Estimation of boswellic acids in herbal formulations containing Boswellia serrata extract and comprehensive characterization of secondary metabolites using UPLC-Q-Tof-MS^e

Boswellia serrata is a widely used herb in Indian systems of medicine and is well known for its potential medicinal properties.A chromatographic method was developed for the analysis and quanti cation of six boswellic acid marker compounds,i.e.,keto boswellic acid(1),3-O-Acetyl 11-keto-boswellic acid(2),-b Boswellic acid(3),-Boswellic acid(4),3-O-Acetyl--boswellic acid(5)and 3-O-Acetyl--boswellic acid b(6)in commercial herbal products containing B.serrata as an ingredient.Combining UPLCbwith Q-Tof-MS/MS makes the better identi cation of secondary metabolites and adulterants in the herbal formulations containing B.serrata in rapid time using fragmentation approach than the traditional approaches.In this study quanti cation of boswellic acids with UPLC-PDA method was performed as per the pharmacopeia guidelines.Furthermore,minor phytochemical constituenBoswellia serrata is a widely used herb in Indian systems of medicine and is well known for its potential medicinal properties.A chromatographic method was developed for the analysis and quantification of six boswellic acid marker compounds,i.e.,keto boswellic acid(1),3-O-Acetyl 11-keto b-boswellic acid(2),ɑ-Boswellic acid(3),b-Boswellic acid(4),3-O-Acetyl-ɑ-boswellic acid(5)and 3-O-Acetyl-b-boswellic acid(6)in commercial herbal products containing B.serrata as an ingredient.Combining UPLC with Q-Tof-MS/MS makes the better identification of secondary metabolites and adulterants in the herbal formulations containing B.serrata in rapid time using fragmentation approach than the traditional approaches.In this study quantification of boswellic acids with UPLC-PDA method was performed as per the pharmacopeia guidelines.Furthermore,minor phytochemical constituents were identified and characterized with the help of LC-Q-Tof-MS/MS fragmentation data and various isoforms of boswellic acids and tirucallic acids in B.serrata oleo-gum-resin extract were identified.ts were identi ed and characterized with the help of LC-Q-Tof-MS/MS fragmentation data and various isoforms of boswellic acids and tirucallic acids in B.serrata oleo-gum-resin extract were identi ed.

Gum resin extract of Boswellia serrata attenuates lipopolysaccharide-induced inflammation and oxidative damage in hepatic and renal tissues of rats

Objective:To explore the effect of ethyl acetate gum resin extract of Boswellia serrata on lipopolysaccharide(LPS)induced inflammation and oxidative damage in hepatic and renal tissues of rats.Methods:The rats were divided into four groups:control,LPS,LPS+Boswellia serrata extracts(100 mg/kg and 200 mg/kg).LPS(1 mg/kg)and the extract(100 and 200 mg/kg,30 min before LPS)were administered intraperitoneally for 3 weeks.The levels of liver enzymes,albumin,total protein,creatinine,blood urea nitrogen(BUN),interleukin(IL)-6,malondialdehyde(MDA),and total thiol groups and superoxide dismutase(SOD)and catalase(CAT)activities were measured.Results:The levels of liver enzymes,creatinine,and BUN,IL-6,MDA in the LPS group were markedly increased(P<0.001)while albumin,total protein,and total thiol concentration,as well as SOD and CAT activities,were decreased compared with the control group(P<0.05 or 0.01).Boswellia serrata extracts diminished the levels of liver enzymes,creatinine,BUN,IL-6,and MDA(P<0.01 and P<0.001),and elevated the concentration of total protein and total thiol and SOD and CAT activities(P<0.05 or 0.01).Conclusions:The ethyl acetate gum resin extract of Boswellia serrata reduces LPS-induced inflammatory reactions and oxidative damage,thus ameliorating hepatic and renal function.

Boswellia resin extract and propolis derived polyphenols in patients with type III chronic prostatitis/chronic pelvic pain syndrome:An Italian prospective multicenter study

Objective:To assess the efficacy and safety of a treatment regimen based on rectal administration of Boswellia resin extract and propolis derived polyphenols in patients with type IIIa and type IIIb chronic prostatitis and chronic pelvic pain syndrome(CP/CPPS).Methods:Patients with type IIIa and type IIIb CP/CPPS received one rectal suppository a day for 15 days per month for 3 consecutive months.Participants were evaluated with National Institutes of Health-Chronic Prostatitis Symptom Index(NIH-CPSI),the International Prostate Symptom Scores(IPSS),International Index of Erectile Function(IIEF),four-glass test,uroflowmetry,and prostate-specific antigen assessments at baseline and at Week 4,and Week 12.Primary endpoints were improvement in pain domain of NIH-CPSI and improvement of NIH-CPSI total score.Secondary outcomes included improvement of micturition and quality of life(QoL)domains of NIH-CPSI questionnaire.Results:A total of 61 males were enrolled.No adverse events were reported.Significant improvements from baseline to Day 30 were reported for NIH-CPSI total score(mean difference:-9.2;p<0.01),NIH-CPSI pain domain(mean difference:-5.5;p<0.01),NIH-CPSI micturition domain,NIH-CPSI QoL domain,and IPSS total score(mean difference:-5.6;p<0.01).No significant changes from baseline in terms of IIEF score or maximum flow rate were observed.At final follow-up(Day 90),further significant improvements in terms of NIH-CPSI total score(mean difference:-12.2;p<0.01),NIH-CPSI pain domain(mean difference:-6.6;p<0.01),NIH-CPSI micturition domain,NIH-CPSI QoL domain,and IPSS total score were reported.Conclusion:Rectal administration of Boswellia resin extract and propolis derived polyphenols is well tolerated and delivers a significant symptomatic improvement in most patients with type IIIa and type IIIb CP/CPPS.

Phytochemistry and potential therapeutic actions of Boswellic acids:A mini-review

The pentacyclic triterpenic acids isolated from the oleo gum resin of various Boswellia species are collectively called as Boswellic acids(BA).The oleo gum resin obtained from Indian variety i.e.Boswellia serrata(Family – Burseraceae) is commonly known as Salai guggal.The resin fraction of Salai guggal is rich in Boswellic acids and its essential oil is composed of a mixture of mono,di and sesquiterpenes while gum fraction chiefly contains pentose and hexose sugars.This oleo-gum resin is quite popular among traditional practitioners of traditional Chinese and Indian Systems of medicine owing to their wide range of useful biological properties such as anti-inflammatory,anti-arthritic,antirheumatic,anti-diarrheal,anti-hyperlipidemic,anti-asthmatic,anti-cancer,anti-microbial anti-fungal,anti-complementary and analgesic activity,etc.It has been used as a herbal medicine since the prehistoric time to cure acute and chronic ailments including inflammatory diseases.Phytochemical investigation of this herbal medicine lead to identification of Boswellic acids which are found to be novel,potent,specific antiinflammatory agents due to non-redox inhibition of 5-lipoxygenase(5-LO) enzyme.However,the other important targets of Boswellic acids also include topoisomerases,angiogenesis,and cytochrome p450 enzymes.This review is a sincere attempt to discuss and present the current status of therapeutic potential,phytochemical as well as pharmacological profile of Boswellic acids primarily obtained from B.serrata.

总乳香酸与乳香肝毒性比较研究

目的:研究乳香和从中提取的总乳香酸对大鼠肝脏毒性作用。方法:60只Wistar大鼠随机分为对照组、乳香组、总乳香酸低、中、高剂量组。乳香组给药剂量为6g生药/kg,总乳香酸低、中、高剂量组给药剂量分别为1.5、3、6g生药/kg。连续灌胃给药4周后,检测血清AST、ALP及ALT指标和血清、肝组织中氧化应激指标MDA、SOD;进行大鼠骨髓微核试验。结果:与对照组相比,乳香组肝系数显著升高;血清ALT、MDA升高,肝组织MDA升高,SOD降低;总乳香酸组血清SOD升高,肝组织MDA、SOD降低;各给药组微核率与对照组无明显差异。结论:乳香在6g生药/kg剂量下有一定的肝毒性,总乳香酸没有明显的肝损伤;乳香及总乳香酸无明显遗传毒性。

Relief of osteoarthritis with a herbal-amino acid supplement: A randomized double-blind placebo controlled trial

A redox active medicinal plant and L-leucine mixture (HLM) was investigated in subjects with established osteoarthritis of the knee in a multi-center, rando- m-ized, placebo-controlled, double-blind clinical trial. A total of 96 subjects with osteoarthritis were enrolled and randomized to either placebo (n = 38) or HLM treatment group (n = 38). The HLM group re- ceived a combination of Uncaria tomentosa (300 mg), Boswellia serrata (200 mg), Lepidium meyenii (1000 mg) and L-Leucine (700 mg) given as 3 capsules once a day. The placebo group received matching capsules with carboxymethylcellulose. The treatment period was 8 weeks, with assessments made at days 7, 14, 28 and 56. The primary outcome was reduction in total WOMAC score. VAS pain, tolerability, investigator assessments, use of rescue medication (acetominophen), and safety assessments of vital signs and laboratory assessments were included. Subject randomization was effective for age, gender and disease severity. In the placebo group 32/38 subjects completed the trial and for HLM 35/38. WOMAC scores (pain, stiffness, physical performance and total) steadily declined over the course of the 8 week study in both groups, but the magnitude was significantly greater for HLM (P < 0.05). Total WOMAC was reduced 46.5% for HLM and 25.4 % for placebo. VAS pain was reduced 21.8% in the placebo group (p < 0.002) but the changes were significantly greater (37.8% p < 0.03) with HLM treatment. Investigator’s global assessment rating of good-excellent was 24/35 (69%) for HLM and 14/32 (44%) for placebo (P = 0.05). Rescue medication consumption and tolerability were comparable for HLM and placebo. No safety issues were evident with either group. As expected a placebo effect was observed, nevertheless HLM was clearly more effective in relieving the symptoms of osteoarthritis. This HLM represents a safe and effective new approach to the management of osteoarthritis symptoms.

乳香中5种乳香酸成分含量分析

目的：建立乳香中5种乳香酸的含量测定方法,为评价乳香质量提供依据。方法：采用HPLC测定,Agilent SB-C18色谱柱（4.6 mm×150 mm,5μm）;流动相0.1%磷酸-乙腈梯度洗脱;检测波长210,250 nm;柱温30℃。结果：12个批次乳香中α-乳香酸的质量分数为8.6816.1 mg.g-1,β-乳香酸的质量分数为53.5246.9 mg.g-1,3-乙酰-β-乳香酸的质量分数为38.4192.9 mg.g-1,11-羰基-β-乳香酸的质量分数为4.485.81 mg.g-1,11-羰基-β-乙酰乳香酸的质量分数为32.744.2 mg.g-1,5种乳香酸的总质量分数为146.1500.7 mg.g-1。结论：检测的乳香样品中5种乳香酸成分含量有一定差异。

乳香中α-蒎烯和乙酸辛酯含量测定方法研究

目的:建立乳香中α-蒎烯和乙酸辛酯含量测定方法,为制订乳香和制乳香质量标准提供参考。方法:采用气相色谱-质谱法测定,Rxi-5ms石英毛细管柱,进样口温度250℃,程序升温,起始温度50℃,保持1 min,以5℃.min-1程序升温至130℃,保持1 min。进样量1μL;分流比1∶60;载气为氦气。质谱电离方式为EI,离子源温度200℃,接口温度为250℃,电子能量70 eV,电离电压0.78 KV,扫描范围m/z 45～450。结果:以50倍量正己烷超声提取30 min;10批次乳香中α-蒎烯和乙酸辛酯的质量分数分别为0.021 3～0.149 5,2.519 6～9.098 0 mg·g-1,10批制乳香中分别为0.015 9～0.065 9和0.801 0～12.812 2 mg·g-1。结论:建立了乳香中α-蒎烯和乙酸辛酯含量测定方法,方法稳定、可靠。