no toxicity. While the IC50 value of doxorubicin is 1.611 μM after 24 hours, 2.334 μM after 48 hours, and 5.324 μM after 72 hours, it is classified as a compound with highly toxic activity
Turkic loanwords in the Slavonic-Russian Pentateuchs edited according to the Masoretic Text
No full textThis article presents eighteen glosses and emendations borrowed from Turkic dialects into the Slavonic-Russian Pentateuch edited according to the Hebrew Masoretic Text (in manuscripts from the 15th–16th centuries). The first group of these words — including proper names — has Arabic or Persian origins; they came into East Slavonic with obvious Turkic mediation (Skandryja ‘Alexandria’, Bagadad ‘Baghdad’, Misurʹ ‘Egypt’, Šam ‘Damascus’, Isup ‘Joseph’, sturlabʹ ‘astrolabe’, soltan ‘sultan’, olmas ‘diamond’, ambar ‘ambergris’, and brynec ‘rice’). The second group is proper Turkic: saigak ‘saiga antelope’, ošak ‘donkey’, katyrʹ ‘mule’, kirpič ‘brick’, talmač ‘interpreter’, čalma ‘turban’, and saranča ‘locust’. The author agrees with the hypothesis that this glossing/emendation was made for the East Slavonic Judaizers. Furthermore, the author suggests that there was participation of a group of merchants interested in a new and mysterious knowledge promulgated by learned rabbis
