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Abstrak :
This book presents an comprehensive reviews on the antimicrobial and antiviral properties of numerous recently reported phytochemicals, and their mechanisms of antimicrobial actions. Some of the chapters have critically discussed the beneficial and adverse effects of antibacterial, and stimulatory activities of dietary phytochemicals on rumen microbial populations, and gut microbial populations of humans and animals. Microbial adaptation and resistance of microbes to phytochemicals has also been highlighted. On the applied apects, the use of phytochemicals against drug resistance microbes, to treat microbial diseases, for food preservation, to inhibit methanogenic archaea in the rumen, and to modulate lipid biohydrogenating microbial populations to increase conjugated linoleic acids in animal-derived foods have been presented in different chapters.

Abstrak :
Propolis merupakan substansi resin alami yang terbentuk dari kuncup bunga, pohon, dan eksudat resin yang dikumpulkan lebah. Propolis memiliki beberapa sifat terapeutik seperti antibakteri, anti-inflamasi, penyembuhan, anestesi, antioksidan, antifungal, antiprotozoan, dan antiviral. Pada penelitian sebelumnya, ditemukan senyawa asam calophylloidic A, yang diketahui memiliki aktivitas antimikroba. Penelitian ini dilakukan untuk melakukan eksplorasi aktivitas antijamur propolis Lombok terhadap empat spesies jamur yaitu Candida albicans, Candida glabrata, Candida Krusei, dan Cryptococcus neoformans. Metode pengujian antijamur yang dilakukan adalah agar difusi dan mikrodilusi. Selain itu, pada penelitian ini juga dilakukan analisis fitokimia yaitu LC-MS/MS, total kandungan polifenol dan flavonoid. Berdasarkan penelitian yang dilakukan, teridentifikasi 21 senyawa dan 4 diantaranya ditemukan pada ketiga sampel propolis yaitu asam galat, ellagic acid, 18-β-Glycyrrhetinic acid dan maslinic acid. Total kandungan polifenol propolis Rempek, Sekotong, dan Bayan secara berurutan adalah 248,05±39,42; 222,96±31,24; dan 278,15±120,64 mg GAE/g. Sedangkan untuk total kandungan polifenol adalah 1023,71±140,15; 1104,22±73,90; dan 512,01±42,79 mg QE/g. Berdasarkan hasil uji antijamur yang dilakukan, sampel propolis menunjukkan aktivitas antijamur pada spesies C. albicans, C. glabrata, C. krusei, dan Cryptococcus neoformans. Zona hambatan terbaik pada C. albicans, C.glabrata, dan C. krusei secara berurutan adalah 10,4±1,97; 10,0±1,0; dan 9,67±0,58 mm. Sedangkan pada uji antijamur mikrodilusi, ekstrak propolis berpengaruh terhadap pertumbuhan jamur C. albicans, C.glabrata dan Cryptococcus neoformans. ......Propolis is a natural resinous substance formed from flower buds, trees, and resinous exudates collected by bees. Propolis has several therapeutic properties such as antibacterial, anti-inflammatory, healing, anesthetic, antioxidant, antifungal, antiprotozoan, and antiviral. Based on previous study, a new compound was found in Propolis Lombok, which is calophylloidic acid A with antimicrobial activity. The aim of this study is to explore antifungal activity of Lombok Propolis against Candida albicans, Candida glabrata, Candida krusei, and Cryptococcus neoformans. Two methods use on antifungal test, which are agar diffusion and microdilution. In addition, phytochemical analysis also carried out with LC-MS/MS, total polifenol content, and total flavonoid content. 21 compounds found in this study with 4 of them were found in three samples Lombok propolis, namely gallic acid, ellagic acid, 18-β Glycyrrhetinic acid and maslinic acid. The total polyphenol content of Rempek, Sekotong, and Bayan propolis respectively was 248,05±39,42; 222,96±31,24; and 278,15±120,64 mgGAE/g. Meanwhile, the total polyphenol content was 1023,71±140,15; 1104,22±73,90; and 512,01±42,79 mg QE/g. Based on the antifungal tests, propolis samples showed an antifungal activity in C. albicans, C. glabrata, C. krusei, and Cryptococcus neoformans species. Inhibition fungal growth zone for C. albicans, C. glabrata, and C. krusei respectively are 10,4±1,97; 10,0±1,0; and 9,67±0,58 mm. While for microdilution antifungal method, propolis extract only affects C. albicans, C. glabrata and Cryptococcus neoformans growth.

Abstrak :
Latar belakang: Kanker kolon merupakan salah satu kanker yang mengalami peningkatan insidensi saat ini, hal tersebut terjadi karena konsumsi lemak tinggi yang menyebabkan absorbsi senyawa karsinogenik dalam tubuh dan memperlambat waktu pengangkutan ke usus. Doksorubisin sebagai obat kanker kolon memiliki kelemahan yaitu dapat menginduksi apoptosis dan nekrosis sel yang sehat serta menimbulkan toksisitas pada hati, otak, ginjal dan jantung sehingga diperlukan alternatif pengobatan kanker kolon. Spirulina platensis dapat dikembangkan sebagai antikanker karena ketersediaannya di perairan Indonesia dan terbukti memiliki banyak manfaat. Tujuan: mengetahui kandungan fitokimia dan efek sitotoksik ekstrak Spirulina platensis terhadap sel kanker kolon WiDr.  Metode: Maserasi dan ekstraksi Spirulina platensis dengan menggunakan pelarut etanol, etil asetat dan n-heksana. Komponen fitokimia ekstrak Spirulina platensis dianalisis melalui uji fitokimia, dan uji kromatografi lapis tipis (KLT). Analisis aktivitas sitotoksik ekstrak etil asetat, ekstrak n-heksana dan ekstrak etanol terhadap sel WiDr dilakukan dengan metode uji MTT assay.  Hasil: Komponen senyawa fitokimia ekstrak etil asetat dan ekstrak etanol Spirulina platensis masing-masing mengandung metabolit sekunder flavonoid, triterpenoid, steroid, alkaloid dan glikosida. Ekstrak n-heksana Spirulina platensis mengandung metabolit sekunder triterpenoid, steroid dan alkaloid. Pada uji KLT, didapatkan tujuh komponen fitokimia pada ekstrak n-heksana serta terdapat enam komponen pada ekstrak etanol dan etil asetat Spirulina platensis. Ekstrak etanol, n-heksana dan etil asetat Spirulina platensis pada penelitian ini memiliki aktivitas inhibisi terhadap sel kanker kolon WiDr. Nilai IC50 yang didapatkan pada ekstrak etanol, ekstrak etil asetat dan ekstrak n-heksana Spirulina platensis terhadap sel WiDr secara berurut adalah 6,764 ± 1,691¼g/mL; 42,509 ± 1,603¼g/mL dan 71,257 ± 3,4¼g/mL, sedangkan kontrol positif doksorubisin memiliki nilai IC50 sebesar 0,226 ± 0,185¼g/mL. Kesimpulan: Ekstrak Spirulina platensis terbukti memiliki potensi untuk dapat dikembangkan sebagai terapi alternatif dalam tata laksana kanker kolon.  ......Background: Colon cancer is one of the cancers that has an increasing incidence at this time, this happens because of high-fat consumption which causes absorption of carcinogenic compounds in the body and slows transport time to the intestine. Doxorubicin as a colon cancer drug has a weakness that is it can induce apoptosis and necrosis of healthy cells and cause toxicity to the liver, brain, kidney and heart, so an alternative treatment for colon cancer is needed. Spirulina platensis can be developed as an anticancer because of its availability in Indonesia’s ocean and has been proven to have many benefits. Objective: to determine the phytochemical content and cytotoxic effects of Spirulina platensis extract on WiDr colon cancer cells.  Methods: Maceration and extraction of Spirulina platensis using ethanol, ethyl acetate and n-hexane as solvents. The phytochemical components of the Spirulina platensis extract were analysed by means of phytochemical tests, and thin layer chromatography (TLC) tests. Analysis of the cytotoxic activity of ethyl acetate extract, n-hexane extract and ethanol extract on WiDr cells was carried out using the MTT assay method. Results: The phytochemical components of the ethyl acetate extract and the ethanol extract of Spirulina platensis each contain secondary metabolites in the form of flavonoids, triterpenoids, steroids, alkaloids and glycosides. N-hexane extract of Spirulina platensis contains secondary metabolites in the form of triterpenoids, steroids and alkaloids. In the TLC test, seven phytochemical components were found in the n-hexane extract and six components in the ethanol and ethyl acetate extracts of Spirulina platensis. The ethanol, n-hexane and ethyl acetate extracts of Spirulina platensis in this study had inhibitory activity against WiDr colon cancer cells. IC50 values ​​obtained in ethanol extract, ethyl acetate extract and n-hexane extract Spirulina platensis against WiDr cells were 6.764 ± 1.691 g/mL; 42.509 ± 1.603 g/mL and 71.257 ± 3.4 g/mL respectively, whereas the positive control of doxorubicin has IC50 value of 0.226 ± 0.185 g/mL. Conclusion: Spirulina platensis extract has proven potential to be developed as an alternative therapy in the treatment of colon cancer.

Abstrak :
Latar belakang: Terapi target dengan EGFR TKI merupakan terapi utama untuk kanker paru, khususnya KPKBSK. Selain permasalahan efektivitas harga, permasalahan lain terkait penggunaan EGFR TKI adalah resistansi primer dan sekunder seperti T790M, C797S dan insersi ekson 20. Penelitian in silico QSAR berbasis machine learning dan molecular docking dapat mempercepat penemuan senyawa EGFR TKI baru berbasis senyawa fitokimia. Metode: Penelitian ini adalah penelitian in silico untuk mengembangkan model QSAR berbasis machine learning yang dilanjutkan dengan molecular docking untuk penapisan senyawa fitokimia yang memiliki efek EGFR TKI terhadap mutasi T790M, C797S dan insersi ekson 20. Model machine learning dibuat untuk memprediksi nilai IC50 berdasarkan struktur kimia senyawa. Data pembelajaran berasal dari pangkalan data ChEMBL, data senyawa fitokimia dari KEGG, dan data makromolekul dari RCSB PDB. Simulasi molecular dynamics dilakukan untuk memvalidasi lebih lanjut hasil molecular docking. Hasil: Didapatkan 8627 senyawa EGFR TKI dari ChEMBL, yang dibagi menjadi set pembelajaran dan set uji dengan rasio 9:1. Model machine learning dengan algoritma LGBM berhasil dikembangkan dengan nilai R2 sebesar 73%. Lima senyawa fitokimia dengan nilai IC50 prediksi terbaik adalah orobol, norswertianin, isokaempferide, isoathyriol, dan norathyriol. Kelima senyawa memiliki profil farmakokinetik dan toksikologi yang cukupbaik. Hasil molecular docking menunjukkan norswertianin memiliki kemampuan ikatan terbaik terhadap EGFR mutasi T790M dan T790M/C797S/L858R, sedangkan orobol terhadap mutasi T790M/C797S dan insersi ekson 20. Kedua senyawa dapat membentuk ikatan yang stabil pada simulasi molecular dynamics. Kesimpulan: Model QSAR berbasis machine learning dengan algoritma LGBM dapat digunakan untuk memprediksi nilai IC50 EGFR TKI senyawa berdasarkan struktur kimianya. Senyawa fitokimia dapat digunakan sebagai dasar pengembangan EGFR TKI baru. Senyawa norswertianin dan orobol memiliki potensi terbesar sebagai EGFR TKI yang efektif untuk mutasi T790M, C797S dan insersi ekson 20. ......Background: Targeted therapy with EGFR TKI has been the mainstay of lung cancer treatment, especially NSCLC. Besides the poor cost-effectiveness, primary and secondary resistances, such as T790M, C797S, and exon 20 insertion mutation, have been problematic in EGFR TKI clinical utilization. In silico research, such as machine learning-based QSAR dan molecular docking, has the potential to hasten the discovery of novel EGFR TKI based on phytochemicals. Method: This study is an in silico research to develop a machine learning-based QSAR model, followed by molecular docking experiments for virtual screening of phytochemicals that have bioactivity as EGFR TKI against T790M, C797S, and exon 20 insertion mutation. A machine learning model will be developed to predict IC50 based on chemical structure. The learning set is sourced from the ChEMBL database, phytochemical data from KEGG, and macromolecule data from RCSB PDB. Molecular dynamic simulation is carried out to validate the molecular docking result further. Results: A total of 8627 compounds was procured from ChEMBL database, which was split into training and test sets with a ratio of 9:1. LGBM based machine learning model with considerable accuracy can be developed, with R2 of 73%. The five compounds with the best predicted IC50 value was orobol norswertianin, isokaempferide, isoathyriol, and norathyriol. All compounds possess a good pharmacokinetics and toxicology profile. The molecular docking result showed that norswertianin has the best binding affinity against EGFR with T790M and T790M/C797S/L8568R. Orobol has the best binding affinity against EGFR with T790M/C797S and exon 20 insertion. Both compounds can form a stable binding in molecular dynamics simulation. Conclusions: Machine learning-based QSAR model utilizing the LGBM algorithm can predict IC50 value as EGFR TKI based on the compound’s chemical structure. Phytochemicals can be used as the basis for novel EGFR TKI. Norswertianin and orobol have the best EGFR TKI potential against T790M, C797S, and exon 20 insertion mutations.

Abstrak :
The content of this book gives a multi-disciplinary approach into the anti-cancer research field related to natural products and dietary compounds. Mainly, it covers the area of antitumor activity through an in-depth description of the cytotoxic, anti-inflammatory and anti-oxidant properties in cancer, inflammatory and cardio-vascular diseases. The cell death inducing mechanisms (apoptosis, anti-proliferative activity, angiogenesis, cell cycle control, cytostatic property and autophagy) give an overview of how natural products are able to target cancer cells.

Abstrak :
ABSTRAK
The search for novel biological activities from plant-based natural products is gaining traction due to the high abundance and accessibility of the plants, with consequent lower cost for discovery, and lesser side effects and toxicity on human health and the environment. This study focused on the phytochemical analyses and the potency of mangrove-associated Hibiscus tiliaceus extracts and fractions as anti-bacteria and anti- biofilm agents against Pseudomonas aeruginosa. The bacterial strain contributes towards biofilm formation of various infectious diseases such as cystic fibrosis in lung, and causes blockage in urinary catheter. It is also an initiator of biofouling in shipping and maritime facilities. the methanol extracts of each part of fruits, leaves, and twigs were fractionated into chloroform, ethyl acetate, and methanol fractions using column chromatography. crystal violet assay was carried out for anti-biofilm activity in a 96 well-plate to evaluate the bacterial inhibition and biofilm formation. Phytocemical analyses suggested the presence of protein, carbohydrate, phenols, tannin, flavonoids, saponins, glycoside, steroids, terpenoids, and alkaloids in Hibiscus tiliaceus. The strongest anti-bacterial and anti-biofilm activities were exhibited by the chloroform fraction of fruits (HFC). the methanol crude of fruits (HFMc), methanol fraction of fruits (HFM), and chloroform fraction of twig (HTC) showed more than 80% inhibition as compared to the control.the results suggested that Hibiscus tiliaceus had a good potential to be developed as anti-bacterial and anti-biofilm agents.

Abstrak :
Diabetes melitus merupakan gangguan metabolisme karbohidrat, lipid, dan protein yang ditandai dengan kondisi hiperglikemia, serta dapat meningkatkan risiko komplikasi dari penyakit pembuluh darah. Salah satu pendekatan terapi untuk mengurangi hiperglikemia postprandial pasien diabetes yaitu dengan memperlambat penyerapan glukosa melalui penghambatan enzim yang menghidrolisis karbohidrat dalam saluran pencernaan, seperti a-glukosidase dan a-amilase. Penelitian ini bertujuan untuk mengetahui aktivitas penghambatan enzim α-glukosidase dan enzim α-amilase dari ekstrak daun Garcinia mangostana, serta mengidentifikasi golongan senyawa kimia yang terkandung dalam ekstrak teraktif daun Garcinia mangostana. Pengujian dilakukan pada ekstrak metanol, etil asetat, dan n-heksana. Pada uji penghambatan aktivitas α-amilase, digunakan Spektrofotometer UV-Vis dengan λ=490 nm. Hasil menunjukkan bahwa ekstrak metanol memiliki persen penghambatan tertinggi (93,76 %) dengan nilai IC50 sebesar 2,33 µg/mL. Sementara itu, pada penghambatan α-glukosidase digunakan Microplate Reader dengan λ=405 nm. Hasil menunjukkan ekstrak metanol juga memiliki IC50 terkecil, yaitu 48,97 µg/mL yang dibandingkan dengan nilai IC50 Akarbose sebesar 91,17 µg/mL sebagai kontrol positif. Pada penapisan senyawa kimia, ekstrak metanol daun Garcinia mangostana mengandung alkaloid, flavonoid, glikosida, saponin, dan tannin. ...... Diabetes mellitus consists of disorders altered metabolism of carbohydrates, lipids, and proteins; characterized by hyperglycemia and an increased risk of complications from vascular disease. One therapeutic approach to reduce postprandial hyperglycemia in diabetic patients is to slow the absorption of glucose by inhibiting enzymes that hydrolyze the carbohydrates in the digestive tract, such as a-glucosidase and a-amylase. This research aims to determine the inhibitory activity of the α-glucosidase and α-amylase enzyme from leaf extracts of Garcinia mangostana, and to identify the class of chemical compounds contained in the most active extract of Garcinia mangostana. The tests carried out at methanol, ethyl acetate, and n-hexane extracts. In the test of α-amylase inhibitory activity, using UV-Vis Spectrophotometer with λ = 490 nm. The results showed that the methanol extract had the highest inhibition percentage (93.76%) with IC50 values is 2.33 μg/mL. Meanwhile, the inhibition of α-glucosidase was tested by Microplate Reader with λ = 405 nm. The results showed methanol extract also has the smallest IC50, 48.97 μg/mL, was compared with the value of acarbose IC50 = 91.17 μg/mL as positive control. At the screening of chemical compounds, methanol extract of Garcinia mangostana leaves contain alkaloids, flavonoids, glycosides, saponins, and tannins.