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Journal : INDONESIAN JOURNAL OF PHARMACY

The determination of quercetin in Plectranthus scutellarioides(L.) R.Br. leaves extract and its In SilicoStudy on Histamine H4 Receptor Moektiwardoyo, Moelyono; Levita, Jutti; Sidiq, Syafrudin Purnama; Ahmad, Khoziah; Mustarichie, Resmi; Subarnas, Anas; ., Supriyatna
Indonesian Journal of Pharmacy Vol 22 No 3, 2011
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (337.578 KB) | DOI: 10.14499/indonesianjpharm0iss0pp191-196

Abstract

Plectranthus  scutellarioides  (L.)  R.Br.,  or  jawer  kotok,  Family  Lamiaceae, grows  widely  in  Indonesia,  and  has  a  long  history  of  therapeutic  usage  in Indonesian traditional jamuto cure various diseases. The brownish purple leaves of  Plecranthus  contain  alkaloids,  saponin,  flavonoids,  tannin,  volatile  oils,  and quercetin  which  has  been  proven  to  exert  antiinflammatory  activity.  In  this research,  a  determination  of  quercetin  in  Plecranthus  leaves  extract  was performed and followed by a study of its interaction with histamine H4 receptor to  understand its  anti-inflammatory  activity.  The  dry  leaves  were  macerated by using  a  mixture  of  methanol  and  water  (1:1)  for  48  hours  and  the  solvent  was evaporated  at  low  temperature  (40-50oC).  Analysis  of  quercetin  in  the  extract was performed by using reversed-phase HPLC method LC-10AT VP (Shimadzu), Atlantis  Hilicsilica  C18  (Waters®)  150  mm  x  4.6  mm,  5  µm  as  stationary  phase and  a  mixture  of  acetonitrile,  phosphoric  acid,  and methanol  (40:50:10),  flow rate 0.8 mL/minute.  In silicostudy of quercetin with histamine H4 receptor was performed by using AutoDock Tools 3.0.5. Histamine H4 receptor (H4R) belongs to  G  protein-coupled  receptors  which  is  involved  in arthritis,  asthma,  and inflammations.  The  3D  structure  model  of  H4R  was  built  by  using  MODELLER 9v7.  Quercetin  contained  in  Plecranthus  leaves  extract  was  0.05  %.  This compound interacted with H4R viahydrogen bond formation with Lys158 (2.006 Å)  and  Glu182  (2.048  Å),  and  van  der  Waals  interaction  with  Trp90,  Leu91, Asp94, Tyr95, Phe168, Thr178, Ser179, Tyr319, Phe344, and Tyr340, therefore Plecranthus  leaves  extract  might  have  a  chance  to  be  used  as  histamine  H4 receptor inhibitor.Key  words  :   histamine  H4  receptor,  in  silico  study,  Plecranthus  leaves,  Plectranthus scutellarioides, quercetin
Radioiodination of andrographolide and its biodistribution in mice for inflammatory tracer Jutti Levita; Cahya Nova A.; As’ari Nawawi; Slamet Ibrahim
Indonesian Journal of Pharmacy Vol 21 No 4, 2010
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (489.965 KB) | DOI: 10.14499/indonesianjpharm0iss0pp258-265

Abstract

Andrographolide,  a  bioactive  component  of  Andrographis  paniculata (Burm.F)  Nees,  is  the  major  lactone  diterpenoidal  bicyclic  constituent  in  this plant  which  has  proven  to  exert  anti-inflammatory  activity  in  vitro  which  was occurred via  several mechanism, e.g inhibition of inducible nitric oxide synthase (iNOS),  inhibition  of  radical  oxygen  species,  and  inhibition  of  NF-kappaB activation. The labeling with radionuclide is often used for therapy, detection and quantification of metabolites in the body. Even though the metabolites are very low  in  concentration  they  can  be  detected  by  the  energy  they  emitted. Radionuclide  can  be  used as  radiotracer  to  detect  whether  drug  really interacts with  its  target.  The  objective  of  this  research  is  to  synthesize 131I-labelled andrographolide  and  to  study  its  biodistribution  in  mice  to  understand  the location  of  its  organ  target.  Indirect  radioiodination  of  andrographolide  wascarried  out  by  using  bromine  as  the  leaving  group  and  followed  by  fast iodination  at  40oC,  yielded  72.6  %  purity  of  the  labeled  compound.  Iodination was occurred through proton substitution at C-12. Then the andrographolide-131I was  injected  into  lateral  vein  of  mice’s  tail  to  study  its  biodistribution.  The compound  was  distributed  in  all organs  with the  highest  accumulation  occurred in  the  stomach  (16.87  %/gram  organ).  The  result  showed  that  inducing  the animals  with  LPS  caused  inflammation  in  the  stomach  and  increased  the production  of  prostaglandin  as  proven  by  the  distribution  of  the  radioligand  in that organ.Key words: andrographolide, radioiodination, anti-inflammatory, biodistribution
BIOAVAILABILITY STUDY OF SAMBILOTO (Andrographis paniculata) HERBS INFUSION IN RABBIT Jutti Levita
Indonesian Journal of Pharmacy Vol 25 No 3, 2014
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (992.952 KB) | DOI: 10.14499/indonesianjpharm25iss3pp138

Abstract

Andrographis paniculata or sambiloto is one of the most widely used medicinal herbs in Indonesia. The main bioactive chemical constituent, andrographolide, has been reported to have various pharmacological activities. Besides its function for medical purposes, the sambiloto herbs infusion is frequently taken to maintain health. This study was conducted to determine the bioavailability of sambiloto herbs infusion in rabbit plasma, stomach, and liver, calculated as total andrographolide. Fourteen male New Zealand white rabbits were used in this study. Sambiloto herbs infusion were administered orally at the dose 7.04mL/kg body weight to each rabbit. Blood samples were taken at intervals 0.0; 0.5; 1.5; 2.0; 3.0; and 5.0h after infusion administration. Sambiloto herbs infusion, which are calculated as andrographolide, levels in plasma, stomach, and liver were analyzed by high performance liquid chromatography using C-18 column as stationary phase and a mixture of methanol-double distilled water (60:40) as mobile phase. Bioavailability parameters obtained were Cmax 0.5549µg/mL (in stomach), 0.2136µg/mL (in plasma), 0.0051µg/mL (in liver); while tmax 1h (in stomach), 1.5h (in plasma), 2h (in liver); and AUC 1.7451µg.h/mL (in stomach), 0.434µg.h/mL (in plasma), 0.0038µg.h/mL (in liver). These data showed that in healthy animals, sambiloto herbs infusion was fastly absorbed from the stomach, distributed in the circulation system, and metabolized in the liver, in subsequent process. Sambiloto herbs infusion showed good bioavailability in rabbit. 
Co-Authors A. Diantini - A. Mutalib - Abdul Mutalib Abdul Mutalib Abdul Mutholib Achmad Al Baihaqi Ade Zuhrotun Agung Karuniawan Ahmad Muhtadi AINAA HAZIRAH SHAMSUL ANUAR AJENG DIANTINI Ajeng Diantini, Ajeng Amalia, Riezki Ami Rahmati Syadiah Anas Subarnas Anas Subarnas Anggraeni, Sra R. Anis Khoirunisa Anis Khoirunisa, Anis Anis Yohana Chaerunisaa Anisa Pebiansyah Anna Yuliana, Anna Ardiansyah, Fahriza As'ari Nawawi As'ari Nawawi As’ari Nawawi Aulifa, Diah L. Batari A. Larasati Bawono, Lidya Cahyo Billy Dwi Saputra Cahya Nova A. Chyntia R. Wijaya Dani Sujana Debby Ustari Diah Lia Aulifa DIANTINI, AJENG - Diina, Tresnafuty Rasyiida Dina Mulyana Syafitri DINA SEMBIRING Dinny Andriany Dinny Andriany, Dinny DOLIH GOZALI Dolih Gozali Driyanti Rahayu Driyanti Rahayu Dwi Lestari Sulistyaningsih Eli Halimah Eli Halimah, Eli Ellin Febrina Ellin Febrina Ellin Febrina Ellin Febrina Enade P. Istyastono Ervita Indriani Fara Warhead Fara Warhead, Fara Fathurrahmi Fathurrahmi Fattah, Miswar Fauzan Fikri Febrina Amelia Saputri Fikri, Fauzan Firdha S Maelaningsih Firdha S Maelaningsih, Firdha S Gofarana Wilar Herawati, Irma E. HILMA AWALIA RAHMAH Ida Musfiroh Ida Musfiroh - Ika WAHYUNI Imam A. Wicaksono Indah Suasani Wahyuni Indah Suasani Wahyuni INDRIANI, ERVITA Indriyanti R. Sukmana Irma Erika Herawati Irma Erika Herawati Irma Erika Herawati Irma Erika Herawati Irma M. Puspitasari, Irma M. Irma Melyani Puspitasari Irma Meylani Puspitasari Iwan J. P. de Esch IYAN RIFKY HIDAYAT Jennifer Kolina Jiranusornkul, Supat Jopi Arpina Kee P. Shan Keri Lestari Khairinisa, Miski Aghnia Khoziah Ahmad, Khoziah KIKI IKRIMA Kolina, Jennifer Marline Abdassah Marline Abdassah Marline Abdassah, Marline Maryam Hasymia Ishmatullah Masripah Masripah Masripah Megantara, Sandra MEGANTARA, SANDRA Meigita Indah Farkhani Ming, Wong Chun Miswar Fattah Mochamad Rizal Moelyono Moektiwardoyo Moelyono Moektiwardoyo, Moelyono Monika Novryanti Monika Novryanti, Monika Muchtaridi Muchtaridi Muhammad Ikhsan Muhammad Ryan Radix Rahardhian Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Mutakin Nawawi, Asari Nela - Simanjuntak Nuraeni Nuraeni Nurdjanah Azinar Nyi M. Saptarini Nyi M. Saptarini Nyi M. Saptarini Nyi Mekar Saptarini Pratidina, Malfa Laila Putri, Refitha Nurul Raden Maya Febriyanti Renny Amelia Renyiska Yula Resha Resmawati Shaleha Resmi Mustarichie Ridwan, Hanna Salwa Riezki Amalia Riezki Amalia Riezki Amalia Riezki Amalia Rini Daud Supu Rini Hendriani Ronny Lesmana Rosdianto, Aziiz M. Rusdianto, Aziiz M. Saeful Amin, Saeful Saptarini, Nyi M. Shaleha, Resha Resmawati Shan, Kee P. Shelvy E Suherman Shelvy E Suherman Shelvy E Suherman, Shelvy E Sitepu, Rini Daud Slamet Ibrahim Slamet Ibrahim Slamet Ibrahim Slamet Ibrahim Slamet Ibrahim Sofa D. Alfian Sofa D. Alfian, Sofa D. Sohadi Warya Sohadi Warya Sra R. Anggraeni Sri A. Sumiwi Sri Adi Sumiwi Sri Adi Sumiwi Sriwidodo Sriwidodo STEFANNY AGNES SALIM Steffi Liem Steffi Liem Sukmana, Indriyanti R. Sumiwi, Sri A. Sumiwi, Sri A. Supriyatna ., Supriyatna Susilawati, Elis Syadiah, Ami Rahmati Syafrudin Purnama Sidiq, Syafrudin Purnama Tarkus Suganda Tenri Noviardani Tenri Noviardani, Tenri TIANA MILANDA Tina Rostinawati Tresnafuty Rasyiida Diina Trixie A. Ulimaz Ulfinana Hafni Vergel Concibido Virda Aziza Wahyuni, Indah S. Wijaya, Chyntia R. Winarni, Rina Wiwiek Indriyati - Wong Chun Ming Yasmiwar Susilawati Yogiyanto Yogiyanto Yudha Prabowo Yuli Andriani Yulin Prisdiany ZAHRA DZAKIRAH ABNAZ Zain, Dichy Nuryadin ZELIKA MEGA RAMADHANIA