Exploration of Xanthone Derivatives as Anti-Cancer Agents against Colorectal Cancer

Colorectal cancer currently occupies the third position of globally cancer morbidity and is the second leading cause of cancer death after lung cancer. Chemotherapy administration is still the main modality for the colorectal cancer stage I to III. Its usage is limited, since its high resistance and risk of side effects. Thus, exploration and development of novel colorectal anti-cancer drugs, including compounds derived from nature origin is needed. Xanthone becomes one natural compound which may be potentially developed as an anti-colorectal cancer due to its cytotoxic and anti-proliferative activities. The in vitro cytotoxic and anti-proliferative actions of xanthone compounds occur through a variety of mechanisms involving both apoptotic induction and inhibition of cell cycle, while in vivo may reduce the tumor size. Since colorectal cancer is frequently treated in a combination therapy, xanthone compounds have also been studied in a combination use and proven effective as co-chemotherapy with the standard chemotherapy drugs. This paper aims at providing an overview of colorectal cancer, pathology, risk factors and protective factors, as well as discussing the current therapies and potential xanthone compounds as an alternative therapy which may be developed later for the colorectal cance

Aspirin as a Chemopreventive Agent for Cancer: a New Hope?

Introduction: inflammation has been shown to play a major role in the pathogenesis of cancer. Inflammatory process activates the immune system through pro-inflammatory mediators and subsequent triggers transformation into malignant cells. Some tumors or cancers has been associated with chronic infections, such as hepatitis B and C viruses (hepatocellular carcinoma), human papilloma virus (cervical cancer), Helicobacter pylori (gastric cancer and lymphoma), and prostatitis (prostate cancer). A considerable study have investigated the benefits of aspirin for the prevention and treatment of cancer or tumors. Objectives: This paper aims to describe the relationship between inflammation and cancer incidence, so that use of aspirin as an anti-inflammatory agent is a rational choice in the treatment and prevention of cancer. Conclusion: Aspirin potential for chemoprevention of various types of cancer. Considering the high risk of side effects of aspirin, aspirin is not intended as a routine therapy to prevent the occurrence of cancer

Analysis of Capecitabine Plus Oxaliplatin (Xelox) Combination in the Management of Metastatic Colorectal Cancer Compare with Fluorouracil and Oxaliplatin Combination (Folfox)

Background : Combinations of Fluorouracil (FU) and biomodulator Leucovorin (LV) established as a standard regimen for therapy of colorectal cancer with metastases. To give better antitumor activity in colorectal cancer therapy, oxaliplatin is combined with FU/LV and give significant improvement. Fluorouracil can only be given by intravenous administration. This limitation raised effort to find alternative drugs that can be given orally, such as capecitabine. Capecitabine is an oral FU prodrug, with high oral bioavailability, highly accumulated in neoplastic tissue to be converted in FU, and well tolerated. Some clinical studies revealed effectivity of capecitabine plus oxaliplatin (XELOX) compared to FU/LV plus oxaliplatin (FOLFOX). Objective : This article is aimed to compare non inferiority of XELOX to FOLFOX in colorectal cancer with metastases, viewed form primary outcomes and secondary outcomes. Results : XELOX was comparable to FOLFOX with some benefitsover FOLFOX. Conclusion : XELOX could be considered as FOLFOX replacement as a standard therapyfor colorectal cancer with metastases

Therapeutic Drug Monitoring (TDM) in The Use of Aspirin as Antirheumatoid Drugs

Therapeutic drug monitoring (TDM) is used in drug therapy for selected drugs with narrow therapeutic index, or a broad range of kinetics variation, or drugs with strong correlation between plasma concentration and clinical effects or toxicity. Aspirin is one of the widely used old generation drugs, with a broad range of activity spectrum: analgesic, antipyretic, antiâ€inflammatory, and antiplatelet. As antiâ€inflammatory drug, aspirin directed as therapy for many of chronic inflammation, such as rheumatoid arthritis. As an antirheumatic agent, aspirin shows a wide variation in the pharmacokinetic of aspirin metabolism, and has a narrow therapeutic index because it effectives at concentration of 10â€30 mg/dl, but at more than 40 mg/dl intoxication occurs (metabolic acidosis, hyperpnea, and death). Those are why aspirin use as antirheumatic agent need therapeutic drug monitoring, so that doctors can guarantee that plasma aspirin concentration is in the therapeutic range, to achieve optimilization of therapy with minimal side effects. This article reveals about use of aspirin as antirheumatoid drugs and why therapeutic drug monitoring is needed in aspirin use (Sains Medika, 4(2):210â€226)

Analysis of capecitabine plus oxaliplatin (xelox) combination in the management of metastatic colorectal cancer compare with fluorouracil and oxaliplatin combination (folfox)

Background : Combinations of Fluorouracil (FU) and biomodulator Leucovorin (LV) established as a standard regimen for therapy of colorectal cancer with metastases. To give better antitumor activity in colorectal cancer therapy, oxaliplatin is combined with FU/LV and give significant improvement. Fluorouracil can only be given by intravenous administration. This limitation raised effort to find alternative drugs that can be given orally, such as capecitabine. Capecitabine is an oral FU prodrug, with high oral bioavailability, highly accumulated in neoplastic tissue to be converted in FU, and well tolerated. Some clinical studies revealed effectivity of capecitabine plus oxaliplatin (XELOX) compared to FU/LV plus oxaliplatin (FOLFOX). Objective : This article is aimed to compare non inferiority of XELOX to FOLFOX in colorectal cancer with metastases, viewed form primary outcomes and secondary outcomes. Results : XELOX was comparable to FOLFOX with some benefitsover FOLFOX. Conclusion : XELOX could be considered as FOLFOX replacement as a standard therapyfor colorectal cancer with metastases

PENGEMBANGAN EKSTRAK FLAVONOID MADU MONOFLORA SEBAGAI INGREDIENT MINUMAN FUNGSIONAL TINGGI ANTIOKSIDAN

Beberapa tahun terakhir telah terlihat meningkatnya minat konsumen, industri makanan, dan peneliti ke pangan dan cara-cara yang dapat membantu menjaga kesehatan manusia, salah satunya minuman fungsional. Madu mempunyai aktivitas antioksidan yang signifikan yang berkorelasi kuat dengan kandungan flavonoidnya dari berbagai sumber bunga, sehingga madu sangat potensial sebagai bahan baku minuman fungsional. Namun sampai saat ini belum ada minuman fungsional yang ingredient-nya flavonoid dari madu. Penelitian tahun pertama bertujuan untuk mengetahui: 1) kadar flavonoid total, 2) aktivitas antioksidan metode DPPH, 3) kapasitas antioksidan metode FRAP, 4) hubungan kadar flavonoid total dengan aktivitas antioksidan metode DPPH, 5) hubungan kadar flavonoid total dengan kapasitas antioksidan metode FRAP, 6) hubungan aktivitas antioksidan metode DPPH dengan kapasitas antioksidan metode FRAP dari beberapa jenis madu monoflora, dan 7) proses pembuatan ekstrak flavonoid dari madu monoflora terbaik. Bahan baku madu didapat dari peternak lebah di Daerah Istimewa Yogyakarta dan Jawa Tengah. Analisis kadar flavonoid total menurut metode Al dkk (2009) dan analisis aktivitas antioksidan menggunakan metode DPPH (diphenyl-1-picryl hydrazyl) menurut Hussein dkk (2011), dan kapasitas antioksidan metode FRAP dilakukan menurut metode Aljadi & Kamaruddin, (2004). Analisis data dilakukan dengan anava dan dilanjutkan dengan DMRT untuk mengetahui perbedaan antar sampel. Hubungan kadar flavonoid total dan aktivitas antioksidan, kadar flavonoid total dengan kapasitas antioksidan, dan aktivitas antioksidan dan kapasitas antioksidan madu monoflora dihitung dengan regresi sederhana untuk mengetahui nilai korelasinya. Setelah diketahui madu monoflora yang terbaik, selanjutnya dibuat ekstrak flavonoid madu terbaik tersebut menurut metode (Rizzardini, 2009). Hasil penelitian menunjukkan bahwa: 1) kadar flavonoid total madu bunga rambutan, kelengkeng, kopi, randu, dan kaliandra berturut-turut adalah 3,80; 4,94; 23,94; 12,92 dan 33,46 mg quercetin/ 100 g madu, 2) aktivitas antioksidan metode DPPH madu bunga rambutan, kelengkeng, kopi, randu, dan kaliandra berturutturut adalah 11,9; 8,73; 5,56; 13,1 dan 48,0 %, 3) kapasitas antioksidan metode FRAP madu bunga rambutan, kelengkeng, kopi, randu, dan kaliandra berturutturut adalah 1246, 1298, 1807, 1614, dan 5386 μM Fe(II), 4) terdapat hubungan antara kadar flavonoid total dan aktivitas antioksidan madu bunga rambutan, kelengkeng, kopi, randu, dan kaliandra dengan skor korelasi sebesar 0,922, 5) terdapat hubungan antara kadar flavonoid total dan kapasitas antioksidan madu bunga rambutan, kelengkeng, kopi, randu, dan kaliandra dengan skor korelasi sebesar 0,931, 6) terdapat hubungan antara aktivitas antioksidan dan kapasitas antioksidan madu bunga rambutan, kelengkeng, kopi, randu, dan kaliandra dengan skor korelasi sebesar 0,996

PENGARUH UMUR SALAK PONDOH TERHADAP MINUMAN SARI BUAH SALAK PONDOH

Penelitian ini bertujuan untuk mengetahui: 1) karakteristik sensoris buah salak pondoh berdasarkan umur buah, 2) karakteristik sensoris minuman sari buah salak pondoh yang dibuat dari salak pondoh dengan umur buah berbeda, 3) pengaruh karakteristik sensoris buah salak pondoh terhadap karakteristik sensoris minuman sari buahnya. Penelitian ini dilakukan sejak bulan Juli sampai November 2013 di Laboratorium Kimia Jurusan Pendidikan Teknik Boga dan Busana Fakultas Teknik Universitas Negeri Yogyakarta. Penelitian formula minuman sari buah salak dilakukan dengan metode acak lengkap 3x2 (3 umur salak dan 2 batch ulangan). Karakteristik sensoris buah salak dan minuman sari buah salak diuji dengan uji beda dengan 7 skala penilaian (1=intensitas nilai paling rendah, 7=intensitas nilai paling tinggi) oleh 25 orang panelis agak terlatih. Data yang diperoleh selanjutnya dianalisis varians (anava), dan jika berbeda nyata dilanjutkan dengan Least Square Difference (LSD). Korelasi antar perlakuan diuji dengan korelasi Pearson Bivariate dengan menggunakan program komputer SPSS 12.0 for Windows. Hasil penelitian menunjukkan bahwa: 1) buah salak pondoh dengan umur buah yang berbeda mempunyai karakteristik yang sama dalam hal aroma, rasa salak, rasa asam, dan rasa manis, sedangkan teksturnya yang paling lunak adalah salak tua, sedangkan salak muda dan salak sedang teksturnya sama, 2) minuman sari buah salak pondoh dari buah salak dengan umur buah berbeda mempunyai karakter yang sama pada semua sifat yang diujikan, yaitu aroma, kejernihan, rasa asam, dan rasa manis, 3) hasil uji korelasi Pearson menunjukkan korelasi antara: a) aroma buah dan aroma sari buah adalah 0,466, b) tesktur buah dan kejernihan sari buah adalah 0,181, c) rasa asam buah dan rasa asam sari buah adalah 0,619, dan d) rasa manis buah dan rasa manis sari buah adalah 0,347 yang menunjukkan bahwa semua sifat yang diuji tidak menunjukkan korelasi. Hasil ini menunjukkan bahwa untuk membuat sari buah salak pondoh bisa digunakan buah salak pondoh muda, sedang maupun tua tanpa berpengaruh terhadap sari buahnya

Perbandingan Efektivitas Teofilin (1,3-Dimethylxanthine) dan Kafein (1,3,7-Trimethylxanthine) dalam Menunda Kelelahan Otot pada Tikus

Kelelahan otot merupakan suatu kondisi dimana otot kehilangan kemampuan berkontraksi karena stimuli terus menerus dan hal ini dikaitkan dengan penurunan cadangan glikogen. Obat derivat methylxanthine (kafein dan teofilin) bermanfaat untuk menghemat penggunaan glikogen. Penelitian ini bertujuan untuk menggali efektivitas kafein dan teofilin dalam menunda kelelahan otot sebagaimana yang diukur dalam lama struggling. Sebanyak 18 (delapan belas) ekor tikus berusia ± 3 bulan, berat 200-210 gram, kadar Hb 11,5-16 mg/dL dan kadar Hmt 35-51%, dibagi secara acak ke dalam 3 kelompok perlakuan: kontrol (akuades 1 mL/kgBB), kafein 3,78% (1 mL/kgBB) dan teofilin 3,15% (1 mL/kgBB). Kelelahan otot diukur dengan lama struggling dalam detik. Data rerata lama struggling antar kelompok dianalisis dengan one way ANOVA. Hasil menunjukkan bahwa lama struggling untuk kelompok kafein (286.83+7.11) detik dan teofilin (312.33+15.92) detik, lebih lama daripada kelompok kontrol (140.33+23.24) (p0,05), sedangkan lama struggling kelompok kafein dengan teofilin tidak berbeda bermakna (p0,05). Disimpulkan bahwa kafein dan teofilin mampu menunda kelelahan otot pada tikus dan efektifitasnya sebanding

Potency of Xanthone Derivatives as Antibacterial Agent Against Methicillin-Resistant Staphylococcus Aureus (MRSA)

Antibiotic resistance is increasing worldwide and becoming a serious problem for the treatment of patients and also affecting their economy. One instance of bacteria that is resistant to the antibiotic is Methicillin- Resistant Staphylococcus aureus (MRSA). MRSA infections are fatal and even deadly. Some MRSA strain has shown resistance towards currently available antibacterial agents. To overcome this, we need new compound alternatives. One of the compounds currently being developed is xanthone derivatives. Xanthones can be found in many kinds of plants, including Garcinia mangostana , in which the active compounds are mangostanin and α-mangostin. Xanthones is effective against several types of Grampositive and Gram-negative bacterias, including Staphylococcus species. Some studies have shown that xanthone derivatives are effective against Staphylococcus aureus, including MRSA. One of the proposed mechanisms of xanthone's antibacterial activity is the involvement of the bacteria's cytoplasmic membrane. Xanthone amphiphilic compounds are capable of disrupting bacterial membrane through a mechanism called interfacial activity models. Xanthone can also act as the antioxidant and by inducing the release of lipoteichoic acid (LTA) from the cell wall of MRSA. LTA is the main constituent of the cell wall of Gram-positive bacteria, which are covalently bonded to the outside of peptidoglycan. This structure is important for cell division and bacterial osmotic protection. Thus, it is believed that the mechanism of action of xanthones involved damaging bacterial cell membrane