Sel T-regulator (Treg) memainkan peran kunci dalam mengendalikan autoimunitas, respon alergi, per... more Sel T-regulator (Treg) memainkan peran kunci dalam mengendalikan autoimunitas, respon alergi, peradangan, dan respons terhadap infeksi. Sel T Cd4+ yang secara konstitutif mengekspresikan Cd25 dan protein forkhead 3 (Foxp3; yaitu, Cd3+Cd4+Cd25+Foxp3+) atau disebut juga sebagai Treg fungsional, telah terbukti memainkan peran utama dalam pemeliharaan toleransi dan homeostasis imun, sehingga deteksi Treg fungsional sangat penting dilakukan sebagai salah satu parameter imunomodulasi. Penelitian ini bertujuan untuk mendeteksi populasi sel Treg (Cd3+Cd4+Cd25+Foxp3+) pada organ limpa mencit galur Balb/c dan Swiss-webster dengan menggunakan metode yang mudah, cepat, serta terjangkau. Metode deteksi sel Treg dilakukan dengan cara isolasi organ limpa mencit Balb/c dan Swiss-webster kemudian dilakukan preparasi dan deteksi sel menggunakan instrumen flow cytometry. Hasil populasi sel Treg yang didapatkan berturut-turut pada mencit Balb/c dan Swiss-webster adalah 2,02 ± 0,36% dan 3,14 ± 1,64% dar...
The global pandemic related to the coronavirus (2019-nCoV) continues to hit the world, including ... more The global pandemic related to the coronavirus (2019-nCoV) continues to hit the world, including Indonesia until the end of 2021. The efforts to improve health services were carried out by various parties, including by members of the King of Christ Parish church as part of the Surabaya community. From this parish in July 2021, 301 people were sick with COVID-19 and almost 11% of them died. The public and health services were panicked by the occurrence of a wave of viral mutations, with the increasing of sufferers and high mortality rates. Integrated telemedicine services between doctors and pharmacists are one of the best options to prevent transmission and severity to support patient recovery rates. With telemedicine, health care needs are individualized and patient development is more controlled. The method was carried out through direct consultation between doctors, pharmacist, and patients, using the whatsapp call platform. Monitoring of patients was continued by pharmacist usin...
Introduction: Salicylic acid derivate is very popular for its activity to suppress pain, fever, a... more Introduction: Salicylic acid derivate is very popular for its activity to suppress pain, fever, and inflam ma tion. One of its derivatives is acetylsalicylic acid (ASA) wh ich has be en reported repeatedly that, as a nonsteroidal anti-inflam ma tory drug (NSAID), it has a cardioprotective effect. Although ASA has various advantages, several stud ies have reported that it ma y indu ce severe peptic ulcer disease. We recently synthesized a new compoun d derived from salicylic acid, name ly 2-((3-(chloromethyl)be nz oyl)oxy)be nz oic acid (3-CH 2 Cl) wh ich still has the be nefit of acetylsalicylic acid as an analgesic and antiplatelet, bu t lacks its harmful side effects (Caroline et al., 20 19). In addition, in silico stud ies of 3-CH 2 Cl showed a higher affinity towards protein receptor cyclooxygenase-2 (COX-2; PDB: 5F1A) than ASA. We hypothesized that 3-CH 2 Cl inhibits the COX-2 activity wh ich could presumably decrease the inflam ma tory responses. However, no knowledge is available on the anti-inflam ma tory response and molecular signaling of this new compoun d. Henc e, in this stud y, we investigated the potential func tional relevanc e of 3-CH 2 Cl in regulating the inflamma tory response in lipopolysacch aride (LPS)-indu ced rats. The results of this stud y show that this compoun d could significantly redu ce the inflam ma tory parame ter in LPS-indu ced rats. Material and methods: Rats were indu ced with LPS of 0.5 mg/kg bw intravenously, prior oral administration with vehicle (3 % Pulvi s Gumm i Arabicum / PGA), 50 0 mg/60 kg body weight (b w; rat dosage converted to hu ma n) of 3-CH 2 Cl and ASA. The inflam ma tory parame ters such as ch anges in the temperature of septic shock, cardiac blood plasma concentrations of IL-1β and TNF-α (ELISA), blood inflam ma tion parame ters, wh ite blood cell concentrations, and lung histopathology were observed. Meanwh ile, the stability of 3-CH 2 Cl powder was evaluated. Result: After the administration of 50 0 mg/60 kg bw of 3-CH 2 Cl (rat dosage converted to hu ma n) to LPSindu ced rats, we observed a significant redu ction of both TNF-α (5 .70+ /-1.04 × 10 3 pg/mL, p= <0 .001) and IL-1β (2 .32+ /-0.28 × 10 3 pg/mL, p= <0 .001) cardiac blood plasma concentrations. Besides, we foun d a redu ction of wh ite blood cell concentration and the severity of lung injury in the 3-CH 2 Cl group compared to the LPS-indu ced rat group. Ad ditionally, this compoun d ma intained the rat body temperature within norma l limits du ring inflam ma tion, preventing the rats to un dergo septic shock, ch aracterized by hypothermic (t = 12 0 min.) or hyperthermic (t = 36 0 min) conditions. Furthermore, 3-CH 2 Cl was foun d to be stable un til 3 years at 25°C with a relative hu midity of 75 ± 5%. Conclusion: 3-CH 2 Cl compoun d inhibited inflam ma tion in the LPS-indu ced inflam ma tion response model in rats, hypothetically through bind ing to COX-2, and presumably inhibited LPS-indu ced NF-κβ signaling pathways. This stud y could be used as a preliminary hint to investigate the target molecular pathways of 3-CH 2 Cl as a novel and less toxic therapeutical agent in alleviating the COX-related inflam ma tory diseases, and most importantly to support the planning and developme nt of clinical trial.
Acetylsalicylic acid is used as a non-steroidal anti-inflammatory drugs (NSAID) and antiplatelet ... more Acetylsalicylic acid is used as a non-steroidal anti-inflammatory drugs (NSAID) and antiplatelet agents by inhibiting cyclooxygenases. However, therapy using acetylsalicylic acid could induce gastric bleeding and cause other gastrointestinal toxicity. The aim of this study was to demonstrate the synthesis of a new compound bearing salicylic acid residue namely 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid, to analyze its potential as a ligand for human cyclooxygenase-2 (COX-2) receptor, to evaluate its toxicity level and its effectiveness for analgesic and antiplatelet agent compared with acetylsalicylic acid. Synthesis of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid was conducted by microwave irradiation. The purity of this compound was evaluated with TLC, IR, NMR, and EDS spectroscopy. The chemical characterization and docking studies against human COX-2 (PDB:5F1A) was performed in-silico. The acute oral toxicity assay was performed under OECD guidelines. The analgesic activity study was performed by plantar and writhing test on animal model. For anti-platelet activity study, we performed tail-bleeding assay and flow cytometry based platelet aggregation assay. We could successfully synthesize a pure white crystalline 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid. In-Silico G-Score result of those compounds gives us preliminary hint of the potential affinity of this compound as a ligand for COX-2 receptor (PDB: 5F1A). Acute toxicity and microscopic gastrointestinal assessments indicated non-observable harmful toxicity parameters. The plantar response time of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid treated groups showed a significant increment (P < 0.01), and the nociceptive response in writhing test demonstrated a significant dose-dependent decrement. This indicated that its analgesic activity was better than acetylsalicylic acid. The platelet aggregation of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid was lower than its controls, indicating an aggregation inhibition pattern. The animals treated with 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid gave a longer bleeding time. Overall, this study demonstrated a successful synthesis of pure 2-((3-(chloromethyl)benzoyl)oxy) benzoic acid. We postulated that this compound was better than acetylsalicylic acid, exhibiting excellent analgesic and antiplatelet activity with no toxicity impact.
Phytochemical screening and preliminary clinical trials of the aqueous extract mixture of Androgr... more Phytochemical screening and preliminary clinical trials of the aqueous extract mixture of Andrographis paniculata (Burm. f.) Wall. ex Nees and Syzygium polyanthum (Wight.) Walp leaves in metformin treated patients with type 2 diabetes
International Journal of Applied Pharmaceutics, 2019
Objective: A new compound of salicylic acid derivative, namely 2-((3-(chloromethyl)benzoyl)oxy)be... more Objective: A new compound of salicylic acid derivative, namely 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid (3CBB), was synthesized to find a compound exhibiting higher analgesic activity and smaller ulcer irritation than acetylsalicylic acid (ASA). Therefore, this study aimed to investigate the pharmacokinetics of this new compound in rats, following a single dose oral administration of 3CBB (45 mg/kg BW). Methods: Plasma samples of 9 healthy rats were collected before and up to 3 h after its oral administration, following an 18 h fasting period. Plasma concentrations of 3CBB were determined using a validated HPLC-DAD assay. Pharmacokinetic parameters were determined using the compartment model technique. All experiments were carried out in triplicate. Results: The pharmacokinetic parameters of 3CBB obtained were as follows: Tmax= 28.9±1.1 min, Cmax = 0.57±0.02 µg/ml, AUCtotal = 66.3±1.0 µg min/ml, Kel = 0.018±0.002 min-1, and T1/2el = 39.4±3.9 min. The long elimination half-life a...
Sel T-regulator (Treg) memainkan peran kunci dalam mengendalikan autoimunitas, respon alergi, per... more Sel T-regulator (Treg) memainkan peran kunci dalam mengendalikan autoimunitas, respon alergi, peradangan, dan respons terhadap infeksi. Sel T Cd4+ yang secara konstitutif mengekspresikan Cd25 dan protein forkhead 3 (Foxp3; yaitu, Cd3+Cd4+Cd25+Foxp3+) atau disebut juga sebagai Treg fungsional, telah terbukti memainkan peran utama dalam pemeliharaan toleransi dan homeostasis imun, sehingga deteksi Treg fungsional sangat penting dilakukan sebagai salah satu parameter imunomodulasi. Penelitian ini bertujuan untuk mendeteksi populasi sel Treg (Cd3+Cd4+Cd25+Foxp3+) pada organ limpa mencit galur Balb/c dan Swiss-webster dengan menggunakan metode yang mudah, cepat, serta terjangkau. Metode deteksi sel Treg dilakukan dengan cara isolasi organ limpa mencit Balb/c dan Swiss-webster kemudian dilakukan preparasi dan deteksi sel menggunakan instrumen flow cytometry. Hasil populasi sel Treg yang didapatkan berturut-turut pada mencit Balb/c dan Swiss-webster adalah 2,02 ± 0,36% dan 3,14 ± 1,64% dar...
The global pandemic related to the coronavirus (2019-nCoV) continues to hit the world, including ... more The global pandemic related to the coronavirus (2019-nCoV) continues to hit the world, including Indonesia until the end of 2021. The efforts to improve health services were carried out by various parties, including by members of the King of Christ Parish church as part of the Surabaya community. From this parish in July 2021, 301 people were sick with COVID-19 and almost 11% of them died. The public and health services were panicked by the occurrence of a wave of viral mutations, with the increasing of sufferers and high mortality rates. Integrated telemedicine services between doctors and pharmacists are one of the best options to prevent transmission and severity to support patient recovery rates. With telemedicine, health care needs are individualized and patient development is more controlled. The method was carried out through direct consultation between doctors, pharmacist, and patients, using the whatsapp call platform. Monitoring of patients was continued by pharmacist usin...
Introduction: Salicylic acid derivate is very popular for its activity to suppress pain, fever, a... more Introduction: Salicylic acid derivate is very popular for its activity to suppress pain, fever, and inflam ma tion. One of its derivatives is acetylsalicylic acid (ASA) wh ich has be en reported repeatedly that, as a nonsteroidal anti-inflam ma tory drug (NSAID), it has a cardioprotective effect. Although ASA has various advantages, several stud ies have reported that it ma y indu ce severe peptic ulcer disease. We recently synthesized a new compoun d derived from salicylic acid, name ly 2-((3-(chloromethyl)be nz oyl)oxy)be nz oic acid (3-CH 2 Cl) wh ich still has the be nefit of acetylsalicylic acid as an analgesic and antiplatelet, bu t lacks its harmful side effects (Caroline et al., 20 19). In addition, in silico stud ies of 3-CH 2 Cl showed a higher affinity towards protein receptor cyclooxygenase-2 (COX-2; PDB: 5F1A) than ASA. We hypothesized that 3-CH 2 Cl inhibits the COX-2 activity wh ich could presumably decrease the inflam ma tory responses. However, no knowledge is available on the anti-inflam ma tory response and molecular signaling of this new compoun d. Henc e, in this stud y, we investigated the potential func tional relevanc e of 3-CH 2 Cl in regulating the inflamma tory response in lipopolysacch aride (LPS)-indu ced rats. The results of this stud y show that this compoun d could significantly redu ce the inflam ma tory parame ter in LPS-indu ced rats. Material and methods: Rats were indu ced with LPS of 0.5 mg/kg bw intravenously, prior oral administration with vehicle (3 % Pulvi s Gumm i Arabicum / PGA), 50 0 mg/60 kg body weight (b w; rat dosage converted to hu ma n) of 3-CH 2 Cl and ASA. The inflam ma tory parame ters such as ch anges in the temperature of septic shock, cardiac blood plasma concentrations of IL-1β and TNF-α (ELISA), blood inflam ma tion parame ters, wh ite blood cell concentrations, and lung histopathology were observed. Meanwh ile, the stability of 3-CH 2 Cl powder was evaluated. Result: After the administration of 50 0 mg/60 kg bw of 3-CH 2 Cl (rat dosage converted to hu ma n) to LPSindu ced rats, we observed a significant redu ction of both TNF-α (5 .70+ /-1.04 × 10 3 pg/mL, p= <0 .001) and IL-1β (2 .32+ /-0.28 × 10 3 pg/mL, p= <0 .001) cardiac blood plasma concentrations. Besides, we foun d a redu ction of wh ite blood cell concentration and the severity of lung injury in the 3-CH 2 Cl group compared to the LPS-indu ced rat group. Ad ditionally, this compoun d ma intained the rat body temperature within norma l limits du ring inflam ma tion, preventing the rats to un dergo septic shock, ch aracterized by hypothermic (t = 12 0 min.) or hyperthermic (t = 36 0 min) conditions. Furthermore, 3-CH 2 Cl was foun d to be stable un til 3 years at 25°C with a relative hu midity of 75 ± 5%. Conclusion: 3-CH 2 Cl compoun d inhibited inflam ma tion in the LPS-indu ced inflam ma tion response model in rats, hypothetically through bind ing to COX-2, and presumably inhibited LPS-indu ced NF-κβ signaling pathways. This stud y could be used as a preliminary hint to investigate the target molecular pathways of 3-CH 2 Cl as a novel and less toxic therapeutical agent in alleviating the COX-related inflam ma tory diseases, and most importantly to support the planning and developme nt of clinical trial.
Acetylsalicylic acid is used as a non-steroidal anti-inflammatory drugs (NSAID) and antiplatelet ... more Acetylsalicylic acid is used as a non-steroidal anti-inflammatory drugs (NSAID) and antiplatelet agents by inhibiting cyclooxygenases. However, therapy using acetylsalicylic acid could induce gastric bleeding and cause other gastrointestinal toxicity. The aim of this study was to demonstrate the synthesis of a new compound bearing salicylic acid residue namely 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid, to analyze its potential as a ligand for human cyclooxygenase-2 (COX-2) receptor, to evaluate its toxicity level and its effectiveness for analgesic and antiplatelet agent compared with acetylsalicylic acid. Synthesis of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid was conducted by microwave irradiation. The purity of this compound was evaluated with TLC, IR, NMR, and EDS spectroscopy. The chemical characterization and docking studies against human COX-2 (PDB:5F1A) was performed in-silico. The acute oral toxicity assay was performed under OECD guidelines. The analgesic activity study was performed by plantar and writhing test on animal model. For anti-platelet activity study, we performed tail-bleeding assay and flow cytometry based platelet aggregation assay. We could successfully synthesize a pure white crystalline 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid. In-Silico G-Score result of those compounds gives us preliminary hint of the potential affinity of this compound as a ligand for COX-2 receptor (PDB: 5F1A). Acute toxicity and microscopic gastrointestinal assessments indicated non-observable harmful toxicity parameters. The plantar response time of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid treated groups showed a significant increment (P < 0.01), and the nociceptive response in writhing test demonstrated a significant dose-dependent decrement. This indicated that its analgesic activity was better than acetylsalicylic acid. The platelet aggregation of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid was lower than its controls, indicating an aggregation inhibition pattern. The animals treated with 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid gave a longer bleeding time. Overall, this study demonstrated a successful synthesis of pure 2-((3-(chloromethyl)benzoyl)oxy) benzoic acid. We postulated that this compound was better than acetylsalicylic acid, exhibiting excellent analgesic and antiplatelet activity with no toxicity impact.
Phytochemical screening and preliminary clinical trials of the aqueous extract mixture of Androgr... more Phytochemical screening and preliminary clinical trials of the aqueous extract mixture of Andrographis paniculata (Burm. f.) Wall. ex Nees and Syzygium polyanthum (Wight.) Walp leaves in metformin treated patients with type 2 diabetes
International Journal of Applied Pharmaceutics, 2019
Objective: A new compound of salicylic acid derivative, namely 2-((3-(chloromethyl)benzoyl)oxy)be... more Objective: A new compound of salicylic acid derivative, namely 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid (3CBB), was synthesized to find a compound exhibiting higher analgesic activity and smaller ulcer irritation than acetylsalicylic acid (ASA). Therefore, this study aimed to investigate the pharmacokinetics of this new compound in rats, following a single dose oral administration of 3CBB (45 mg/kg BW). Methods: Plasma samples of 9 healthy rats were collected before and up to 3 h after its oral administration, following an 18 h fasting period. Plasma concentrations of 3CBB were determined using a validated HPLC-DAD assay. Pharmacokinetic parameters were determined using the compartment model technique. All experiments were carried out in triplicate. Results: The pharmacokinetic parameters of 3CBB obtained were as follows: Tmax= 28.9±1.1 min, Cmax = 0.57±0.02 µg/ml, AUCtotal = 66.3±1.0 µg min/ml, Kel = 0.018±0.002 min-1, and T1/2el = 39.4±3.9 min. The long elimination half-life a...
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