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Pharmacology of an extract of Salai guggal ex-Boswellia serrata, a new non steroidal anti-inflammatory agent

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Abstract

Pharmacological evaluation of alcoholic extract of salai guggal (AESG) has been carried out in experimental animals. AESG displayed marked anti-inflammatory activity in carrageenan induced oedema in rats and mice and dextran oedema in rats. It was equally effective in adrenalectomised rats. In formaldehyde and adjuvant arthritis, AESG produced prominent anti-arthritic activity but no significant effect was observed in cotton pellet-induced granuloma test. It inhibited inflammation induced increase in serum transaminase levels and leucocyte counts but lacked any analgesic or anti-pyretic effects. The gestation period or parturition time in pregnant rats or onset time of castor oil-induced diarrhoea was unaffected by AESG and no significant effect was seen on cardiovascular, respiratory and central nervous system functions. No ulcerogenic effects were found in the rat stomach. The oral and intraperitoneal LD50 was greater than 2 g/Kg in mice and rats.

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... [18] Moreover, the CRP level elevation for disease detection in blood and urine have been established by many researchers [17,19] but biochemical biomarkers can easily be identified by their declining efficacy when the extracts of Indian medicinal plants applied topically. [13][14][15] The extracts from plants have already been used for treatment traditionally and this knowledge has implicated in medicinal usage for the prevention of several diseases after experimenting in microbes and animals and ultimately in human [20][21][22] but research works have been reported for the usage orally with plant extracts in case of osteoarthritis treatment [23][24][25][26] but phytochemicals applied tropically few research works reported. [13][14][15] Major researchers have documented CRP individually or with other parameters for only disease diagnosis [10,12,[27][28][29] but this biomarker can easily be monitored by declining impact when the combination extracts of Indian medicinal plants applied topically. ...
... [36][37] It was also observed that without pain, muscle stiffness and ability to physical function in WOMAC index scale, which is a suitable parameter to detect recovery of KOA (Bellamy et al., 1988). [38] The varieties of medicinal plants found and these plants are containing phytoconstituents that potent to cure inflammatory diseases reported by several researchers [20][21][22]31,[40][41] and major research works have been reported orally with plant extracts in case of knee osteoarthritis treatment [23][24][25][26] but normalization of KOA along with CRP level declining in serum is a first time approach in modern science by topical phytotherapeutic specialized protocol and combination of six plants extract found more effective results. In general, OA treatment is based on oral and topical medicines as pain killers, gels and finally surgery to get recovery [42][43][44][45] and till date medical practitioners are concentrating on pain relief therapy by using NSAIDs (nonsteroidal anti-inflammatory drugs), etc. but no one has been attempted before a combination of medicinal plants extract on the topical application through phytotherapy and the level of CRP within the normal range along with symmetrical anatomical features supported by radiological images for this present findings. ...
... [2] The medication is only available as NSAIDs to prevent the pain for certain period of time but inflammation unable to prevent. But few phytoconstituents have potent anti-inflammatory properties [13][14][15][23][24][25][26]31] as individual application. For the first time, the author is reporting a novel method of organic phytotherapeutic treatment technique with topical application of phytoformulation for 42 nd session, where increased levels of CRP have been brought back to within normal level. ...
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Background: Knee-osteoarthritis (KOA) is a common disease worldwide. C-reactive protein (CRP) in serum is a marker enzyme for inflammation and elevated in KOA. The present study was aiming to normalize the elevated level of CRP by topical phytotherapeutic protocol correlated with anatomical measurements, body mass index and radiological images in KOA. Materials & Methods: Baseline data from153 patients (101 females and 52 males) with KOA aged 40-70 years old were recruited in this cross-sectional study. Bilateral anatomical measurements included the gap at the knee between the short head of the biceps femoris and the surface of the bed, diameter of muscles 4cm above and below the patella and calf, and flexion and extension in supine, prone and standing positions and body mass index (BMI) were measured using appropriate instruments. The elevated level of serum CRP and pain under visual analogue scale (VAS) and WOMAC osteoarthritis index were also evaluated at the baseline and after 42 nd sessions by topically applied specialized phytotherapeutic treatment protocol. Results: All the bilateral leg anatomical measurements were symmetry at the end of the 42 nd sessions (P<0.0001). The significant changes were observed in pain under VAS (P<0.0001) and WOMAC scales (P<0.0001), CRP level (P<0.0001) and BMI (P<0.0001). The radiological features of the knee-joints were also revealed the improvement in KOA. Conclusion: The improvements of inflammation and normalization of elevated serum CRP level confirmed by anatomical measurements, BMI, VAS and WOMAC index and radiological images in KOA by topical phytotherapy. This study revealed that combinations of phytochemicals during topical application may be synergistic effect.
... Boswellia tree abundantly grows in dry hilly tracts of Gujarat and also in some parts of Madhya Pradesh states of India. This plant yields oleo-gumresin which is used for variety of therapeutic purposes [1,6,11,12,13,14,15,16,17,18,19,20]. Although the oleo-gum-resin which was a component of European Pharmacopoeia until the beginning of this century fell into oblivion with the use of synthetic drugs and still it is widely used in regions from North Africa to China. ...
... Although the oleo-gum-resin which was a component of European Pharmacopoeia until the beginning of this century fell into oblivion with the use of synthetic drugs and still it is widely used in regions from North Africa to China. Alcoholic extract of Salai guggal (AESG) has been reported to possess anti-inflammatory and anti-arthritic activities in animals [13,20] which were due to BA's. Salai guggal contains 8-9 % essential oil, 20-23 % gum, and about Fig. 1 Chemical structure of different Boswellic acids 50 % resin [21,22]. ...
... These residues were subjected to crystallization and re-crystallization in appropriate organic solvents to yield pure crystals of different boswellic acids (BAs). Various spectroscopic techniques i.e. 1 H NMR, 13 C NMR and mass spectral data were employed to identify these compounds. ...
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Background Boswellia serrata, also known as Indian frankincense is a commercially important medicinal plant which has been used for hundreds of years as an Ayurvedic medicine for the attempted treatment of arthritis. It contains naturally occurring triterpenoic acids, called as boswellic acids (BA’s). ResultsA highly reproducible High performance liquid chromatography-ultraviolet diode array detection (HPLC-UV-DAD) method was developed for the simultaneous determination and quantitative analysis of eight major triterpenoic acids in Boswellia serrata gum resin obtained by different extraction techniques. All the calibration curves exhibited good linear regression (R2 > 0.997) within the test ranges. The established method showed good precision and overall recoveries of the boswellic acids. Conclusions The eight triterpenoic acids coded as BS-1 (11-keto-beta-boswellic acid), BS-2 (3-O-acetyl-11-keto-beta-boswellic acid), BS-3 (3-keto tirucallic acid), BS-4 (3-O-acetyl-alpha-tirucallic acid), BS-5 (3-O-acetyl-beta-tirucallic acid), BS-6 (alpha-boswellic acid), BS-7 (beta-boswellic acid) and BS-8 (3-O-acetyl-beta-boswellic acid) were isolated from the processed gum resin of Boswellia serrata by column chromatography. The proposed HPLC method is simple, reliable and has been very useful for the qualitative as well as quantitative analysis of boswellic acids in the gum resin of Boswellia serrata. The proposed method allows to quantify boswellic acids in appreciable amounts by HPLC-UV (DAD) method in the extracts and the available marketed formulations.Graphical abstractIsolation & separation of eight Triterpenoic acids from Boswellia serrata
... The anti-inflammatory actions are directed toward the mucus and synovial membranes or lining tissues (respiratory tract, gut, urinary and reproductive tract). It also shows anti-bacterial and anti-fungal effect on skin and is effective against acne and retards the aging of skin [169][170][171][172][173] . Regarding spiritual practices, it offers calming effect and help meditate. ...
... Its anti-inflammatory and antiarthritic role relies on by preventing the immunomodulatory components. The most distinct is the inhibition of 5 -LOX enzyme 173 . In addition, several other factors are also inhibited, for example, cytokine productions like ILs and TNF -α, blocking the activation of complements and preventing the actions of ROS and NO [169][170][171][172][173][174] . ...
... The most distinct is the inhibition of 5 -LOX enzyme 173 . In addition, several other factors are also inhibited, for example, cytokine productions like ILs and TNF -α, blocking the activation of complements and preventing the actions of ROS and NO [169][170][171][172][173][174] . It is noteworthy that it can inhibit leucocyte elastase thereby preventing the collagen degradation usually occurred during arthritis or asthma. ...
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The article provides information regarding pharmacological and biochemical aspects of few herbs (Turmeric, Ginger, Capsicum, Devils' claw, Meadowsweet, Willow, Evening primrose, Juniper, Nettle and Boswellia) that are commonly used in treating arthritis and associated inflammations. All of them have substantialability to reduce pain and inflammation without the side effects. Distinctively, the herbs synthesize multiple phyto-chemicals that are chemically categorized as terpenes, flavins and tannins offering irrefutable impact on the patients providing significant relief. Advantageously, due to less side effects, the presence of multiple anti-inflammatory components insists patients to rely on herbs as a viable alternative in place of commercial therapeutic drugs available to control the arthritis. Many also use herbs as a supplement for additional therapeutic measure. It is proven that naturally occurring terpenes, sterols, flavins and polyphenols exert significant immune modulatory function to inhibit the inflammatory processes normally observed owing to the eruption of arthritis. So, by preventing the actions of NF-κβ and other associated factors these herbs control the arthritic problems. The co-presence of numerous ingredients in a single species often synergize the anti-inflammatory encounter while also preventing the generations of free radicals/ ROS which normally accelerate the inflammatory process. Intermittent assistance is occasionally provided by the few fatty acids within some herbs for their metabolic conversion to PGE1 or TXA1 adding additional preventive role. So less side effects along with the traditionally proven positive records ensure many to use herbs while managing the arthritic problems.
... The recorded data were analyzed using paired t-test and analysis of variance test using SPSS (IBM SPSS Statistics Gum resin of Boswellia serrata extract (BSE) has been found to possess anti-inflammatory potential with better tolerability. [9] In India, extract of BSE has been used for centuries as traditional Ayurvedic medicine for treatment of the inflammatory conditions. [10] Boswellia serrata has also shown the ability to inhibit pro-inflammatory cytokines. ...
... [19] Anti-inflammatory, antioxidant, antipyretic, antiatherosclerotic, and analgesic activity of Boswellia serrata has been described in earlier studies. [7,9,20] The symptoms of RA such as pain, stiffness, swelling, redness, and weight loss are mainly due to inflammation and immunological injury. The present study showed that BSE lessened the inflammation observed by changes in inflammatory parameters of joint-like reduction in ankle diameter, paw volume, and arthritis index. ...
... Singh and Atal also showed the anti-inflammatory effects of Boswellia serrata in carrageenan-induced rat model of inflammation. [9] Anti-inflammatory effects of BSE were further supported by our histopathological findings of the joints. BSE showed a marked reduction in cartilage disruption, fibro-osseous proliferation, pannus formation, vascular proliferation, synovial hyperplasia, vasculitis, study in which Boswellia serrata reduces cellular infiltrates in carrageenan-induced inflammation model of RA. [21] Along with other symptoms, decrease in weight also has been observed in RA. ...
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Context The worldwide prevalence of rheumatoid arthritis (RA) is about 1%, whereas in India, it is approximately 0.75%. The current therapy for RA includes nonsteroidal anti-inflammatory drugs corticosteroids, disease-modifying anti-rheumatic drugs and some recently developed biologic agents, but all of these are associated with adverse effects. Some herbal drugs, such as Boswellia serrata, have been reported to possess anti-inflammatory activity. Aims The aim of this study is to evaluate the anti-arthritic activity of Boswellia serrata extract (BSE) in complete Freund's adjuvant (CFA)-induced arthritis in rats. Materials and Methods Thirty-six Wistar rats were divided into six equal groups. RA was induced by intradermal injection of 0.1 ml CFA in hind paw. Body weight, ankle diameter, paw volume, arthritic index, tumor necrosis factor-α (TNF-α), and histopathological examination were assessed. The experimental data were statistically assessed by one-way analysis of variance (ANOVA). Statistical Analysis Used The recorded data were analyzed using paired t-test and ANOVA test using SPSS. The data were analyzed and represented as mean difference. Value of P < 0.05 was considered statistically significant. Results BSE at dose 180 mg/kg showed statistically significant improvement in body weight and decrease in ankle diameter and arthritic index (P < 0.05); however, there was insignificant change in paw volume (P = 0.056). This improvement was comparable with Indomethacin. The level of TNF-α did not show any statistically significant change (P = 0.076). Histopathological results also exhibited a reduction in inflammatory parameters. Conclusions BSE might have usefulness as an adjunct to conventional therapy of RA.
... The side effects of frankincense in humans are very rare and can be disregarded. Furthermore, no adverse interaction of frankincense with other medications has been reported [26]. Previous studies have confirmed improved memory due to the consumption of frankincense in animals [21,25,27,28]. ...
... These could decrease the nervous degeneration by affecting the brain [47]. Laboratory studies using animal models suggested that the boswellic Motor memory score is based on error acid caused inhibition of the inflammatory prefactors [26]. In other words, immunohistochemistry studies showed that patients with memory disorder had inflammation in certain areas of the brain. ...
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Background/aim: Memory is a mechanism for coding, storing, and recalling information. Weak memory and learning disability are common psychological problems in the elderly. The aim of this study was to investigate the effect of 4 weeks of frankincense consumption on explicit motor memory and serum BDNF in the elderly. Materials and methods: Twenty elderly men (mean age of 60.2 ± 1.7 years) were randomly divided into two groups: experimental (n = 12) and placebo (n = 8). The first blood samples were collected 24 h before the pretest. Then both groups participated in a 4-week exercise program based on the protocol of exercising motor memory. During this period, the experimental group received 500-mg frankincense pills two times a day. The second blood sample collection and acquisition test were conducted following the last session of the exercise program. A retention test and a third blood sampling were performed 2 weeks after the last training session. Mixed analysis of variance (2 × 3) for repeated measures was used to analyze the data. Results: Intergroup comparisons showed that frankincense had a significant effect on the acquisition and retention of explicit motor memory. No difference was observed in serum BDNF between the experimental and placebo groups. Conclusion: This study revealed that 4 weeks of frankincense consumption facilitates the acquisition and retention of motor memory in older men with moderate mental status.
... It is warm-natured, bitter in taste, with the functions of promoting circulation of blood and qi, relieving pain, and detoxifying. It is clinically mainly used for the treatment of qi and blood stagnation, abdominal pain, carbuncle sore swelling, poison, injury, dysmenorrhea, postpartum blood stasis, [3] etc., Studies have shown that frankincense mainly contains triterpenoids, which have anti-inflammatory [4] as well as analgesic, immunosuppressive, and antitumor properties. [5] Frankincense is often used in perfumes and aromatherapy, and it is sometimes used as an ingredient in skincare products. ...
... These data are hyperspectral raw data (digital number value), which have been calibrated by the device's built-in RAD and obtained by two lenses (410-990 nm and 950-2500 nm) with a spectral resolution of 6 nm. The hyperspectral image data of India level 1 (India [1]), Ethiopia level 4 (Ethiopia [4]), and Somalia level 2 (Somalia [2]) are shown in Figure 6. The average value of all ROI samples from each origin is calculated to obtain the spectral curves corresponding to the data of three origins, as shown in Figure 7. ...
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Background: As the demand for traditional Chinese medicinal materials increases in China and even the world, there is an urgent need for an effective and simple identification technology to identify the origin and quality of the latter and ensure the safety of clinical medication. Mineral element analysis and isotope finger-printing are the two commonly used techniques in traditional origin identification. Both of these techniques require the use of stoichiometric methods in the identification process. Although they have high accuracy and sensitivity, they are expensive and inefficient. In addition, near-infrared spectroscopy is a fast, nondestructive, and widely used identification technique developed in recent years, but its identification results are susceptible to samples’ states and environmental conditions, and its sensitivity is low. Hyperspectral imaging combines the advantages of imaging technology and optical technology, which can simultaneously access the image information and spectral information which reflect the external characteristics, internal physical structure, and chemical composition of the samples. Hyperspectral imaging is widely applied to agricultural product inspection, but research into its application in origin and quality identification of TCM materials is rare. Methods: In this study, the algorithm framework discriminative marginalized least squares regression (DMLSR) was used for feature extraction of frankincense hyperspectral data. The DMLSR with intraclass compactness graph and manifold regularization can efficiently learn the projective samples with higher separability and less redundant information than the original samples. Then, the discriminative collaborative representation with Tikhonov regularization (DCRT) was applied for classifying the geographical origin and level of frankincense. DCRT introduces the discriminant regularization term and incorporates SID, which is more sensitive to the spectrum as the measurement method and is more suitable for the frankincense spectral data compared with SVM. Results: For the origin classification task, samples of all levels from each origin were, respectively, selected for three‑way classification. We used 10-fold cross-validation to select a model parameter in the experiment. When obtaining the optimal parameters, we randomly selected the training set and testing set, where the training set accounts for 70% and the training set for 30%. After repeating this random process 10 times, we obtained the final average classification accuracy, which is higher than 90%, and the standard deviation fluctuation is usually small. For the level classification task, samples of each level from three origins were separately selected for multiclassification. We randomly selected the training set and testing set from each origin. The level classification results of the three origins are good on D4350 data, and the classification accuracy of each level is basically above 80%. Conclusion: Experiments and analysis show that our algorithm framework has excellent classification performance, which is stable in origin classification and has potential for generalization. In addition, the experiments show that in our algorithm framework, different classification tasks need to combine different data sources to achieve better classification and recognition, as the origin classification task uses frankincense’s D3000 data, and level classification task uses frankincense’s D4350 data.
... Pharmacological applications have recently justified the use of frankincense for its anti-tumour and anti-carcinogenic (Huang et al. 2000), anti-inflammatory (Shao et al. 1998, Safayhi et al. 2000, Krieglstein et al. 2001, anti-proliferative (Glaser et al. 1999, Hoernlein et al. 1999, anti-chronic colitis (Gupta et al. 2001) and anti-bronchial asthma (Gupta et al. 1998) effects, as well as for anti-human leukaemia HL-60 cells and the DNA, RNA and protein synthesis in HL-60 cells (Shao et al. 1998). Controlled, double-blind studies have shown that Boswellia extracts are very helpful for ulcerative colitis (Singh and Atal 1986). The antiinflammatory effects of treatment with Boswellia extract or AKBA (acetyl-11keto-β-boswellic acid) in experimental ileitis in rats are comparable to those achieved by treatments with standard drugs for inflammatory bowel disease such as prednisolone and sulfasalazine (Yamada et al. 1993). ...
... Boswellia extract was found to inhibit pro-inflammatory mediators in the body, such as leukotrienes (Singh and Atal 1986) and, in contrast to non-steroidal anti-inflammatory drugs, long-term use of Boswellia extracts does not lead to irritation or ulceration of the stomach (Gupta et al. 2001). ...
... Boswellia serrata is a branching tree found abundantly in the dry regions of India, Africa and Middle East. Traditionally resin which is available under the bark of the tree, is used in various religious and socio-cultural activities as incense and also in various therapeutic purposes [2][3] .Resin, gum, essential oils and terpenoids are the reported chemical constituents of the exudate 4 .Boswellic acid, medicinally important terpenoids makes up 25-35% of the resin [5][6][7][8][9] . Boswellic acids are pentacyclic triterpenes, which may exist in an aconfiguration (geminal methyl groups at C- 20) or a bb configuration (vicinal methyl groups at C-19/C-20). ...
... Boswellia serrata extract (BSE) has been stated to have analgesic and psychopharmacological effect from the non-phenolic extract and the alcohol extracted portion is effective in management of inflammatory conditions, arthritis and hyperlipidaemia 11 .The major effect of the BSE is attributed by two boswellic acids namely 11-keto-β-boswellic acid (KBA) and acetyl-11-keto-β-boswellic acid (AKBA). The European Pharmacopoiea 6.0 includes these two boswellic acids as markers to confirm the quality of the air-dried gum resin exudate of B. serrata 12 .Further, β-boswellic acid, 11-keto-βboswellic acid and acetyl-11-keto-β-boswellic acid have been used in apoptosis of tumor cells, specifically affected by leukemia or colon cancer 6 . ...
... 12 Guggulu has laghu ruksha guna, ushna virya, katu vipaka, and tridoshahara properties. 13 Anti-inflammatory and anti-arthritic activities of guggulu have been proven by various studies. 14,15 The contents of drug are predominantly having ushna, laghu, ruksha guna, and tikta-katu rasa, which can act by kapha chedana, ama nirharana, and agni deepana and, hence, become an ideal and effective drug in Amavata. ...
... 12 Guggulu has laghu ruksha guna, ushna virya, katu vipaka, and tridoshahara properties. 13 Anti-inflammatory and anti-arthritic activities of guggulu have been proven by various studies. 14,15 The contents of drug are predominantly having ushna, laghu, ruksha guna, and tikta-katu rasa, which can act by kapha chedana, ama nirharana, and agni deepana and, hence, become an ideal and effective drug in Amavata. ...
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ABSTRACT Introduction: Rheumatoid arthritis (RA) is a chronic, progressive, inflammatory autoimmune disease associated with articular, extra-articular, and systemic effects. Similar symptoms are found in Amavata described in Ayurveda. Simhanada Guggulu and Brihat Saindhavadi Taila are classical formulations that are used commonly in the management of Amavata. Aims and objectives: To assess the clinical efficacy and safety of the classical Ayurvedic formulations Simhanada Guggulu and Brihat Saindhavadi Taila in patients with RA. Materials and methods: A prospective, open label, multicenter study was carried out at two peripheral centers of the Central Council for Research in Ayurvedic Sciences (CCRAS). A total of 111 patients were administered Simhanada Guggulu and Brihat Saindhavadi Taila in the dose of 1.5 gm (3 tablets of 500 mg each) twice daily after food with lukewarm water and local application twice a day respectively, for a period of 12 weeks. Clinical assessment of symptoms, disease activity score-28 (DAS-28), short form 36 (SF-36), and disability index scoring were done at the baseline and at every subsequent visit at an interval of 14 days up to the 12th week and also in the follow-up without medication at the end of the 14th week. Paired sample t-test was used to compare mean change from baseline to 12th and 14th week respectively. Results: At the end of 12 weeks, statistically significant changes in symptoms, DAS 28, SF-36, and disability index score with p-value <0.001 were observed, compared with baseline. No adverse drug reaction (ADR)/adverse events (AEs) were reported during and after the trial. Conclusion: Simhanada Guggulu and Brihat Saindhavadi Taila administered together in the above-mentioned dose were found effective, safe, and tolerable in patients with RA. Keywords: Amavata, Brihat saindhavadi taila, Rheumatoid Arthritis, Simhanada Guggulu. How to cite this article: D eep V C, Sangvikar S , Sunita, Jameela S, Chaudhary S, Sharma BS, Khanduri S, Yadav B, Dua P, R ao B CS, R ana R , S inghal R , B harti, P adhi M M, Srikanth N. Clinical Evaluation of Classical Ayurvedic Formulations Simhanada Guggulu and Brihat Saindhavadi Taila in the Management of Rheumatoid Arthritis (Amavata): A Multicentric Open Label Prospective Study. J Res Ayurvedic Sci 2017;1(4):238-246. Source of support: Nil Conflict of interest: None
... The Alcoholic Extract of Salai Guggal (AESG), the oleogum resin of Boswellia serrata, has been shown to possess prominent anti-inflammatory and anti-arithritic activities [61]. Reduction of humoral antibody and development of DTH reaction to SRBC by AESG and Boswellic acids has been reported by [62]. ...
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Immunomodulation is basically a process that can alter the immune system of an organism by interfering with its functions. The current approach is to know about the medicinal plants that are biologically active and could potentially be of help in the development of modern and new immunomodulating agents. As in modern-day life, extensive exposure to industry-based pollutants/xenobiotics has resulted in the emergence of a variety of immune deficiencies or hypersensitivity situations, where immunology can play an important role. The inference results in either immune-stimulation, an enhancement of immune reactions, or immune-suppression imply mainly to reduce resistance against infection, stress which may be because of environmental or chemotherapeutic factors. Bioactive natural products provide the excellent raw material for the discovery and development of novel immune-modulatory compounds. A good number of bioactive natural products used as medicinal plants have stood the test of time, particularly for the treatment of allergic metabolic and degenerative diseases associated with aging. These bioactive natural products are believed to promote positive health and maintain organic resistance against infections by reestablishing body equilibrium and conditioning the body tissues. A large variety of natural bioactive plants mentioned in Ayurveda for their immunomodulation, adaptogenic and rejuvenating properties have been under study.
... Regarding the immune system, decreased invasion of neutrophilic granulocytes, mast cell stabilization, decreased differentiation of T-effector cells and increased differentiation of T-regulatory cells, decreased Ca 2+ mobilization in platelets, decreased infiltration of immune cells and platelets in inflamed tissues, and less leukocyte-endothelial cell adhesive interactions has been frequently observed [32,[41][42][43][44][45][46][47][48][49][50][51]. Importantly, inflammatory symptoms were relieved, including decreased edema, pleural exudates, pleurisy, ulcer formation, arthritis, pain, fever, inflammation-related bleeding, and hypersensitivity reactions [35,36,38,42,44,[52][53][54][55][56][57][58][59][60][61][62][63][64][65][66][67][68][69]. Other effects included hepatic symptoms (decreased hepatic steatosis, insulin resistance and liver enzyme release to the blood stream) [70,71] and metabolic symptoms: reduction of serum lipids and blood glucose, and less atherosclerotic plaques [71]. ...
Article
The oleogum resins of Boswellia species known as frankincense have been used for ages in traditional medicine in India, China and the Arabian world independent of its use for cultural and religious rituals in Europe. During the past two decades, scientific investigations provided mounting evidence for the therapeutic potential of frankincense. We conducted a systematic review on the anti-inflammatory and anti-cancer activities of Boswellia species and their chemical ingredients (e.g. 3-O-acetyl-11-keto-β boswellic acid, α- and β-boswellic acids, 11-keto-β-boswellic acid and other boswellic acids, lupeolic acids, incensole, cembrenes, triterpenediol, tirucallic acids, and olibanumols). Frankincense acts by multiple mechanisms, e.g. by the inhibition of leukotriene synthesis, of cyclooxygenase 1/2 and 5-lipoxygenase, of oxidative stress, and by regulation of immune cells from the innate and acquired immune systems. Furthermore, frankincense modulates signaling transduction responsible for cell cycle arrest and inhibition of proliferation, angiogenesis, invasion and metastasis. Clinical trials showed the efficacy of frankincense and its phytochemicals against osteoarthritis, multiple sclerosis, asthma, psoriasis and erythematous eczema, plaque-induced gingivitis and pain. Frankincense revealed beneficial effects towards brain tumor-related edema, but did not reduce glioma size. Even if there is no treatment effect on brain tumors itself, the management of glioma-associated edema may represent a desirable improvement. The therapeutic potential against other tumor types is still speculative. Experimental toxicology and clinical trials revealed only mild adverse side effects. More randomized clinical trials are required to estimate the full clinical potential of frankincense for cancer therapy.
... 93 This particular acid has shown significant results in several inflammatory conditions such as rheumatoid arthritis, asthma, and inflammatory bowel disease. 94,95 Several clinical studies have shown that boswellia is not only effective at treating inflammation and arthritis but also has positive effects in patient-reported outcome measures such as improvements in pain and physical function. [96][97][98][99] A systematic review by Yu et al explored the effectiveness of boswellia as an alternative form of treatment for OA. ...
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Osteoarthritis is a prevalent degenerative disease affecting a large portion of the world’s aging population. Currently, nonsteroidal anti-inflammatory drugs and acetaminophen are first-line medications for treating osteoarthritis patients’ pain. However, several studies have noted that while these medications control pain they do not halt progressive degeneration and tend to have an unfavorable side-effect profile with prolonged use. Recently, due to their more favorable side-effect profiles, herbal alternatives for controlling osteoarthritis symptoms and for alleviating the progression of the disease are being increasingly studied. Synogesic is a newly developed herbal supplement blend by renowned orthopedic surgeons and physiatrists consisting of turmeric, rutin, ginger root, vitamin C, vitamin D, and boswellia extracts. A study by Sharkey et al. has commented on the efficacy of the blend on the patients with knee osteoarthritis. So far, a review on the ingredients of the blend has not yet carried outbeen. By exploring prominent literature databases including PubMed and ScienceDirect, our aim is to write a narrative review to explore the individual ingredients of this blend and delve into their characteristics, as well as the most recent literature on their mechanism and efficacy in patients with osteoarthritis. Through this, we hope to inform clinicians and patients alike on relevant up-to-date research on the supplement and provide insight on the potential for this supplement for alleviating the disease course of patients with osteoarthritis.
... Presently most scientific interest has been attributed to 11-keto-ß-boswellic acid (KBA) and O-acetyl-11-keto-ß-boswellic acid (AKBA) (Fig. 1.) and their anti-inflammatory properties. Singh and Atal (1986) reported that an alcoholic extract from the gum resin of Boswellia serrata-called salai guggal in India-inhibited edema production induced by carrageenan injection into rat paws, an acknowledged pharmacological model to test the anti-inflammatory effects of drugs. These observations initiated various preclinical studies concerning the mechanism of the anti-inflammatory actions of boswellic extracts (BEs) and boswellic acids (BAs) as well as related clinical trials in patients with chronic inflammatory diseases with an autoimmune character. ...
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Background: Type 1 diabetes is an autoimmune disease directed to the pancreatic islets where inflammation leads to the death of insulin-producing ß cells and insulin deficiency. Type 2 diabetes, which is closely related to overweight, is characterized by insulin resistance. In both cases, proinflammatory cytokines play an important role by causing insulitis and insulin resistance. The gum resin of Boswellia species and its pharmacologically active compounds, including 11-keto-ß-boswellic acids have been shown to suppress the expression of proinflammatory cytokines in various immune-competent cells. Purpose: To review the present evidence of the therapeutic effects of boswellic extracts (BE) and/or 11-keto-ß-boswellic acids in the prevention/treatment of diabetes mellitus and to provide comprehensive insights into the underlying molecular mechanisms. Methods: This review considers all available informations from preclinical and clinical studies concerning BEs, 11-keto-ß-boswellic acids, proinflammatory cytokines and diabetes mellitus collected via electronic search (PubMed) and related publications of the author. Results: Type 1 diabetes: Studies in mice with autoimmune diabetes revealed that in the model of multiple injections of low doses of streptozotocin (MLD-STZ), an extract of the gum resin of Boswellia serrata and 11-keto-ß-boswellic acid (KBA) suppressed the increase in proinflammatory cytokines in the blood, infiltration of lymphocytes into pancreatic islets and increase in blood glucose. In a second model, i.e. the nonobese diabetic (NOD) mouse, KBA prevented the infiltration of lymphocytes into pancreatic islets. Regarding the clinical effects, a case report provided evidence that BE suppressed the blood levels of tyrosine phosphatase antibody (IA2-A), a marker for insulitis, in a patient with late-onset autoimmune diabetes of the adult (LADA). Type 2 diabetes: In a preclinical study in rats where obesity was alimentary induced, the administration of BE significantly reduced food intake, overweight, proinflammatory cytokines such as interleukin-1ß (IL-1ß), and tumor necrosis factor-α (TNF-α) and ameliorated the parameters of glucose and lipid metabolism. Similar results were obtained in a second animal study, where type 2 diabetes was induced by a combination of a high-fat/high-fructose diet and a single dose of streptozotocin. Two clinical trials with patients with type 2 diabetes receiving the resin of Boswellia serrata demonstrated improvement in the blood glucose, HbA1c and lipid parameters. Conclusion: Preclinical and clinical data suggest that BE and/or 11-keto-ß-boswellic acids by inhibiting the expression of proinflammatory cytokines from immune-competent cells, may prevent insulitis and insulin resistance in type 1 and type 2 diabetes, respectively, and therefore may be an option in the treatment/prevention of type 1 and type 2 diabetes. It is hypothesized that molecularly, BE and 11-keto-ß-boswellic acids act via interference with the IκB kinase/Nuclear Transcription Factor-κB (IKK/NF-κB) signaling pathway through inhibition of the phosphorylation activity of IKK. However, further investigations and well-designed clinical studies are required.
... [16] According to Ganguly, [16] this is a novel technique and observed first time with the help of aqueous phytoextraction as remedial measures. The aqueous extracts from plants have already been used for treatment traditionally and this knowledge has implicated in medicinal usage for the prevention of several diseases after experimenting in microbes and animals and ultimately in human body [5,[10][11]15,16] but research works have been reported for the oral usage with plant extracts in case of osteoarthritic treatment [21][22][23][24][25][26] except in the study of mice. [27] An established research work when phytochemicals applied topically, phytoconstiuents help in normalization of anatomical derangement in knee-joints supported by radiological images [16] but no one has not been reported before that CK- MM can be in a normal range after the topical application of phytoconstiuents of above-mentioned plants along with other two phytoextracts viz, 90% bowsellic acid and 20% nano- curcumin (collected from M/S Ambe Phyto Extracts Private Limited, New Delhi). ...
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Background: The knee-osteoarthritis (KOA) is a risk for muscular degeneration by the elevation of creatine kinase-muscle (CK-MM). The present study was aiming to normalize the elevated level of CK-MM by topical phytotherapeutic protocol correlated with anatomical measurements, the Kellgren-Lawrence (KL) grading systems of radiographic KOA, body mass index (BMI), overall improvement of pain under visual analogue scale (VAS) and pain, stiffness and physical function under WOMAC index. Methods: Baseline data from 108 patients (66.67 % females) with KOA aged 40-75 years old were recruited in this cross-sectional study. Bilateral anatomical measurements included the gap at the knee between the short head of the biceps femoris and the surface of the bed, diameter of muscles of thighs and calves, angles of straight leg raising, flexion and extension in different positions and BMI were measured using appropriate instruments. The elevated level of CK-MM, scored KL grading system and pain under VAS and WOMAC index were also evaluated at the baseline and after 42 days of treatment. Results: All the bilateral leg anatomical measurements were symmetry at the end of the 42 nd session (P<0.0001). The significant changes were observed in VAS (P<0.00001), WOMAC index (P<0.0001), CK-MM level (P<0.0001), BMI (P<0.0001) and improvement of KL grading scores. Conclusions: The improvements of damaged leg muscles due to muscular dystrophy, connective tissue damage etc. confirmed with normalization of elevated serum CK-MM level, above mentioned anatomical measurements, BMI, VAS, WOMAC index and KL grading systems may be synergistic effect of phytochemicals during specific phytotherapeutic treatment protocol.
... 보스웰리아는 암 (Shao et al., 1998), 염증 (Singh and Atal, 1986), 관절염 (Sharma et al., 1989), 천식 (Gupta et al., 1998), 건선 (Chopra et al., 1956), 대장염 (Gupta et al., 2001), 고지혈 증 (Pandey et al., 2005) ...
... In another study in chondrocytes, EGCG was shown to inhibit COX-2 mRNA/protein expression or prostaglandin E 2 (PGE 2 ) production via up-regulating microRNA hsa-miR-199a-3p (Rasheed, Rasheed, & Al-Shobaili, 2016). Although metabolic pathways may differ with different delivery methods (Gan, Li, Sui, & Corke, 2016), (2011) 0.1 μM after a multiple-dose administration of 786 mg of B. serrata extract Elimination half-life of nearly 6 h (Sharma, Thawani, et al., 2004) LD50: N2 g/kg (Singh & Atal, 1986) Capsaicin TRPV1 agonist Yang et al. (2015) N/A N/A Topical unknown Curcumin IL-1β, TNF-α (Z. Zhang et al., 2016). ...
Article
Arthritis is a chronic disease of joints. It is highly prevalent, particularly in the elderly, and is commonly associated with pain that interferes with quality of life. Because of its chronic nature, pharmacological approaches to pain relief and joint repair must be safe for long term use, a quality many current therapies lack. Nutraceuticals refer to compounds or materials that can function as nutrition and exert a potential therapeutic effect, including the relief of pain, such as pain related to arthritis, of which osteoarthritis (OA) is the most common form. Of interest, nutraceuticals have recently been shown to have potential in relieving OA pain in human clinical trials. Emerging evidence indicates nutraceuticals may represent promising alternatives for the relief of OA pain. In this paper, we will overview OA pain and the use of nutraceuticals in OA pain management, focusing on those that have been evaluated by clinical trials. Furthermore, we discuss the biologic and pharmacologic actions underlying the nutraceutical effects on pain relief based on the potential active ingredients identified from traditional nutraceuticals in OA pain management and their potential for drug development. The review concludes by sharing our viewpoints that future studies should prioritize elucidating the mechanisms of action of nutraceuticals in OA and developing nutraceuticals that not only relieve OA pain, but also mitigate OA pathology.
... Different medicinal plants have been found to have a hypoglycemic effect both in normal and diabetic human patients (15). Among herbal drugs, dry extract of the B. serrata gum resin have been used in traditional medicine for a variety of therapeutic purposes (16) without adverse effects or interferences with other drugs reported to date in experimental animals and humans (17,18,19). Boswellic acids, including O-acetyl-11-ketoβboswellic acid (AKBA) and 11-keto-β-boswellic acid (KBA), present in B. serrata gum resin, are novel, specific inhibitors of 5-lipoxygenase with a wide therapeutic potential (20). ...
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Diabetes mellitus (DM) is a common disorder in middle-aged to older dogs. Treatment options, similar to those for humans, include insulin injection, dietary changes and exercise. Since some diabetic dogs may develop humoral immune responses to exogenous insulin resulting in treatment failure, the use of alternative medicine could represent an interesting new therapeutic strategy for DM in addition to the traditional insulin therapy. The main objective of this report was to evaluate a new therapeutic strategy for DM, based on the association of insulin injections with an orally administered extract of Boswellia serrata to improve glycemic control in a diabetic dog. A nine year old female neutered mixed breed dog diagnosed with DM was treated with increasing doses of a porcine insulin zinc suspension starting from 0.2 U/kg up to 0.6 U/kg q 12 hours. Twenty weeks after the start of insulin therapy the duration of effect and glucose nadir were ideal and clinical symptoms had disappeared but hyperglycemia, although less severe, persisted. Supplementation with a dry extract from the gum- resin of Boswellia serrata was initiated, at a dosage of 15 mg/kg q 12 hours, to improve insulin sensitivity or possibly increasing endogenous insulin secretion. B. serrata supplementation led to good glycemic control. No side-effect or adverse reaction were observed during the study. The present case report provides the first evidence in veterinary medicine of a positive effect of dietary supplementation with boswellic acids associated with traditional insulin therapy on glycemic control in a diabetic dog. A major pitfall of the study is the lack of a control. More extensive clinical trials are required to provide definitive evidence of B. serrata efficacy.
... Boswellic acid is the active ingredient in Boswellia serrata; it has shown significant pharmacological activity in the treatment of inflammatory diseases such as rheumatoid arthritis, chronic bronchitis, asthma and chronic inflammatory bowel diseases (ulcerative colitis and Crohn's disease) [11,12]. Current research showed that 3-O-Acetyl-11-keto-beta-boswellic acid (AKBA) is the one boswellic acid with strong pharmacological activity; for example, AKBA has a powerful inhibitory effect on 5-lipoxygenase (5-LOX) [13,14]. ...
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Background: Osteoarthritis (OA) is the commonest form of inflammatory joint disease. Unfortunately, to date, there is no appropriate treatment for OA. Boswellia serrata was considered as a potent anti-inflammatory, anti-arthritic and analgesic agent that may be a drug for OA. Methods: In this meta-analysis, data from randomized controlled trials were obtained to assess the effects of Boswellia or its extract versus placebo or western medicine in patients with OA. The primary outcomes included visual analogue score (VAS), WOMAC pain, WOMAC stiffness, WOMAC function and lequesne index. Result: Seven trials involving 545 patients were included. Compared with the control group, Boswellia and its extract may relieve the pain [VAS: (WMD -8.33; 95% CI -11.19, - 5.46; P<0.00001); WOMAC pain: (WMD -14.22; 95% CI -22.34, - 6.09; P = 0. 0006)] and stiffness [WOMAC stiffness: (WMD -10.04; 95% CI -15.86, - 4.22; P = 0. 0007)], and improve the joint's function [WOMAC function: (WMD -10.75; 95% CI -15.06, - 6.43; P<0. 00001); lequesne index: (WMD -2.27; 95% CI -3.08, - 1.45; P<0. 00001)]. Conclusion: Based on current evidence, Boswellia and its extract may be an effective and safe treatment option for patient with OA, and the recommended duration of treatment with Boswellia and its extract is at least 4 weeks.
... The gum-resin of Boswellia serrata or Bfrankincense^is known for its anti-inflammatory effect in vivo [23]. Boswellic acids are the main active constituents of the oleogum-resin of the plant. ...
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Neuroinflammation is one of the most important mechanisms underlying neurodegeneration. Lipopolysaccharide (LPS) is a potent inflammogen which causes cognitive dysfunction. Boswellia serrata is known since many years as a powerful anti-inflammatory herbal drug. Its beneficial effect mainly arises from inhibition of 5-lipoxygenase (5-LO) enzyme. 3-acetyl-11-keto-β-boswellic acid (AKBA) is the most potent 5-LO inhibitor extracted from the oleo-gum-resin of Boswellia serrata. The aim of the present work is to study the molecular mechanisms underlying the anti-inflammatory and neuroprotective effects of AKBA and dexamethasone (DEX) in LPS-induced neuroinflammatory model. A single intraperitoneal (i.p.) dose of LPS (0.8 mg/kg) was injected to induce cognitive dysfunction. The LPS-treated mice were administered for 7 days with either AKBA or DEX at intraperitoneal doses of 5 and 1 mg/kg, respectively. Cognitive, locomotor functions, and anxiety level were first examined. The level of the phosphorylated inhibitory protein for NF-κB, IκB-α (P-IκB-α), was measured, and the expression levels of the inflammatory microRNA-155 (miR-155) and its target gene, suppressor of cytokine signaling-1 (SOCS-1), were determined in the brain. Moreover, the level of carbonyl proteins as a measure of oxidative stress and several cytokines as well as markers for apoptosis and amyloidogenesis was detected. Results showed that AKBA and DEX reversed the behavioral dysfunction induced by LPS. AKBA decreased P-IκB-α, miRNA-155 expression level, and carbonyl protein content. It restored normal cytokine level and increased SOCS-1 expression level. It also showed anti-apoptotic and anti-amyloidogenic effects in LPS-injected mice. These findings suggest AKBA as a therapeutic drug for alleviating the symptoms of neuroinflammatory disorders.
... *P < 0.05; **P < 0.01; ***P < 0.001. of liver function as a result of biological supplementation with B. serrata, which is consistent with observations reported in other studies. A similar effect of B. serrata extracts has been described in rat experiments (Singh and Atal, 1986), where treatment with the extracts inhibited an inflammation-induced increase in serum transaminase levels. Similarly, the results obtained by Aliyu et al. (2007) reported that the Boswellia dalzielii extract decreased AST activities in the treated groups, compared with the control. ...
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Boswellia serrata resin (BSR), exhibiting a variety of therapeutic properties, is applied in Asian traditional medicine. These properties can be used in poultry production as well. Application of the resin as a phytobiotic in broiler chicken rearing can increase the productivity and improve meat quality. However, the optimum and maximum levels of BSR in broiler diets need to be assessed. The study determined the effect of different levels of supplementation of BSR (directly derived, unprocessed) in diets for broiler chickens on the production traits, selected slaughter analysis parameters, nutrient digestibility and selected hematological, biochemical and immunological parameters. In total, 200 1-day-old broiler chickens were assigned randomly to four treatments with five replicate cages of 10 broiler chickens/cage (five females and five males). The experiment lasted 6 weeks, and the broiler chickens were fed diets containing 0% (control), 3% (BSR3), 4% (BSR4) or 5% (BSR5). In the broiler chickens receiving diets with addition of resin BSR3 and BSR4, there was an increase in ( P <0.05) BW gain, ether extract, ADF, organic matter and energy digestibility of the diets. Moreover, the best carcass quality with a high proportion of muscles and low abdominal fat content ( P <0.05) was noted in these groups. The content of uric acid ( P <0.01) and the activity of aspartate aminotransferase ( P <0.001) and alkaline phosphatase ( P <0.05) in blood plasma decreased upon the BSR supplementation. Globulin content increased in blood plasma ( P <0.05) along the increasing level of BSR. The blood immunoglobulin A concentration was only affected by the BSR treatments ( P <0.05). It may be concluded that BSR can be regarded as a safe and effective dietary additive for broiler chicken.
... The resins of Boswellia serrata have been used for the treatment of rheumatoid arthritis and other inflammatory diseases (Banno, 2006) such as Crohn's disease (Langmead, 2006) in traditional medicine of many countries. The anti-inflammatory activity has been attributing to the resin's ability in regulating immune cytokines production (Chevrier, 2005) and leukocyte infiltration (Sharma et al., 1988;Singh and Atal, 1986). Boswellia serrata extract also exhibits antibacterial and anti-fungal activities (Weckesser,2007). ...
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This work describes the in-vitro screening of anti microbial activity of frankincense of Boswellia serrata. Different concentrations (25, 50, 75 and 100 mg /ml) was evaluated for the investigation of antimicrobial efficacy using Gram positive (Bacillus subtilis, Staphylococcus aureus and Streptococcus pneumonia) and Gram negative (E.coli, Klebsiella pneumonia, Enterobacter aerogenes, Pseudomonas aeruginosa and Proteus vulgaris) microbes. Inhibition halos were evaluated and compared with antibiotic Ciprofloxacin (5μg/ml) as positive control. DMSO was used as a negative control. Results demonstrated significant antimicrobial activity. In this assay, extracts of frankincense showed antimicrobial activity comparable with standard and can be used in combating the bacterial infested diseases caused by the studied bacterial strains.
... The resinous gum of the bark is known as guggulu in Ayurveda and is also used in modern phytomedicine. It has been reported to be a powerful anti-inflammatory agent without the ulceration or irritation as observed in non-steroidal anti-inflammatory drugs [14]. Bosewellia has been shown to possess sedative, analgesic [15,16], anti-inflammatory [17,18] and anticancer [19,20,21] effects. ...
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The use of traditional medicine is expanding to newer horizons and plants still remain as the novel source of structurally important compounds that lead to the development of innovative drugs. India has about 45,000 plant species among which medicinal property has been attributed to several thousands. The traditional Indian system of medicine, the Ayurveda, mentions the use of plants in the treatment of various diseased conditions. Ethnobotanical research done in last few decades have revealed the anti-inflammatory and analgesic properties of plants cited in the traditional literature. Many herbal preparations are being prescribed as anti-inflammatory and analgesic in the traditional literature. The search for new anti-inflammatory and analgesic agents from the huge array of medicinal plant resources is intensifying. This is because such taxa may hold assurance for the discovery of novel therapeutic agents capable of suppressing, reducing or relieving pain as well as inflammation. This chapter reviews such plant species and their products that have shown experimental or clinical anti-inflammatory or analgesic activities, M. Anilkumar 268 the possible mechanism of action and their therapeutic value. Some of the important taxa which are found effective as anti-inflammatory and analgesic agents are Ananas comosus (L.) Merr. Bosewellia serrata Roxb., Callophyllum inophyllum L., Calotropis gigantea (L.) R.Br., Calotropis procera (Ak.) R.Br., Camellia sinensis (L.) Kuntz., Cannabis sativa L., Centella asiatica (L.) Urban, Curcuma longa L., Euphorbia heterophylla L., Gastrodia elata Blume, Harpagophytum procumbens (Burch.) DC, Kalanchoe crenata Andr., Mangifera indica L., Mesua ferrea L., Plumeria accuminata W.T. Aiton., Ricinus communis Linn., Salix alba L., Sida cordifolia L., Sylibium marianum L., Spillanthes acmella Murr, Tripterygium wilfordii Hook f., Uncaria tomentosa (Willd.) DC, U. guianensis, J.F.Gmel and Zingiber officinale Roscoe. These plants have shown varying degrees of anti-inflammatory and analgesic activities.
... Mikaeli et al. 2003; Hamm et al. 2005; Kumbmarawa et al. 2006; Mathe et al. 2004; Frank & Unger, 2006; Umezu et al. 2000;Sharma et al. 1988;Singh & Atal, 1986). Balsam is aromatic oleoresins and from this essential oils can be extracted by distillation process. ...
... serrata) displayed marked antiinflammatory activity in carrageenan-induced paw edema in rats and mice. It was equally effective in adrenalitemized rats [17].Alcohol extract of salaiguggul strongly inhibited antibody production and the infiltration of polymorphonuclear leukocyte; it decreased the volume of pleural exudates [18].The plant extract has antihyperlipidemic activity also [19,20]. The compound also protected mice against galactosamine / endotoxininduced hepatitis in mice [21]. ...
Article
Rheumatoid arthritis (RA) is a systemic inflammatory disorder which mainly affects the diarthrodial joint. It is very common auto immune inflammatory disease causing disability in old as well as young age group. Various drugs are useful in RA but longer term use of these drugs produce adverse effects. Because of the limitations and risks of conventional therapy, people are exploring alternative measures to treat the disease. Herbal medicine provides a foundation for various traditional medicine systems worldwide. Herbal therapies occupy a large section of alternative therapy. Herbal drugs are used single or in combination for treatment of RA.These plants are exhibiting active constituents which act by different mechanisms such as suppression of the immune system and control of inflammation to bring relief to painful conditions
... Boswellia serrata is a tree of the Burseraceae (frankincense) species that abundantly grows in India, Africa and the Middle East (Dalla Libera et al., 2014). The oleo gum resin of B. serrata has been traditionally used in folk medicine for a variety of therapeutic purposes such as headache (Dalla Libera et al., 2014), hyperlipidemia (Gerhardt et al., 2001), colitis (Gupta et al., 2001), arthritis (Sharma et al., 1989), cancer (Shao et al., 1998) and inflammation (Singh and Atal, 1986;Darshan and Doreswamy, 2004;Sferra et al., 2012). ...
Article
Oxidative stress and cell apoptosis play major roles in neuronal injury after ischemia–reperfusion (I-R) injury. Boswellia serrata is a medicinal plant with antioxidant properties. Acetyl-11-keto-β-boswellic acid (AKBA) is an active triterpenoid compound from B. serrate. In the current study, the neuroprotective effects of aqueous and ethanolic extracts of B. serrata (named ABS and EBS, respectively) and AKBA were investigated against middle cerebral artery occlusion-induced cerebral I-R injury in rats. ABS and EBS with doses of 125, 250 and 500 and AKBA with a dose of 50 mg/kg were administered (intraperitoneally) just after middle cerebral artery occlusion induction for 30 min and reperfusion for 24 h. HPLC analysis suggested that ABS and EBS had AKBA of 8.8% and 9.5% (w/w), respectively. B. serrata and AKBA significantly improved neurological deficit and reduced brain infarction, neuronal cell loss and apoptosis and also attenuated lipid peroxidation while increasing glutathione content and superoxide dismutase activity in the cerebral cortex following a stroke. Apoptosis suppression was found to be mediated through regulating caspase-3 and bax/bcl-2 expressions. In conclusion, our results demonstrated that B. serrata and AKBA attenuate oxidative damage and inhibit cell apoptosis, subsequently protecting cerebral I-R injury in rats. Copyright
... Toxicology academic works of B. serrata resin directed on animals showed no notable histopathological, genotoxic, and hematological changes after consumption of this resin at doses up to 1000 mg/kg. Furthermore, the adverse effects are insignificant in humans, and occasionally nausea, acid reflux and digestive complaints have been reported in some consumers (16,17). Based on the above mentioned information, the current study was conducted to evaluate neuroprotective effects of B. serrata extract on the neuronal tissues in experimental SCI in rat model. ...
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Introduction: The severe inflammatory responses that occurs after traumatic spinal cord injury (SCI) is with great strength related to the further tissue damage. As such, developmental strategies have been investigated, aimed at restricting inflammation and encouraging regeneration of injured neural tissue. One of those encouraging strategies is administration of traditional medicinal plants. The current study was conducted to evaluate the neuroprotective effects of Boswellia serrata extract on the neuronal tissue inflammation and white blood cells (WBCs) responses in rats with SCI. Methods: Forty adult female rats were randomly assigned into 2 equal groups as experimental and control groups. Under general inhalation anesthesia, in both groups, SCI was created, at T9-10 level of the column. On the third day after the operation, an oral supplement of B. serrata extract was administered to the experimental group at 100 mg/kg/d. The histology of the site of injury and changes in the WBCs were examined in both groups at different pre-surgical and post-surgical times. Results: The total population of WBCs in the current study was significantly less in the experimental group, compared to the control group at third and fourth weeks of the study which could be related to the anti-inflammatory effects of B. serrata extract. Histopathological evaluation of lesion sites confirmed the reduced inflammatory responses in the experimental group compared to the control group (P < 0.05). Conclusion: The decrease in the number of inflammatory cells after oral consumption of B. serrata extract and the histopathological results confirm the neuroprotective effects of this extract.
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Introduction: Lumber slipped disc (LSD) attributes to a problem with an intervertebral disc of the lumber spine, whereby a gel-like material (nucleus-pulposus) inside the disc that protrudes through a crack in the outer-wall (annulus-fibrosus) of the disc and compressed a nearby nerve root causes inflammation, pain, numbness or weakness in the leg that lead to abnormal quality of life. The aim of the study is to normalize the LSD with the aberrant levels of Interleukin-10 (IL-10), Tumor necrosis factor-alpha (TNF-α), Creatine kinase-muscle (CK-MM) and AldolaseA (AldoA)along with anomalous anatomical and international acclaimed functional disability parameters and radiological images by topical phytotherapeutic treatment protocol within six-week. Methods: Baseline data were collected and evaluated from 108 patients, aged 58.60±9.94 years, suffering with LSD for 4.68±2.22years. Serum IL-10, TNF-α, CK-MM and AldoA levels were measured for all the patients at the baseline and post-treatment using appropriate kits. All patients underwent standardized physical, radiographic examinations, and completed a questionnaire. Results: The abnormal levels of above-mentioned biomarkers during LSD were recorded as their mean±SD values, 16.06±1.98pg/ml, 12.54±0.95pg/ml,106.89±30.06U/L, and 5.28±1.13U/L respectively at post-treatment and all were highly significant(p<0.0001). The improvements on deranged anatomical features, international-approved functional disability parameters and reduction of overweight under VAS, KPS, LEFS, ODI, and BMI were all highly significant(p<0.0001) and radiological images under KL scale at post-treatment when compared to the baseline. Conclusions: It is firmly concluded that LSD resulted in the anomalous levels of above-mentioned biomarkers along with the aforesaid aberrant parameters can be successfully normalized by topical phytotherapeutic treatment protocol within six-week.
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الحمد لله رب العالمين والصلاة والسلام على محمد سيد الأنبياء والمرسلين وعلى آله الطيبين الطاهرين وصحبه الغر الميامين وأمته المؤمنين. لقد أشار الكثير من الباحثين الى أن البشرية قد تعلمت الطب بطرق شتى فمنهم من يقول انه قياس ومنهم من يقول انه تجربة، ومنهم من يقول انه الهامات ومناجاة وحدس صائب ومنهم من يقول أن البشرية قد حاكت البهيمة والحيوان، وأي كان طريق اخذ الطب فانه لايرتقي علماً وممارسة الى الطب الذي اخذ بالوحي والذي لاتصل إليه علوم الناس وتجاربهم وأقيستهم. ولم يعرف التاريخ غير محمد (ص) رجلاً افرغ الله وجوده في الوجود الإنساني كله، لقد علمه الله ما لم يكن يعلم فكان المرآة الساطعة التي انعكست على صفحتها أوامر الله سبحانه وتعالى ونواهيه. (وانزل الله عليك الكتاب والحكمة، وعلمك ما لم تكن تعلم، وكان فضل الله عليك عظيماً) (النساء 113) (وما أرسلناك إلا رحمة للعالمين) (الأنبياء 107). وكان رسول الله (ص) قد شرع التداوي وكان يستعمله في نفسه ويأمر به غيره وقد ثبت ان رسول الله (ص) كان يديم التطبيب في حال صحته ومرضه ومن الجدير بالذكر انه لم يكن من هدي الرسول (ص) استخدام الأدوية المركبة وكان جل الطب النبوي يعتمد على استخدام الأدوية المفردة وهذا ما مال إليه الطب الحديث اليوم تلافياً من حدوث التضاربات الدوائية. وكان الرسول (ص) يراعي صفات الأطعمة وطبائعها ويراعي استعمالها على قاعدة الطب الغذائي وكان يعدل الغذاء بالغذاء فلا يمزج غذائين يرتفع مستوى محتواهما من عنصر غذائي واحد ويخلوان من عنصر آخر بل كان يجمع من الأغذية ما يمنحهما الجمع تكاملاً غذائياً. وقد استخدم الرسول (ص) الدواء بطرق إعطاء شتى، عن طريق الفم ودهناً وغسولاً وحقنةً وحجامةً وكيَا، ولكنه كان لايحب ان يكتوي. وقد أرسى الرسول (ص) أسس الأخلاق الطبية في ممارسة الطب فقد أخرج أبو داود والنسائي وابن ماجة حديث عمرو بن شعيب عن أبيه عن جده قال: قال رسول الله (ص) (من تطبب ولم يكن بالطب معروفاً فأصاب نفساً فما دونها فهو ضامن) وإذ يقسم الطب النبوي الى طب علاجي وطب وقائي وطب غذائي، فان الطب النبوي طباً مرتبطاً بالإيمان والأخلاقيات السماوية، فقد أعار الطب النبوي الجوانب الروحية والأخلاقية حصة كبيرة مع انه ليس محصوراً فيها. ولضرورة هذا الجانب ولسوء استخدام الطب وكثرة الأمراض النفسية والجسمانية من جانب آخر فان الكثير من المختصين اليوم يدعون لمزج التعاليم الإسلامية بالطب الحديث لخلق خليطا متفرداً من الفن العلاجي. وفي هذا الكتاب جمعنا الاحاديث النبوية الطبية ثم استعرضنا البحوث الطبية والدوائية التي استقصت واوضحت الفعاليات الدوائية للعلاجات النبوية وتركنا للقارئ متعة المقارنة لادراك الاعجاز في الطب النبوي.
Article
There is considerable evidence that nutraceuticals from natural herbs may play a significant role in inflammation and joint destruction in OA. These supplements have been found to be effective in knee OA in various studies. No serious side effects have been reported for any of these supplements. Overall, our study identifies and support the use of these nutraceuticals to provide symptomatic relief to patients with knee OA and justify their use as an adjunct therapy for the management. More good quality trials are needed to provide definitive answers to questions related to their efficacy and safety for OA prevention and treatment.
Chapter
Pharmacokinetics: Whereas KBA is absorbed reaching blood levels being close to in vitro IC50, AKBA which is more active in in vitro studies than KBA, but undergoes much less absorption than KBA. However, absorption of both is increased more than twice when taken together with a high-fat meal.Clinical Studies There are a variety of chronic inflammatory diseases which respond to treatment with extracts from the resin of Boswellia species. Though, the number of cases is small in related clinical studies, their results are convincing and supported by the preclinical data. These studies include rheumatoid arthritis, osteoarthritis, chronic colitis, ulcerative colitis, collagenous colitis, Crohn's disease and bronchial asthma. It can not be expected that there is cure from these diseases but at least improvement of symptoms in about 60-70 % of the cases. Side Effects The number and severity of side effects is extremely low. The most reported complaints are gastrointestinal symptoms. Allergic reactions are rare. And most authors report, that treatment with BEs is well tolerated and the registered side effects in BE- and placebo groups are similar.
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Background: Laboratory Studies show that Olibanum boosts the process of learning and memory. Alzheimer' disease is one of the important cognitive abnormalities which affect memory. Moreover, increased expression of amyloid precursor protein (A pp) results in Alzheimer' disease. This study aimed to compare the effects of Olib-anum aqueous extract and rivastigmin on the expression of A pp gene in rats that are treated by AlCl 3 .
Article
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Background: Knee-osteoarthritis (KOA) is a degenerative joint disease. Elevated level of aldolase-A (AldoA) in serum indicates skeletal muscle damage in KOA. The present study was attempted to normalize the elevated level of AldoA by topical phytotherapeutic protocol correlated with leg-anatomy, body mass index (BMI), pain, stiffness and physical function and the Kellgren-Lawrence (KL) grading-systems. Methods: Baseline data from144 patients (61.80% females) with KOA aged 40-75 years old were recruited in this cross-sectional study. Bilateral anatomy of legs including the gap at the knee between the short head of the biceps femoris and the surface of the bed, diameter of muscles 4cm above and below the patella, angles of straight leg raising, flexion and extension in different positions and BMI were measured using appropriate instruments. AldoA was estimated in serum. The KL grading-system of radiographic KOA and overall pain under VAS and pain, stiffness and physical function under WOMAC index were also evaluated. All the parameters were compared between the baseline and post-42 days of treatment. Results: The anatomical features were observed symmetry in both legs at the end of the 42 nd session with highly statistical significance (P<0.0001). The significant changes were also observed in VAS (P<0.00001), WOMAC index (P<0.001), AldoA level (P<0.0001), BMI (P<0.0001) and improvement of KL grading systems was noted for both knee-joints. Conclusion: The functional improvements of skeletal muscles confirmed with normalization of elevated AldoA level, leg-anatomical measurements, BMI, VAS, WOMAC index and KL grading systems of radiographic KOA due to the effects of phytochemicals present in phytoextracts.
Article
Ethnopharmacological relevance Rheumatoid arthritis is one of the most common disabling chronic progressive autoimmune diseases affecting the adult world population. Boswellia serrata has been a known anti-inflammatory agent since ancient times. Therefore, research on Boswellia extract based on Acetyl Keto Boswellic Acid (AKBA) content evaluating its efficacy and safety is necessary. The study aimed to find a suitable Boswellia extract rich in AKBA to evaluate its bioavailability, anti-inflammatory, and anti-arthritic effect. In addition, the synergistic action of AKBA extract with methotrexate (MTX) was also assessed on an animal model. Materials and methods Oral bioavailability of AKBA and the anti-inflammatory activity of 10% AKBA (5, 10, 20, 40 mg/kg b.w) was assessed and compared with 2% AKBA (40 mg/kg) and diclofenac (10 mg/kg). The effect of 10% AKBA at 20 mg/kg and 40 mg/kg was evaluated in the FCA induced arthritis animal model alone and combined with methotrexate (MTX) at 2 mg/kg b.w. Subplantar injection of FCA produced edema within a few hours with progressive arthritis by the 9th day after injection. All the treatments were initiated from the 10th day until the 45th day. Oral administration of 10% AKBA was done daily and MTX by intraperitoneal route once a week from day 10 to day 45. Paw volume, erythrocyte sedimentation rate (ESR), serum glutamic oxaloacetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT), alkaline phosphatase (ALP), total bilirubin, oxidative markers (superoxide dismutase (SOD) levels, malondialdehyde (MDA), total proteins and liver histopathology were examined. Results 10% AKBA provided 8.48-fold, 24.22-fold, 47.36-fold, and 110.53-fold higher AUC (0-α) of AKBA at 5 mg/kg, 10 mg/kg, 20 mg/kg and 40 mg/kg, respectively compared to 2% AKBA at 40 mg/kg. Percentage paw edema inhibition of 10% AKBA at 20 mg/kg and 40 mg/kg were significantly higher than 2% regular AKBA (40 mg/kg) and diclofenac (10 mg/kg). 10% AKBA at a dose of 20 and 40 mg/kg significantly reduced ESR compared with FCA treated group. A combination of methotrexate with 10% AKBA showed the highest reduction in ESR. 10% AKBA at both dose levels significantly reduced hepatic marker enzymes and total bilirubin levels. Treatment with 10% AKBA showed a significant increase in total proteins, antioxidant enzymes and a decrease in malondialdehyde levels. Similarly, 10% AKBA protected the hepatocytes compared with the FCA and FCA + MTX treated group. 10% AKBA was capable of significantly minimizing FCA and FCA + MTX induced changes. Conclusion Anti-inflammatory activity of AKBA due to inhibition of lipoxygenase (LOX) enzymes supports the use of AKBA in inflammatory disorders. Combination therapy of 10% AKBA with MTX is effective in inhibiting arthritis and circumventing hepatotoxicity produced by MTX in arthritic animals.
Article
Mold growth is among the major causes of health impairment of cereals, in particular durum wheat ( Triticum durum ) for the synthesis of mycotoxins such as aflatoxins B1 and ochratoxin A (OTA), originally from poisoning in the consumer. In this context, the objectives of this work is the search and characterization of fungal strains Producers mycotoxins such as Aspergillus, Penicillium in semolina and their derivatives (traditional and industrial couscous) and detect and quantify total aflatoxins, aflatoxins B1 and ochratoxin mycotoxicologique to assess the risk associated with the consumption of these foods. In this regard, our work focuses on mycological and mycotoxicologique study of semolina and couscous deemed most commercialized in the town of Bechar-Algeria after a socio-economic survey. The mycological study testifies the high degree of pollution of our samples by Aspergillus , Penicillium . The expertise of genera reveals the high degree of invasion of our samples by Aspergillus , Penicillium . The examination of fungal procession characterizing our samples shows a very high index of distribution, or of fidelity of Penicillium 43.75% of our sample and 28.38% Aspergillus . The presence of these species is evidence that our samples have been abused, but especially poorly stored; should be noted the involvement of the genera Alternaria 7.10%, Fusarium 13.70%. Thin-layer chromatographic (TLC) analysis revealed that 50% of Aspergillus flavus-parasiticus strains were aflatoxin G-producing and aflatoxin B-free in our samples. Of the Aspergillus ochraceus strains 50% were OTA producers. The presumption of toxicity of the various samples appeared positive on TLC. The test of Elisa has confirmed the presence of the OTA in our samples, the analysis of its results shows that the majority of the rates of OTA taken on our analyzed samples follow the European standard, these rates are between 1.01 and 1.9, except for one sample (couscous) which has shown a rate much higher than the standard recommended by the regulation (> 100 ppb), the samples of semolina had a rate of OTA lower than the beginning of the detection (1 ppb). The results of the presence of AFB spread out between 4.93 ppb and > 40 ppb. The antifungal activity of the resin of Boswellia carterii was tested on the following strains: Aspergillus niger , Aspergillus flavus, Penicillium expansum . And kneaded according to the technique of diagonal growth on intermediate solid medium (PDA). The results showed that the yield of the aqueous extract varied between 96.2 and 99.8%. The results of the extracts also showed activity against the fungi studied 48.6% and 96.2%.
Book
Inflammation and Natural Products brings together research in the area of the natural products and their anti-inflammatory action in medical, nutraceutical and food products, addressing specific chronic inflammatory diseases like cancer and the mechanistic aspects of the mode of action of some key natural products. Inflammation is a complicated process, driven by infection or injury or genetic changes, which results in triggering signalling cascades, activation of transcription factors, gene expression, increased levels of inflammatory enzymes, and release of various oxidants and pro-inflammatory molecules in inflammatory cells. Excessive oxidants and inflammatory mediators have a harmful effect on normal tissue, including toxicity, loss of barrier function, abnormal cell proliferation, inhibiting normal function of tissues and organs and finally leading to systemic disorders. The emerging development of natural product formulations utilizing the unique anti-inflammatory compounds such as polyphenols, polysaccharides, terpenes, fatty acids, proteins and several other bioactive components has shown notable successes. Inflammation and Natural Products: Recent Development and Current Status provides a comprehensive resource, ranging from detailed explanation on inflammation to molecular docking strategies for naturally occurring compounds with anti-inflammatory activity. It is useful for graduate students, academic and professionals in the fields of pharmaceutical and medical sciences and specialists from natural product-related industries.
Chapter
In the present chapter the antiinflammatory and antiarthritic effects of extracts, fractions, and/or isolated compounds from several medicinal plants is reviewed, including Boswellia serrata Roxb. (Shallaki), Curcuma longa Linn. (turmeric), Cinnamomum zeylanicum Blume (cinnamon), Echinodorus grandiflorus (Cham. & Schltdl.) Micheli. (Chapéu-de-couro), Colchicum luteum Baker (Suranjan-Talkh), Tripterygium wilfordii Hook F. (Thunder God Vine), Andrographis paniculata (Burm. fil.) Nees (creat or green chiretta), and Nigella sativa L. (black caraway). The revision covers the in vitro and in vivo preclinical data reported to date for the aforementioned species, in addition to clinical trials, antiinflammatory mechanisms of action, and toxicological studies, when available.
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This Reference e-Book contain 11 Chapters with an attempt to summarize the current knowledge of promising ethnomedicines and their phytophores, to compounds tested against diverse diseases. The therapeutic properties and structure activity relationship (SAR) of some important and potentially useful ethnomedicines is addressed with a focus on how these ethnic knowledge can led to the development of useful therapeutic lead for preclinical or clinical evaluation. In general it is a snapshot of different areas of research on the role of phytochemicals in health, comprehensively presented and is useful of tidbits of knowledge or ideas for research, covering the ethnomedicines uses in the management of several diseases, particularly, infectious diseases (like viral, bacterial and fungal) and lifestyle related disorders mostly validated by modern scientific methods. In depth information prepared by experts all over the globe traces the evolution of herbal drugs with civilization and their use as antiviral, antibacterial, antifungal, antiparasitic, antioxidants, anticancerous, chemopreventors, memory enhancers, neuroprotective, immunomodulator, laxatives, analgesic and anti-inflammatory disorders, along with safety issues and toxic effects.
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Full-text available
A vast majority of the world’s population lacks access to essential medicines and the provision of safe healthcare services. Medicinal plants and herbal medicines can be applied for pharmacognosy, or the discovery of new drugs, or as an aid for plant physiology studies. In recent years, there has been increased interest in the search for new chemical entities and the expression of resistance of many drugs available in the market has led to a shift in paradigm towards medicinal research. Herbal treatments, the most popular form of folk medicine, may become an important way of increasing access to healthcare services. Advanced Pharmacological Uses of Medicinal Plants and Natural Products provides emerging research exploring the theoretical and practical aspects of drug discovery from natural sources that allow for the effective treatment of human health problems without any side effects, toxicity, or drug resistance. Featuring coverage on a broad range of topics such as ethnobotany, therapeutic applications, and bioactive compounds, this book is ideally designed for pharmacologists, scientists, ethnobotanists, botanists, health researchers, professors, industry professionals, and health students in fields that include pharmaceutical drug development and discovery.
Chapter
Traditionally, the gum resin produced from the Boswellia serrata plant has been used in as a therapeutical compound. The gum that contains a chemical known as boswellic acid, AKBA (3-O-acetyl-11 keto-β-boswellic acid), and widely in ayurvedic medicines. This is used to treat the disease like reduction in various inflammatory conditions of the skin, eye, as well as respiratory disorders such as asthma, bronchitis, and laryngitis. The boswellic acids were also found capable to inhibit both hemolysis and chemotaxis of leukocytes and were shown to work by inhibiting C3-convertase, a key enzyme of the classical complementary pathway. In addition to this, the compound shows beneficial effects in various pharmacological properties like immunomodulation activity, polyarthritis, activity against Hepatitis C-virus and other harmful microbes, Colitis and Crohn's disease, and so on. The boswellic acid is also used to treat patients with memory disorders. In this chapter, the chemical nature and isolation of boswellic acid and its therapeutic importance have been highlighted.
Article
Background: Osteoarthritis (OA) is a joint disease involving articular cartilage degeneration causing patients pain, joint stiffness, physical disability, and significantly reducing their quality of life (QoL). Purpose: The aim of this study was to assess whether the daily consumption of a gastroresistant food supplement formulation containing a combination of Boswellia serrata and bromelain could improve the QoL of patients suffering from various forms of OA. Materials and Methods: Forty-nine patients were enrolled in this pilot study conducted from June 2015 to October 2016. Patients took a Boswellia- and bromelain-based supplement for a period between 1 and 6 months. At baseline and at the end of the study, patients completed a self-assessment QoL questionnaire regarding their independence in performing daily activities. QoL scores were compared between baseline and follow-up by means of the Wilcoxon signed-rank test in all patients and in the subgroups of patients with knee, hip, or generalized OA. Results: Forty-nine patients, 6 men and 43 women, aged between 23 and 92 years, (mean age 63.24) participated in the study. At follow-up (3.0 ± 0.7 months), a significant improvement was observed for 7 of 10 QoL questions and, overall, for the total QoL score. The most significant improvements were observed in the joints that were more strongly affected at baseline. A similar trend was observed when separately considering patients with knee, hip, or generalized OA. No patients experienced adverse events and no drug interactions were reported. Conclusions: From this pilot study, it emerges that the use of the gastroresistant formulation containing the combination of Boswellia and bromelain supplements can represent a valuable nonpharmacological tool for improving the QoL of patients suffering from different forms of OA. Further studies should be conducted to confirm this first evidence.
Chapter
The gum resin from Boswellia serrata (Indian frankincense) has a long history of various medicinal applications and has been appreciated for millennia. Recently, the pharmacological properties and clinical effectiveness of Boswellia serrata have been studied systematically. In particular, B. serrata has been used traditionally against inflammatory diseases. Its main pharmacologically active ingredients are β-boswellic acids with anti-inflammatory properties. Among the members of β-boswellic acid family, 3-O-acetyl-11-keto-β-boswellic acid (AKBA) has been demonstrated as the most active ingredient with anti-5-lipooxygenase activity, which is mainly responsible for Boswellia serrata's anti-inflammatory properties. This chapter describes molecular insight of anti-inflammatory properties of an AKBA enriched extract of B. serrata (5-LOXIN) and its clinical efficacy in management of osteoarthritis. A series of in vitro and in vivo experiments including GeneChip Microarray study reveal that 5-LOXIN modulates several key pro-inflammatory cytokines/chemokines. A double-blind placebo controlled clinical study conducted on subjects with knee osteoarthritis (OA) demonstrates that oral supplementation of 5-LOXIN significantly helps in relieving the clinical symptoms of OA and also decreases cartilage destruction by reducing matrix metalloproteinase-3 (MMP-3) production in synovial membrane of OA subjects. Together, a battery of safety studies and clinical studies demonstrate that oral supplementation of this AKBA enriched extract of B. serrata gum resin (5-LOXIN) is safe and tolerable for clinical applications. Furthermore, a proprietary composition (Aflapin) has been developed recently, which contains B. serrata extract with at least 30% AKBA and B. serrata non-volatile oil. In vitro and in vivo experiments suggest that this advanced composition significantly enhances the anti-inflammatory efficacies by improving the bioavailability of AKBA. In addition, randomized double blinded placebo controlled clinical studies have demonstrated that Aflapin provides a prompt and significant improvement in pain relief, physical ability and quality of life in OA subjects.
Article
Cell migration is a cardinal feature of the inflammatory response. This phenomenon is characterised by emigration of leucocytes from small blood vessels and their accumulation in inflamed or injured tissues. The early morphological event is the movement of leucocytes from the center to the periphery of the bloodstream, followed by the adhesion of the cells to the luminal surface of the vascular endothelium, especially of the postcapillary venules.
Chapter
This review is mainly concerned with the mechanism of action of those non-steroid anti-inflammatory drugs used to ameliorate the signs and symptoms of human acute and chronic inflammation which have the common property of inhibiting fatty acid oxidative cyclization, in particular the formation of prostaglandins (PGs) and throm-boxanes. We have retained for this group of substances the term PG synthetase inhibitors because thromboxane synthetase can be selectively inhibited by substances which do not affect PG synthesis and do not show anti-inflammatory activity (Moncada et al., 1976). Other types of non-steroid anti-inflammatory agents are reviewed in subsequent chapters.
Article
Twenty-one 3-aryloxy or 3-alkoxy-2-hydroxy-n-propyl derivatives of norpethidine were tested subcutaneously for analgesic activity in mice. Many of them are more potent than pethidine. The 2-hydroxy-3-phenoxypropyl derivative (B.D.H. 200) is at least three times more active than morphine and ten times more active than pethidine in this species with a therapeutic index slightly better than morphine and very much better than pethidine. The duration of analgesia is similar to morphine and pethidine and it is less constipating than pethidine. Its effects on respiration and the cardiovascular systems are counteracted by nalorphine. The decrease in activity after oral administration is probably due to a more rapid metabolic breakdown than poor absorption, as this decrease in activity can be modified by pretreatment with iproniazid and BAL while subcutaneous administration is unaffected.
Article
Benoxaprofen is a potent and long-acting anti-inflammatory and antipyretic compound. Its anti-inflammatory activity has been demonstrated in carrageenan-induced oedema, in cellulose pellet granuloma and in both developing and established adjuvant arthritis tests in rats. Its antipyretic activity is greater than either aspirin or paracetamol in tests inducing pyrexia with yeast of 'E' pyrogen in rats and rabbits. Benoxaprofen has analgesic activity in tests where pain is accompanied by inflammation but not in other experimental models of pain. The weak prostaglandin synthetase inhibiting properties of this compound differentiate it from other acid anti-inflammatory compounds. The low ulcerogenic potential of benoxaprofen seen in animal models may be related to its relative inability to inhibit PG synthetase.
Article
Forty-four non-steroidal anti-inflammatory compounds were tested for possible effects on castor oil-induced diarrhoea in rats. A small but significant delay of intestinal evacuations was found with all compounds. Quantitatively, the oral doses required to delay diarrhoea beyond the first hour after castor oil challenge reflected the acute anti-inflammatory potency of the tested compounds. Qualitatively, the evolution of the effective doses with increasing delay was linear for potent inhibitors of prostaglandin biosynthesis. The evolution for less potent compounds was markedly different and suggested the earlier occurrence of non-specific drug effects. Suprofen, the most potent of the series of compounds, produced the 1 h delay at an oral dose of 1.11 mg kg-1; the ED50 increased linearly to 115 mg kg-1 for a 4 h delay. Compared with other compounds the activity pattern of suprofen was consistent with that of a very potent, short-acting inhibitor of prostaglandin biosynthesis, which maintains its specific action over a wide dose range. It is concluded that delay of castor oil-induced diarrhoea in rats allows a detailed characterization of aspirin-like compounds, and that inhibition of prostaglandin biosynthesis is insufficient to suppress the intestinal effects of the oil.
Article
The tranquillising activity of 3-[gamma-(p-fluorobenzoyl)propyl]-2,3,4,4a,5,6-hexahydro-1-(H)-pyrazino [1, 2-a]quinoline hydrochloride (centpyraquin), a new adrenergic neurone blocking antihypertensive agent, has been evaluated in various laboratory animals. The compound has a calming effect in mice, rats, cats and monkeys. In low doses it reduces the spontaneous motor activity followed in progressively higher doses by hypothermia, ptosis and catalepsy and a taming effect in monkeys and cats. It potentiates pentobarbitone-, hexobarbitone- and ethanol-induced sleep and antagonises amphetamine induced toxicity in mice. It, however, fails to antagonise morphine induced mania and hyperactivity in cats. It blocks conditioned avoidance response in rats at a much lower dose (ED50 = 2.73 mg/kg) than the unconditioned response (ED50 = 10,9 mg/kg). In cats centpyraquin increases the voltage and slows the frequency of cortical EEG discharges. Centpyraquin has the profile of activity of a neuroleptic on the central nervous system.
Article
3-[gamma-(p-Fluorobenzoyl)propyl]-2,3,4,4a,5,6-hexahydro-1-(H)-pyrazinol(1,2-a)quinoline (compound 69/183, centpyraquin) has been found to possess promising hypotensive activity in anaesthetised cat, dog and monkey- It also lowers the blood pressure of unanaesthetised cat, dog and hypertensive rat. The effective doses are between 0.5 to 2.0 mg/kg in all the species except rat, in which doses of 10.0 and 20.0 mg/kg are effective. The compound potentiates epinephrine and norepinephrine pressor responses but inhibits carotid occlusion, tyramine and DMPP induced pressor responses. The contraction of the nictitating membrane due to pre- as well as post-ganglionic sympathetic nerve stimulation is blocked equally. In mice the compound produces ptosis which is antagonised by N-benzyl-N-methylguanidine. Localisation of the compound either to the superior cervical ganglion of cat or to the central cardiovascular loci has no effect on the activities of either of them. No evidence of an initial catecholamine release by the compound could be obtained. It has weak smooth muscle relaxant activity. The mechanism of hypotensive action seems to be the blockade of adrenergic neurones along with direct smooth muscle relaxation.
A concise and general discussion of experimental evidence implicating endogenous prostaglandins (Pg) as indicators of uterine contraction, with emphasis upon effects of aspirin like drugs. Uterus postulated as source of plasma Pg, emphasizing that Pg produced by uterus sensitize the tissue to action of other local or circulating hormones by enhancement or by potentiation. Pregnant uterus source of much prostaglandins. Release increased steadily from day 17 and at day 22 of pregnancy to a dramatic increase prior to delivery, with subsequent decline post partum. Prostaglandin capacity of pregnant rat uterus observed to reside exclusively in endometrium. Aspirin, papaverine or aspirin like drugs reduced spontaneous uterine activity in vitro and ingestion of either Aspirin, Indometacin or Fenclozic acid delayed onset of parturition, linking inhibitory action to prostaglandin synthesis. (Hansard - Knoxville, Tenn.)
This study compares the affects of a new non-steroidal anti-inflammatory drug, d,l-6-chloro-alpha-methyl-carbazole-2-acetic acid, its enantiomers, and indomethacin on platelet aggregation, prostaglandin synthetase, adjuvant arthritis, gastric ulceration and arachidonic acid induced diarrhea. In the adjuvant arthritic rat, doses producing anti-inflammatory activity were similar for all compounds with the exception of the l-isomer which was much less active. On the other hand, indomethacin was 10 to 25 times more potent with regard to inhibition of platelet aggregation, inhibition on prostaglandin synthetase, inhibition of arachidonic acid induced diarrhea, and induction of gastric ulceration than the racemate and its isomers. Such divergence of potencies suggests that the racemate, unlike indomethacin, would have no affect on platelet aggregation and, hence, produce no prolongation of bleeding time at doses possessing anti-inflammatory activity. The data also suggest that the racemate and d-isomer have greater specificity toward anti-arthritic acitvity and are less ulcerogenic than indomethacin. The d-isomer apparently is the more active component of the racemate in all the systems tested since: (a) the d-isomer has 2 to 3 times the inhibitory potency of the racemate and (b) the l-isomer, at high dosages or high concentrations had considerable less affect. Comparison of potencies relative to inhibition of platelet aggregation and of prostaglandin synthetase, are quite close; therefore, mechanistically, the anti-aggregatory affects of these drugs, or lack thereof, may be related to inhibition of prostaglandin synthetase.
Article
Increase of stillbirths and adverse maternal effects in rats after administration of aspirin and indomethacin in the final days of pregnancy warns against their use in the late stages of human pregnancy.
Article
Experiments with guinea-pig lung suggest that some of the therapeutic effects of sodium salicylate and aspirin-like drugs are due to inhibition of the synthesis of prostaglandins.
Article
The non–phenolic fraction obtained from the gurn resin of Boswellia serrata Roxb. was found to exhibit marked sedative and analgesic effects. The drug produced a reduction in the spontaneous motor activity and caused ptosis in rats. A significant analgesic effect was observed as evaluated by both the hot–wire and the mechanical pressure methods. These effect started within 30 minutes and lasted for about 2 hours. Nalorphine caused only an insignificant antagonism to the analgesic effect of the drug. The fraction potentiated the secobarbitone–induced hypnosis in rats. The secondary–conditioned response (SCR) was specifically blocked in the trained rats, whereas the conditioned–avoidance response (CAR) was not significantly affected.
Article
1. Fenclozic acid (2-(4-chlorophenyl)thiazol-4-ylacetic acid; I.C.I. 54,450; "Myalex") is one representative of a new class of compounds with antiinflammatory, analgesic and antipyretic properties as evidenced by its activity in a variety of tests in rats, mice and guinea-pigs.2. In tests of short duration the potency of fenclozic acid is similar to that of phenylbutazone.3. In tests of longer duration fenclozic acid is more potent than phenylbutazone.4. The activity of fenclozic acid is not mediated by stimulation of the adrenals and the compound is devoid of corticosteroid-like activity.
Article
A method is presented for measuring the edema induced by injection of 0.05 ml of 1% solution of carrageenin, an extract of Chondrus, into the plantar tissues of the hind paw of the rat. Peak edema develops within the first 3 to 4 hours, and is inhibited by pretreatment of the animals by single oral doses of antiinflammatory agents, steroid or non-steroid. Log dose responses to drugs are linear and parallel, and yield potency ratios with relatively narrow confidence limits. The potency ratios obtained for aspirin, phenylbutazone and hydrocortisone are fairly close to the ratios of their respective daily doses in the treatment of rheumatic disease. A potent antihistaminic-antiserotonin compound, cyproheptadine, is without effect on carrageenin-induced edema.
Arthritis induced in rats by mycobacterial adjuvant has been used for the study of compounds of known value in the treatment of rheumatoid arthritis in man. The development of the arthritic syndrome in treated and control rats was followed by measuring the changes in foot thickness of both hind-feet with a micrometer. This method allowed the effect of anti-inflammatory compounds to be expressed quantitatively. Anti-inflammatory activity was readily observed in certain steroids, pyrazolidines, salicylates and sodium aurothiomalate. Chloroquine and hydroxychloroquine were inactive. The inhibition obtained by daily treatment with the steroid paramethasone disappeared when treatment was withdrawn.
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